CA3182864A1 - Methods and compositions for treating chemotherapy-induced diarrhea - Google Patents

Info

Publication number

CA3182864A1

CA3182864A1 CA3182864A CA3182864A CA3182864A1 CA 3182864 A1 CA3182864 A1 CA 3182864A1 CA 3182864 A CA3182864 A CA 3182864A CA 3182864 A CA3182864 A CA 3182864A CA 3182864 A1 CA3182864 A1 CA 3182864A1

Authority

CA

Canada

Prior art keywords

crofelemer

cancer

chemotherapy

diarrhea

per day

Prior art date

2020-06-19

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Pending

Links

• Espacenet
• Global Dossier
• CIPO
• Discuss

• 206010012735 Diarrhoea Diseases 0.000 title claims abstract description 122
• 238000000034 method Methods 0.000 title claims abstract description 85
• 238000002512 chemotherapy Methods 0.000 title claims description 90
• 239000000203 mixture Substances 0.000 title claims description 79
• 229920001393 Crofelemer Polymers 0.000 claims abstract description 211
• ADNPLDHMAVUMIW-CUZNLEPHSA-N substance P Chemical group C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 ADNPLDHMAVUMIW-CUZNLEPHSA-N 0.000 claims abstract description 211
• 229940047615 crofelemer Drugs 0.000 claims abstract description 210
• 238000011282 treatment Methods 0.000 claims abstract description 123
• 208000024891 symptom Diseases 0.000 claims abstract description 28
• 239000003112 inhibitor Substances 0.000 claims abstract description 24
• 208000002193 Pain Diseases 0.000 claims abstract description 4
• 230000033001 locomotion Effects 0.000 claims description 43
• 230000007423 decrease Effects 0.000 claims description 40
• 229950008835 neratinib Drugs 0.000 claims description 34
• ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 claims description 34
• 206010028980 Neoplasm Diseases 0.000 claims description 31
• 201000011510 cancer Diseases 0.000 claims description 30
• 241000282414 Homo sapiens Species 0.000 claims description 24
• -1 afatninib Chemical compound 0.000 claims description 21
• 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 21
• 101000851181 Homo sapiens Epidermal growth factor receptor Proteins 0.000 claims description 20
• 239000012829 chemotherapy agent Substances 0.000 claims description 19
• 239000006186 oral dosage form Substances 0.000 claims description 19
• 229960000575 trastuzumab Drugs 0.000 claims description 19
• 239000002246 antineoplastic agent Substances 0.000 claims description 17
• 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 17
• 229960002087 pertuzumab Drugs 0.000 claims description 16
• 230000006872 improvement Effects 0.000 claims description 15
• 239000003795 chemical substances by application Substances 0.000 claims description 14
• 239000005551 L01XE03 - Erlotinib Substances 0.000 claims description 13
• AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 13
• 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 11
• ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 11
• BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims description 11
• 229960001433 erlotinib Drugs 0.000 claims description 10
• BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims description 10
• RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 10
• 239000005517 L01XE01 - Imatinib Substances 0.000 claims description 9
• 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 9
• 229930012538 Paclitaxel Natural products 0.000 claims description 9
• RITAVMQDGBJQJZ-FMIVXFBMSA-N axitinib Chemical compound CNC(=O)C1=CC=CC=C1SC1=CC=C(C(\C=C\C=2N=CC=CC=2)=NN2)C2=C1 RITAVMQDGBJQJZ-FMIVXFBMSA-N 0.000 claims description 9
• 229940127089 cytotoxic agent Drugs 0.000 claims description 9
• 229960003668 docetaxel Drugs 0.000 claims description 9
• XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims description 9
• KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims description 9
• 229960004891 lapatinib Drugs 0.000 claims description 9
• 229960001592 paclitaxel Drugs 0.000 claims description 9
• 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims description 9
• 206010006187 Breast cancer Diseases 0.000 claims description 8
• 208000026310 Breast neoplasm Diseases 0.000 claims description 8
• 239000002146 L01XE16 - Crizotinib Substances 0.000 claims description 8
• 230000000973 chemotherapeutic effect Effects 0.000 claims description 8
• KTEIFNKAUNYNJU-GFCCVEGCSA-N crizotinib Chemical compound O([C@H](C)C=1C(=C(F)C=CC=1Cl)Cl)C(C(=NC=1)N)=CC=1C(=C1)C=NN1C1CCNCC1 KTEIFNKAUNYNJU-GFCCVEGCSA-N 0.000 claims description 8
• 239000003798 L01XE11 - Pazopanib Substances 0.000 claims description 7
• 229960003005 axitinib Drugs 0.000 claims description 7
• LVXJQMNHJWSHET-AATRIKPKSA-N dacomitinib Chemical compound C=12C=C(NC(=O)\C=C\CN3CCCCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 LVXJQMNHJWSHET-AATRIKPKSA-N 0.000 claims description 7
• 229960002584 gefitinib Drugs 0.000 claims description 7
• 229960002411 imatinib Drugs 0.000 claims description 7
• CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims description 7
• MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims description 6
• ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims description 6
• 208000034347 Faecal incontinence Diseases 0.000 claims description 6
• 239000002147 L01XE04 - Sunitinib Substances 0.000 claims description 6
• 239000005511 L01XE05 - Sorafenib Substances 0.000 claims description 6
• 239000002067 L01XE06 - Dasatinib Substances 0.000 claims description 6
• 229940123237 Taxane Drugs 0.000 claims description 6
• 231100000026 common toxicity Toxicity 0.000 claims description 6
• 229960005061 crizotinib Drugs 0.000 claims description 6
• 229940022353 herceptin Drugs 0.000 claims description 6
• 102100033793 ALK tyrosine kinase receptor Human genes 0.000 claims description 5
• 101710168331 ALK tyrosine kinase receptor Proteins 0.000 claims description 5
• 102000003903 Cyclin-dependent kinases Human genes 0.000 claims description 5
• 108090000266 Cyclin-dependent kinases Proteins 0.000 claims description 5
• 239000002145 L01XE14 - Bosutinib Substances 0.000 claims description 5
• 229960003736 bosutinib Drugs 0.000 claims description 5
• UBPYILGKFZZVDX-UHFFFAOYSA-N bosutinib Chemical compound C1=C(Cl)C(OC)=CC(NC=2C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=CC=2C#N)=C1Cl UBPYILGKFZZVDX-UHFFFAOYSA-N 0.000 claims description 5
• 229960004562 carboplatin Drugs 0.000 claims description 5
• 229960002448 dasatinib Drugs 0.000 claims description 5
• 229960000639 pazopanib Drugs 0.000 claims description 5
• 229910052697 platinum Inorganic materials 0.000 claims description 5
• 229960003787 sorafenib Drugs 0.000 claims description 5
• 239000005536 L01XE08 - Nilotinib Substances 0.000 claims description 4
• 239000002144 L01XE18 - Ruxolitinib Substances 0.000 claims description 4
• 239000002176 L01XE26 - Cabozantinib Substances 0.000 claims description 4
• 230000003187 abdominal effect Effects 0.000 claims description 4
• 239000002168 alkylating agent Substances 0.000 claims description 4
• 229960000106 biosimilars Drugs 0.000 claims description 4
• 229960001292 cabozantinib Drugs 0.000 claims description 4
• ONIQOQHATWINJY-UHFFFAOYSA-N cabozantinib Chemical compound C=12C=C(OC)C(OC)=CC2=NC=CC=1OC(C=C1)=CC=C1NC(=O)C1(C(=O)NC=2C=CC(F)=CC=2)CC1 ONIQOQHATWINJY-UHFFFAOYSA-N 0.000 claims description 4
• 229940043355 kinase inhibitor Drugs 0.000 claims description 4
• 229960001346 nilotinib Drugs 0.000 claims description 4
• HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims description 4
• 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims description 4
• 239000003757 phosphotransferase inhibitor Substances 0.000 claims description 4
• 229960000215 ruxolitinib Drugs 0.000 claims description 4
• HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical compound C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims description 4
• 229960001796 sunitinib Drugs 0.000 claims description 4
• WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 claims description 4
• 208000003174 Brain Neoplasms Diseases 0.000 claims description 3
• 206010009944 Colon cancer Diseases 0.000 claims description 3
• 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
• 108090000323 DNA Topoisomerases Proteins 0.000 claims description 3
• 102000003915 DNA Topoisomerases Human genes 0.000 claims description 3
• 102000007537 Type II DNA Topoisomerases Human genes 0.000 claims description 3
• 108010046308 Type II DNA Topoisomerases Proteins 0.000 claims description 3
• 208000002495 Uterine Neoplasms Diseases 0.000 claims description 3
• 229940100198 alkylating agent Drugs 0.000 claims description 3
• 230000001668 ameliorated effect Effects 0.000 claims description 3
• 229940045799 anthracyclines and related substance Drugs 0.000 claims description 3
• 229960001602 ceritinib Drugs 0.000 claims description 3
• VERWOWGGCGHDQE-UHFFFAOYSA-N ceritinib Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1C1CCNCC1 VERWOWGGCGHDQE-UHFFFAOYSA-N 0.000 claims description 3
• 229940127096 cytoskeletal disruptor Drugs 0.000 claims description 3
• 229950002205 dacomitinib Drugs 0.000 claims description 3
• 229930013356 epothilone Natural products 0.000 claims description 3
• HESCAJZNRMSMJG-KKQRBIROSA-N epothilone A Chemical class C/C([C@@H]1C[C@@H]2O[C@@H]2CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 HESCAJZNRMSMJG-KKQRBIROSA-N 0.000 claims description 3
• 239000003276 histone deacetylase inhibitor Substances 0.000 claims description 3
• 229940121372 histone deacetylase inhibitor Drugs 0.000 claims description 3
• 229960003784 lenvatinib Drugs 0.000 claims description 3
• WOSKHXYHFSIKNG-UHFFFAOYSA-N lenvatinib Chemical compound C=12C=C(C(N)=O)C(OC)=CC2=NC=CC=1OC(C=C1Cl)=CC=C1NC(=O)NC1CC1 WOSKHXYHFSIKNG-UHFFFAOYSA-N 0.000 claims description 3
• 125000003729 nucleotide group Chemical group 0.000 claims description 3
• 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 claims description 3
• 239000003910 polypeptide antibiotic agent Substances 0.000 claims description 3
• 239000002243 precursor Substances 0.000 claims description 3
• 206010046766 uterine cancer Diseases 0.000 claims description 3
• STUWGJZDJHPWGZ-LBPRGKRZSA-N (2S)-N1-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)-4-pyridinyl]-2-thiazolyl]pyrrolidine-1,2-dicarboxamide Chemical group S1C(C=2C=C(N=CC=2)C(C)(C)C(F)(F)F)=C(C)N=C1NC(=O)N1CCC[C@H]1C(N)=O STUWGJZDJHPWGZ-LBPRGKRZSA-N 0.000 claims description 2
• SDEAXTCZPQIFQM-UHFFFAOYSA-N 6-n-(4,4-dimethyl-5h-1,3-oxazol-2-yl)-4-n-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]quinazoline-4,6-diamine Chemical compound C=1C=C(OC2=CC3=NC=NN3C=C2)C(C)=CC=1NC(C1=C2)=NC=NC1=CC=C2NC1=NC(C)(C)CO1 SDEAXTCZPQIFQM-UHFFFAOYSA-N 0.000 claims description 2
• 206010003571 Astrocytoma Diseases 0.000 claims description 2
• 206010005003 Bladder cancer Diseases 0.000 claims description 2
• 206010005949 Bone cancer Diseases 0.000 claims description 2
• 208000018084 Bone neoplasm Diseases 0.000 claims description 2
• 206010006143 Brain stem glioma Diseases 0.000 claims description 2
• 201000009030 Carcinoma Diseases 0.000 claims description 2
• 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
• 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
• 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 2
• 206010073069 Hepatic cancer Diseases 0.000 claims description 2
• 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
• 239000002118 L01XE12 - Vandetanib Substances 0.000 claims description 2
• 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
• 206010025323 Lymphomas Diseases 0.000 claims description 2
• 206010027406 Mesothelioma Diseases 0.000 claims description 2
• 206010027476 Metastases Diseases 0.000 claims description 2
• 208000003445 Mouth Neoplasms Diseases 0.000 claims description 2
• 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
• 206010031096 Oropharyngeal cancer Diseases 0.000 claims description 2
• 206010057444 Oropharyngeal neoplasm Diseases 0.000 claims description 2
• 206010033128 Ovarian cancer Diseases 0.000 claims description 2
• 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
• 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
• 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
• 206010060862 Prostate cancer Diseases 0.000 claims description 2
• 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
• 206010038389 Renal cancer Diseases 0.000 claims description 2
• 206010039491 Sarcoma Diseases 0.000 claims description 2
• 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
• 208000024313 Testicular Neoplasms Diseases 0.000 claims description 2
• 206010057644 Testis cancer Diseases 0.000 claims description 2
• 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
• 206010062129 Tongue neoplasm Diseases 0.000 claims description 2
• 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
• 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
• 229950001573 abemaciclib Drugs 0.000 claims description 2
• 229950010482 alpelisib Drugs 0.000 claims description 2
• 201000010881 cervical cancer Diseases 0.000 claims description 2
• 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims description 2
• 201000004101 esophageal cancer Diseases 0.000 claims description 2
• 201000010175 gallbladder cancer Diseases 0.000 claims description 2
• 206010017758 gastric cancer Diseases 0.000 claims description 2
• 201000010536 head and neck cancer Diseases 0.000 claims description 2
• 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
• 201000010982 kidney cancer Diseases 0.000 claims description 2
• 208000032839 leukemia Diseases 0.000 claims description 2
• 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims description 2
• 201000007270 liver cancer Diseases 0.000 claims description 2
• 208000014018 liver neoplasm Diseases 0.000 claims description 2
• 201000005202 lung cancer Diseases 0.000 claims description 2
• 208000020816 lung neoplasm Diseases 0.000 claims description 2
• 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
• 201000001441 melanoma Diseases 0.000 claims description 2
• 206010027191 meningioma Diseases 0.000 claims description 2
• 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
• UZWDCWONPYILKI-UHFFFAOYSA-N n-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine Chemical compound C1CN(CC)CCN1CC(C=N1)=CC=C1NC1=NC=C(F)C(C=2C=C3N(C(C)C)C(C)=NC3=C(F)C=2)=N1 UZWDCWONPYILKI-UHFFFAOYSA-N 0.000 claims description 2
• 201000006958 oropharynx cancer Diseases 0.000 claims description 2
• 201000002528 pancreatic cancer Diseases 0.000 claims description 2
• 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
• 201000002628 peritoneum cancer Diseases 0.000 claims description 2
• 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
• 201000011549 stomach cancer Diseases 0.000 claims description 2
• 201000003120 testicular cancer Diseases 0.000 claims description 2
• 201000002510 thyroid cancer Diseases 0.000 claims description 2
• 201000006134 tongue cancer Diseases 0.000 claims description 2
• 229950003463 tucatinib Drugs 0.000 claims description 2
• 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
• 229960000241 vandetanib Drugs 0.000 claims description 2
• UHTHHESEBZOYNR-UHFFFAOYSA-N vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 claims description 2
• 229960001611 alectinib Drugs 0.000 claims 1
• KDGFLJKFZUIJMX-UHFFFAOYSA-N alectinib Chemical compound CCC1=CC=2C(=O)C(C3=CC=C(C=C3N3)C#N)=C3C(C)(C)C=2C=C1N(CC1)CCC1N1CCOCC1 KDGFLJKFZUIJMX-UHFFFAOYSA-N 0.000 claims 1
• 190000008236 carboplatin Chemical compound 0.000 claims 1
• VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 abstract description 3
• 206010000059 abdominal discomfort Diseases 0.000 abstract description 3
• 241000282472 Canis lupus familiaris Species 0.000 description 129
• 229920000642 polymer Polymers 0.000 description 33
• 210000003608 fece Anatomy 0.000 description 32
• 230000000694 effects Effects 0.000 description 31
• 239000003814 drug Substances 0.000 description 30
• 239000003826 tablet Substances 0.000 description 30
• JPFCOVZKLAXXOE-XBNSMERZSA-N (3r)-2-(3,5-dihydroxy-4-methoxyphenyl)-8-[(2r,3r,4r)-3,5,7-trihydroxy-2-(4-hydroxyphenyl)-3,4-dihydro-2h-chromen-4-yl]-3,4-dihydro-2h-chromene-3,5,7-triol Chemical compound C1=C(O)C(OC)=C(O)C=C1C1[C@H](O)CC(C(O)=CC(O)=C2[C@H]3C4=C(O)C=C(O)C=C4O[C@@H]([C@@H]3O)C=3C=CC(O)=CC=3)=C2O1 JPFCOVZKLAXXOE-XBNSMERZSA-N 0.000 description 29
• 229920001991 Proanthocyanidin Polymers 0.000 description 29
• 239000003819 Toceranib Substances 0.000 description 27
• 230000002550 fecal effect Effects 0.000 description 25
• 229940079593 drug Drugs 0.000 description 22
• 150000001875 compounds Chemical class 0.000 description 20
• AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 19
• 238000009472 formulation Methods 0.000 description 17
• 239000008194 pharmaceutical composition Substances 0.000 description 16
• 210000002784 stomach Anatomy 0.000 description 16
• 229940068196 placebo Drugs 0.000 description 15
• 239000000902 placebo Substances 0.000 description 15
• AOORBROPMMRREB-HBPAQXCTSA-N 5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-n-(2-pyrrolidin-1-ylethyl)-1h-pyrrole-3-carboxamide;phosphoric acid Chemical compound OP(O)(O)=O.CC=1NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C(C)C=1C(=O)NCCN1CCCC1 AOORBROPMMRREB-HBPAQXCTSA-N 0.000 description 14
• 230000009467 reduction Effects 0.000 description 14
• 229960005432 toceranib phosphate Drugs 0.000 description 14
• SRSGVKWWVXWSJT-ATVHPVEESA-N 5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-n-(2-pyrrolidin-1-ylethyl)-1h-pyrrole-3-carboxamide Chemical compound CC=1NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C(C)C=1C(=O)NCCN1CCCC1 SRSGVKWWVXWSJT-ATVHPVEESA-N 0.000 description 13
• 238000012216 screening Methods 0.000 description 13
• 229940090244 palladia Drugs 0.000 description 12
• 244000168525 Croton tiglium Species 0.000 description 11
• 239000002552 dosage form Substances 0.000 description 11
• 239000002702 enteric coating Substances 0.000 description 11
• 238000009505 enteric coating Methods 0.000 description 11
• 238000002560 therapeutic procedure Methods 0.000 description 11
• 241001648676 Croton lechleri Species 0.000 description 10
• 230000002411 adverse Effects 0.000 description 10
• 238000011156 evaluation Methods 0.000 description 10
• DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 9
• 239000002775 capsule Substances 0.000 description 9
• 239000000843 powder Substances 0.000 description 9
• PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 8
• 241001465754 Metazoa Species 0.000 description 8
• 239000002253 acid Substances 0.000 description 8
• 239000003560 cancer drug Substances 0.000 description 8
• 230000003247 decreasing effect Effects 0.000 description 8
• 238000002483 medication Methods 0.000 description 8
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 7
• 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 7
• 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 7
• 238000004458 analytical method Methods 0.000 description 7
• 230000008901 benefit Effects 0.000 description 7
• 230000037396 body weight Effects 0.000 description 7
• 229920002770 condensed tannin Polymers 0.000 description 7
• 229960004679 doxorubicin Drugs 0.000 description 7
• 230000003993 interaction Effects 0.000 description 7
• 239000002904 solvent Substances 0.000 description 7
• FQZYTYWMLGAPFJ-OQKDUQJOSA-N tamoxifen citrate Chemical compound [H+].[H+].[H+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 FQZYTYWMLGAPFJ-OQKDUQJOSA-N 0.000 description 7
• 229940124597 therapeutic agent Drugs 0.000 description 7
• 230000000699 topical effect Effects 0.000 description 7
• CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 6
• 241001246270 Calophyllum Species 0.000 description 6
• GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 description 6
• 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 description 6
• XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 6
• GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 description 6
• 101000653548 Homo sapiens Trichoplein keratin filament-binding protein Proteins 0.000 description 6
• 102100030645 Trichoplein keratin filament-binding protein Human genes 0.000 description 6
• 230000001142 anti-diarrhea Effects 0.000 description 6
• 230000008859 change Effects 0.000 description 6
• 229940044683 chemotherapy drug Drugs 0.000 description 6
• 238000000576 coating method Methods 0.000 description 6
• 239000003937 drug carrier Substances 0.000 description 6
• 229960002949 fluorouracil Drugs 0.000 description 6
• 230000036541 health Effects 0.000 description 6
• HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
• 239000002674 ointment Substances 0.000 description 6
• 239000000546 pharmaceutical excipient Substances 0.000 description 6
• 239000000047 product Substances 0.000 description 6
• 102000005962 receptors Human genes 0.000 description 6
• 108020003175 receptors Proteins 0.000 description 6
• FNHKPVJBJVTLMP-UHFFFAOYSA-N regorafenib Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=C(F)C(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 FNHKPVJBJVTLMP-UHFFFAOYSA-N 0.000 description 6
• YCCHNFGPIFYNTF-UHFFFAOYSA-N tertiary cymene hydroperoxide Natural products CC1=CC=C(C(C)(C)OO)C=C1 YCCHNFGPIFYNTF-UHFFFAOYSA-N 0.000 description 6
• 238000012360 testing method Methods 0.000 description 6
• WLPUWLXVBWGYMZ-UHFFFAOYSA-N tricyclohexylphosphine Chemical compound C1CCCCC1P(C1CCCCC1)C1CCCCC1 WLPUWLXVBWGYMZ-UHFFFAOYSA-N 0.000 description 6
• HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 description 5
• VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 description 5
• 241000282412 Homo Species 0.000 description 5
• BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 description 5
• 108010081667 aflibercept Proteins 0.000 description 5
• DVQHYTBCTGYNNN-UHFFFAOYSA-N azane;cyclobutane-1,1-dicarboxylic acid;platinum Chemical compound N.N.[Pt].OC(=O)C1(C(O)=O)CCC1 DVQHYTBCTGYNNN-UHFFFAOYSA-N 0.000 description 5
• BMQGVNUXMIRLCK-OAGWZNDDSA-N cabazitaxel Chemical compound O([C@H]1[C@@H]2[C@]3(OC(C)=O)CO[C@@H]3C[C@@H]([C@]2(C(=O)[C@H](OC)C2=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=3C=CC=CC=3)C[C@]1(O)C2(C)C)C)OC)C(=O)C1=CC=CC=C1 BMQGVNUXMIRLCK-OAGWZNDDSA-N 0.000 description 5
• 210000004027 cell Anatomy 0.000 description 5
• 239000006071 cream Substances 0.000 description 5
• UFNVPOGXISZXJD-JBQZKEIOSA-N eribulin Chemical compound C([C@H]1CC[C@@H]2O[C@@H]3[C@H]4O[C@@H]5C[C@](O[C@H]4[C@H]2O1)(O[C@@H]53)CC[C@@H]1O[C@H](C(C1)=C)CC1)C(=O)C[C@@H]2[C@@H](OC)[C@@H](C[C@H](O)CN)O[C@H]2C[C@@H]2C(=C)[C@H](C)C[C@H]1O2 UFNVPOGXISZXJD-JBQZKEIOSA-N 0.000 description 5
• 239000012530 fluid Substances 0.000 description 5
• 210000001035 gastrointestinal tract Anatomy 0.000 description 5
• SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 description 5
• GURKHSYORGJETM-WAQYZQTGSA-N irinotecan hydrochloride (anhydrous) Chemical compound Cl.C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 GURKHSYORGJETM-WAQYZQTGSA-N 0.000 description 5
• RDOIQAHITMMDAJ-UHFFFAOYSA-N loperamide Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)N(C)C)CCN(CC1)CCC1(O)C1=CC=C(Cl)C=C1 RDOIQAHITMMDAJ-UHFFFAOYSA-N 0.000 description 5
• 229960001571 loperamide Drugs 0.000 description 5
• 239000000463 material Substances 0.000 description 5
• 239000000523 sample Substances 0.000 description 5
• 239000000243 solution Substances 0.000 description 5
• 239000007921 spray Substances 0.000 description 5
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
• 206010067484 Adverse reaction Diseases 0.000 description 4
• VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
• GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 description 4
• 108020004414 DNA Proteins 0.000 description 4
• 241000196324 Embryophyta Species 0.000 description 4
• ZPLQIPFOCGIIHV-UHFFFAOYSA-N Gimeracil Chemical compound OC1=CC(=O)C(Cl)=CN1 ZPLQIPFOCGIIHV-UHFFFAOYSA-N 0.000 description 4
• NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 description 4
• 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 4
• 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 4
• 239000004480 active ingredient Substances 0.000 description 4
• 239000008186 active pharmaceutical agent Substances 0.000 description 4
• 230000006838 adverse reaction Effects 0.000 description 4
• WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 4
• 239000003963 antioxidant agent Substances 0.000 description 4
• 235000006708 antioxidants Nutrition 0.000 description 4
• 238000003556 assay Methods 0.000 description 4
• 229960004117 capecitabine Drugs 0.000 description 4
• 239000011248 coating agent Substances 0.000 description 4
• PPQREHKVAOVYBT-UHFFFAOYSA-H dialuminum;tricarbonate Chemical compound [Al+3].[Al+3].[O-]C([O-])=O.[O-]C([O-])=O.[O-]C([O-])=O PPQREHKVAOVYBT-UHFFFAOYSA-H 0.000 description 4
• 201000010099 disease Diseases 0.000 description 4
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
• 235000019441 ethanol Nutrition 0.000 description 4
• 230000007717 exclusion Effects 0.000 description 4
• 239000000284 extract Substances 0.000 description 4
• 230000006870 function Effects 0.000 description 4
• 230000002496 gastric effect Effects 0.000 description 4
• 229950009822 gimeracil Drugs 0.000 description 4
• 239000008187 granular material Substances 0.000 description 4
• 229960004768 irinotecan Drugs 0.000 description 4
• 229960005415 pasireotide Drugs 0.000 description 4
• VMZMNAABQBOLAK-DBILLSOUSA-N pasireotide Chemical compound C([C@H]1C(=O)N2C[C@@H](C[C@H]2C(=O)N[C@H](C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@H](C(N[C@@H](CC=2C=CC(OCC=3C=CC=CC=3)=CC=2)C(=O)N1)=O)CCCCN)C=1C=CC=CC=1)OC(=O)NCCN)C1=CC=CC=C1 VMZMNAABQBOLAK-DBILLSOUSA-N 0.000 description 4
• 108700017947 pasireotide Proteins 0.000 description 4
• VCMMXZQDRFWYSE-UHFFFAOYSA-N plumbagin Chemical compound C1=CC=C2C(=O)C(C)=CC(=O)C2=C1O VCMMXZQDRFWYSE-UHFFFAOYSA-N 0.000 description 4
• 229920001223 polyethylene glycol Polymers 0.000 description 4
• 238000002360 preparation method Methods 0.000 description 4
• 108090000623 proteins and genes Proteins 0.000 description 4
• 102000004169 proteins and genes Human genes 0.000 description 4
• 230000028327 secretion Effects 0.000 description 4
• 208000026775 severe diarrhea Diseases 0.000 description 4
• 239000000126 substance Substances 0.000 description 4
• 239000000725 suspension Substances 0.000 description 4
• 239000000454 talc Substances 0.000 description 4
• 235000012222 talc Nutrition 0.000 description 4
• 229910052623 talc Inorganic materials 0.000 description 4
• WFWLQNSHRPWKFK-ZCFIWIBFSA-N tegafur Chemical compound O=C1NC(=O)C(F)=CN1[C@@H]1OCCC1 WFWLQNSHRPWKFK-ZCFIWIBFSA-N 0.000 description 4
• 229960001674 tegafur Drugs 0.000 description 4
• 230000008673 vomiting Effects 0.000 description 4
• LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 description 3
• RYYCJUAHISIHTL-UHFFFAOYSA-N 5-azaorotic acid Chemical compound OC(=O)C1=NC(=O)NC(=O)N1 RYYCJUAHISIHTL-UHFFFAOYSA-N 0.000 description 3
• QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 3
• 241000416162 Astragalus gummifer Species 0.000 description 3
• 108010062745 Chloride Channels Proteins 0.000 description 3
• 102000011045 Chloride Channels Human genes 0.000 description 3
• 102000012605 Cystic Fibrosis Transmembrane Conductance Regulator Human genes 0.000 description 3
• FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 3
• FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 3
• YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
• 208000017891 HER2 positive breast carcinoma Diseases 0.000 description 3
• KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
• 239000002138 L01XE21 - Regorafenib Substances 0.000 description 3
• OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
• BAPJBEWLBFYGME-UHFFFAOYSA-N Methyl acrylate Chemical compound COC(=O)C=C BAPJBEWLBFYGME-UHFFFAOYSA-N 0.000 description 3
• 102000003923 Protein Kinase C Human genes 0.000 description 3
• 108090000315 Protein Kinase C Proteins 0.000 description 3
• 229920002472 Starch Polymers 0.000 description 3
• 229920001615 Tragacanth Polymers 0.000 description 3
• 230000002378 acidificating effect Effects 0.000 description 3
• 230000009471 action Effects 0.000 description 3
• 201000009840 acute diarrhea Diseases 0.000 description 3
• 239000000443 aerosol Substances 0.000 description 3
• YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 description 3
• 230000000118 anti-neoplastic effect Effects 0.000 description 3
• 239000003443 antiviral agent Substances 0.000 description 3
• 229960000397 bevacizumab Drugs 0.000 description 3
• 229960000997 bicalutamide Drugs 0.000 description 3
• 229960001573 cabazitaxel Drugs 0.000 description 3
• 230000001413 cellular effect Effects 0.000 description 3
• 238000009104 chemotherapy regimen Methods 0.000 description 3
• 230000001684 chronic effect Effects 0.000 description 3
• KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
• 229960002465 dabrafenib Drugs 0.000 description 3
• BFSMGDJOXZAERB-UHFFFAOYSA-N dabrafenib Chemical compound S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 BFSMGDJOXZAERB-UHFFFAOYSA-N 0.000 description 3
• 230000018044 dehydration Effects 0.000 description 3
• 238000006297 dehydration reaction Methods 0.000 description 3
• 230000003111 delayed effect Effects 0.000 description 3
• 238000013461 design Methods 0.000 description 3
• 230000000741 diarrhetic effect Effects 0.000 description 3
• XMOCLSLCDHWDHP-IUODEOHRSA-N epi-Gallocatechin Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@H]2O)=CC(O)=C(O)C(O)=C1 XMOCLSLCDHWDHP-IUODEOHRSA-N 0.000 description 3
• 229960003649 eribulin Drugs 0.000 description 3
• 229960005167 everolimus Drugs 0.000 description 3
• 235000013305 food Nutrition 0.000 description 3
• 229960002258 fulvestrant Drugs 0.000 description 3
• 239000000499 gel Substances 0.000 description 3
• 229960005277 gemcitabine Drugs 0.000 description 3
• 235000011187 glycerol Nutrition 0.000 description 3
• 239000004615 ingredient Substances 0.000 description 3
• 238000002347 injection Methods 0.000 description 3
• 239000007924 injection Substances 0.000 description 3
• 239000004816 latex Substances 0.000 description 3
• 229920000126 latex Polymers 0.000 description 3
• 239000007788 liquid Substances 0.000 description 3
• 239000006210 lotion Substances 0.000 description 3
• 239000000314 lubricant Substances 0.000 description 3
• VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 description 3
• 239000000347 magnesium hydroxide Substances 0.000 description 3
• 229910001862 magnesium hydroxide Inorganic materials 0.000 description 3
• 235000019359 magnesium stearate Nutrition 0.000 description 3
• 238000004519 manufacturing process Methods 0.000 description 3
• 239000000178 monomer Substances 0.000 description 3
• LBWFXVZLPYTWQI-IPOVEDGCSA-N n-[2-(diethylamino)ethyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide;(2s)-2-hydroxybutanedioic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O.CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C LBWFXVZLPYTWQI-IPOVEDGCSA-N 0.000 description 3
• 239000003921 oil Substances 0.000 description 3
• 235000019198 oils Nutrition 0.000 description 3
• 239000004006 olive oil Substances 0.000 description 3
• 210000000056 organ Anatomy 0.000 description 3
• 229950000193 oteracil Drugs 0.000 description 3
• 229960001756 oxaliplatin Drugs 0.000 description 3
• DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 description 3
• NEEFMPSSNFRRNC-HQUONIRXSA-N pasireotide aspartate Chemical compound OC(=O)[C@@H](N)CC(O)=O.OC(=O)[C@@H](N)CC(O)=O.C([C@H]1C(=O)N2C[C@@H](C[C@H]2C(=O)N[C@H](C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@H](C(N[C@@H](CC=2C=CC(OCC=3C=CC=CC=3)=CC=2)C(=O)N1)=O)CCCCN)C=1C=CC=CC=1)OC(=O)NCCN)C1=CC=CC=C1 NEEFMPSSNFRRNC-HQUONIRXSA-N 0.000 description 3
• 239000006072 paste Substances 0.000 description 3
• 230000037361 pathway Effects 0.000 description 3
• QOFFJEBXNKRSPX-ZDUSSCGKSA-N pemetrexed Chemical compound C1=N[C]2NC(N)=NC(=O)C2=C1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QOFFJEBXNKRSPX-ZDUSSCGKSA-N 0.000 description 3
• 229960005079 pemetrexed Drugs 0.000 description 3
• 230000000144 pharmacologic effect Effects 0.000 description 3
• 230000026731 phosphorylation Effects 0.000 description 3
• 238000006366 phosphorylation reaction Methods 0.000 description 3
• 229960004063 propylene glycol Drugs 0.000 description 3
• 235000018102 proteins Nutrition 0.000 description 3
• 230000002829 reductive effect Effects 0.000 description 3
• 229960004836 regorafenib Drugs 0.000 description 3
• 238000012552 review Methods 0.000 description 3
• OHRURASPPZQGQM-GCCNXGTGSA-N romidepsin Chemical compound O1C(=O)[C@H](C(C)C)NC(=O)C(=C/C)/NC(=O)[C@H]2CSSCC\C=C\[C@@H]1CC(=O)N[C@H](C(C)C)C(=O)N2 OHRURASPPZQGQM-GCCNXGTGSA-N 0.000 description 3
• OHRURASPPZQGQM-UHFFFAOYSA-N romidepsin Natural products O1C(=O)C(C(C)C)NC(=O)C(=CC)NC(=O)C2CSSCCC=CC1CC(=O)NC(C(C)C)C(=O)N2 OHRURASPPZQGQM-UHFFFAOYSA-N 0.000 description 3
• 108010091666 romidepsin Proteins 0.000 description 3
• 201000009881 secretory diarrhea Diseases 0.000 description 3
• 229940050423 signifor Drugs 0.000 description 3
• 210000000813 small intestine Anatomy 0.000 description 3
• 239000007787 solid Substances 0.000 description 3
• 235000010356 sorbitol Nutrition 0.000 description 3
• 239000000600 sorbitol Substances 0.000 description 3
• 241000894007 species Species 0.000 description 3
• 235000019698 starch Nutrition 0.000 description 3
• 239000000829 suppository Substances 0.000 description 3
• 229960003454 tamoxifen citrate Drugs 0.000 description 3
• 229940120982 tarceva Drugs 0.000 description 3
• DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 3
• 229960004964 temozolomide Drugs 0.000 description 3
• 235000010487 tragacanth Nutrition 0.000 description 3
• 239000000196 tragacanth Substances 0.000 description 3
• 229940116362 tragacanth Drugs 0.000 description 3
• 238000002562 urinalysis Methods 0.000 description 3
• 239000003981 vehicle Substances 0.000 description 3
• 229960003862 vemurafenib Drugs 0.000 description 3
• GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 description 3
• 210000004916 vomit Anatomy 0.000 description 3
• 239000001993 wax Substances 0.000 description 3
• 229960002760 ziv-aflibercept Drugs 0.000 description 3
• PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
• JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 2
• DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 description 2
• 229920003067 (meth)acrylic acid ester copolymer Polymers 0.000 description 2
• IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 2
• RWHRFHQRVDUPIK-UHFFFAOYSA-N 50867-57-7 Chemical compound CC(=C)C(O)=O.CC(=C)C(O)=O RWHRFHQRVDUPIK-UHFFFAOYSA-N 0.000 description 2
• ZKHQWZAMYRWXGA-KQYNXXCUSA-J ATP(4-) Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O)[C@@H](O)[C@H]1O ZKHQWZAMYRWXGA-KQYNXXCUSA-J 0.000 description 2
• 208000004998 Abdominal Pain Diseases 0.000 description 2
• ZKHQWZAMYRWXGA-UHFFFAOYSA-N Adenosine triphosphate Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(=O)OP(O)(=O)OP(O)(O)=O)C(O)C1O ZKHQWZAMYRWXGA-UHFFFAOYSA-N 0.000 description 2
• 229920001817 Agar Polymers 0.000 description 2
• GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
• CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
• 108010006654 Bleomycin Proteins 0.000 description 2
• 206010055113 Breast cancer metastatic Diseases 0.000 description 2
• 239000004322 Butylated hydroxytoluene Substances 0.000 description 2
• NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 2
• 229920000623 Cellulose acetate phthalate Polymers 0.000 description 2
• 206010010774 Constipation Diseases 0.000 description 2
• KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 2
• 102000001301 EGF receptor Human genes 0.000 description 2
• 108060006698 EGF receptor Proteins 0.000 description 2
• LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 2
• 102000004190 Enzymes Human genes 0.000 description 2
• 108090000790 Enzymes Proteins 0.000 description 2
• 239000001856 Ethyl cellulose Substances 0.000 description 2
• ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 2
• 108091008794 FGF receptors Proteins 0.000 description 2
• OHCQJHSOBUTRHG-KGGHGJDLSA-N FORSKOLIN Chemical compound O=C([C@@]12O)C[C@](C)(C=C)O[C@]1(C)[C@@H](OC(=O)C)[C@@H](O)[C@@H]1[C@]2(C)[C@@H](O)CCC1(C)C OHCQJHSOBUTRHG-KGGHGJDLSA-N 0.000 description 2
• 102000044168 Fibroblast Growth Factor Receptor Human genes 0.000 description 2
• 244000060234 Gmelina philippensis Species 0.000 description 2
• BLCLNMBMMGCOAS-URPVMXJPSA-N Goserelin Chemical compound C([C@@H](C(=O)N[C@H](COC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1[C@@H](CCC1)C(=O)NNC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 BLCLNMBMMGCOAS-URPVMXJPSA-N 0.000 description 2
• 108010069236 Goserelin Proteins 0.000 description 2
• 102100022623 Hepatocyte growth factor receptor Human genes 0.000 description 2
• 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 description 2
• ZMOIGGHUSNHCAB-UHFFFAOYSA-N Isoplumbagin Natural products C1=CC(O)=C2C(=O)C(C)=CC(=O)C2=C1 ZMOIGGHUSNHCAB-UHFFFAOYSA-N 0.000 description 2
• XMOCLSLCDHWDHP-UHFFFAOYSA-N L-Epigallocatechin Natural products OC1CC2=C(O)C=C(O)C=C2OC1C1=CC(O)=C(O)C(O)=C1 XMOCLSLCDHWDHP-UHFFFAOYSA-N 0.000 description 2
• GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
• VAYOSLLFUXYJDT-RDTXWAMCSA-N Lysergic acid diethylamide Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N(CC)CC)C2)=C3C2=CNC3=C1 VAYOSLLFUXYJDT-RDTXWAMCSA-N 0.000 description 2
• 108091054455 MAP kinase family Proteins 0.000 description 2
• 102000043136 MAP kinase family Human genes 0.000 description 2
• 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
• LKJPYSCBVHEWIU-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide Chemical compound C=1C=C(C#N)C(C(F)(F)F)=CC=1NC(=O)C(O)(C)CS(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-UHFFFAOYSA-N 0.000 description 2
• 108010016076 Octreotide Proteins 0.000 description 2
• 102000038030 PI3Ks Human genes 0.000 description 2
• 108091007960 PI3Ks Proteins 0.000 description 2
• NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
• 108091000080 Phosphotransferase Proteins 0.000 description 2
• 239000002202 Polyethylene glycol Substances 0.000 description 2
• ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 2
• ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 description 2
• 108010089836 Proto-Oncogene Proteins c-met Proteins 0.000 description 2
• 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 description 2
• 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 description 2
• UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
• CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
• CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 description 2
• IQFYYKKMVGJFEH-XLPZGREQSA-N Thymidine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 IQFYYKKMVGJFEH-XLPZGREQSA-N 0.000 description 2
• IVTVGDXNLFLDRM-HNNXBMFYSA-N Tomudex Chemical compound C=1C=C2NC(C)=NC(=O)C2=CC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)S1 IVTVGDXNLFLDRM-HNNXBMFYSA-N 0.000 description 2
• 206010066901 Treatment failure Diseases 0.000 description 2
• 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 description 2
• 206010047700 Vomiting Diseases 0.000 description 2
• XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
• 230000005856 abnormality Effects 0.000 description 2
• 238000010521 absorption reaction Methods 0.000 description 2
• DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 2
• 230000004913 activation Effects 0.000 description 2
• 238000009098 adjuvant therapy Methods 0.000 description 2
• 229940009456 adriamycin Drugs 0.000 description 2
• 229940042992 afinitor Drugs 0.000 description 2
• 235000010419 agar Nutrition 0.000 description 2
• 229940110282 alimta Drugs 0.000 description 2
• 229940118662 aluminum carbonate Drugs 0.000 description 2
• 229940069428 antacid Drugs 0.000 description 2
• 239000003159 antacid agent Substances 0.000 description 2
• 239000003242 anti bacterial agent Substances 0.000 description 2
• 230000001262 anti-secretory effect Effects 0.000 description 2
• 230000000840 anti-viral effect Effects 0.000 description 2
• 229940088710 antibiotic agent Drugs 0.000 description 2
• 230000006907 apoptotic process Effects 0.000 description 2
• 229940078010 arimidex Drugs 0.000 description 2
• 229940120638 avastin Drugs 0.000 description 2
• 235000012216 bentonite Nutrition 0.000 description 2
• SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 description 2
• ALPCEXCHMFUSAN-UHFFFAOYSA-N beta-Dihydroplumbagin Natural products C1=CC=C2C(=O)C(C)CC(=O)C2=C1O ALPCEXCHMFUSAN-UHFFFAOYSA-N 0.000 description 2
• 229960001561 bleomycin Drugs 0.000 description 2
• OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 description 2
• 230000000903 blocking effect Effects 0.000 description 2
• GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 description 2
• 210000000481 breast Anatomy 0.000 description 2
• 235000010354 butylated hydroxytoluene Nutrition 0.000 description 2
• 229940095259 butylated hydroxytoluene Drugs 0.000 description 2
• 229910000019 calcium carbonate Inorganic materials 0.000 description 2
• 230000005907 cancer growth Effects 0.000 description 2
• 239000012876 carrier material Substances 0.000 description 2
• 229940097647 casodex Drugs 0.000 description 2
• 235000005487 catechin Nutrition 0.000 description 2
• ADRVNXBAWSRFAJ-UHFFFAOYSA-N catechin Natural products OC1Cc2cc(O)cc(O)c2OC1c3ccc(O)c(O)c3 ADRVNXBAWSRFAJ-UHFFFAOYSA-N 0.000 description 2
• 230000004640 cellular pathway Effects 0.000 description 2
• 235000010980 cellulose Nutrition 0.000 description 2
• 229920002678 cellulose Polymers 0.000 description 2
• 239000001913 cellulose Substances 0.000 description 2
• 229920002301 cellulose acetate Polymers 0.000 description 2
• 229940081734 cellulose acetate phthalate Drugs 0.000 description 2
• 229920001688 coating polymer Polymers 0.000 description 2
• 239000003086 colorant Substances 0.000 description 2
• 238000002648 combination therapy Methods 0.000 description 2
• 229940124301 concurrent medication Drugs 0.000 description 2
• 229920001577 copolymer Polymers 0.000 description 2
• 235000012343 cottonseed oil Nutrition 0.000 description 2
• DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 2
• 229940047587 crofelemer 125 mg Drugs 0.000 description 2
• 239000000287 crude extract Substances 0.000 description 2
• 238000013481 data capture Methods 0.000 description 2
• 230000034994 death Effects 0.000 description 2
• 231100000517 death Toxicity 0.000 description 2
• 239000007950 delayed release tablet Substances 0.000 description 2
• 235000015872 dietary supplement Nutrition 0.000 description 2
• 239000003085 diluting agent Substances 0.000 description 2
• 239000006185 dispersion Substances 0.000 description 2
• 238000009826 distribution Methods 0.000 description 2
• 229940115080 doxil Drugs 0.000 description 2
• 238000002651 drug therapy Methods 0.000 description 2
• 229940120655 eloxatin Drugs 0.000 description 2
• 239000003995 emulsifying agent Substances 0.000 description 2
• 229940088598 enzyme Drugs 0.000 description 2
• 235000012734 epicatechin Nutrition 0.000 description 2
• DZYNKLUGCOSVKS-UHFFFAOYSA-N epigallocatechin Natural products OC1Cc2cc(O)cc(O)c2OC1c3cc(O)c(O)c(O)c3 DZYNKLUGCOSVKS-UHFFFAOYSA-N 0.000 description 2
• 229940014684 erivedge Drugs 0.000 description 2
• 235000019325 ethyl cellulose Nutrition 0.000 description 2
• 229920001249 ethyl cellulose Polymers 0.000 description 2
• MMXKVMNBHPAILY-UHFFFAOYSA-N ethyl laurate Chemical compound CCCCCCCCCCCC(=O)OCC MMXKVMNBHPAILY-UHFFFAOYSA-N 0.000 description 2
• LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 2
• 229940093471 ethyl oleate Drugs 0.000 description 2
• GDCRSXZBSIRSFR-UHFFFAOYSA-N ethyl prop-2-enoate;2-methylprop-2-enoic acid Chemical compound CC(=C)C(O)=O.CCOC(=O)C=C GDCRSXZBSIRSFR-UHFFFAOYSA-N 0.000 description 2
• 230000001747 exhibiting effect Effects 0.000 description 2
• 238000013401 experimental design Methods 0.000 description 2
• 229940087861 faslodex Drugs 0.000 description 2
• ZEACOKJOQLAYTD-UHFFFAOYSA-N flavan-3,3',4,4',5,5',7-heptol Chemical compound OC1C(O)C2=C(O)C=C(O)C=C2OC1C1=CC(O)=C(O)C(O)=C1 ZEACOKJOQLAYTD-UHFFFAOYSA-N 0.000 description 2
• 239000000796 flavoring agent Substances 0.000 description 2
• 239000007903 gelatin capsule Substances 0.000 description 2
• 229940020967 gemzar Drugs 0.000 description 2
• 229940080856 gleevec Drugs 0.000 description 2
• 239000003966 growth inhibitor Substances 0.000 description 2
• 229940118951 halaven Drugs 0.000 description 2
• 230000002489 hematologic effect Effects 0.000 description 2
• 238000000338 in vitro Methods 0.000 description 2
• 238000001727 in vivo Methods 0.000 description 2
• 238000001802 infusion Methods 0.000 description 2
• 229940005319 inlyta Drugs 0.000 description 2
• 210000004347 intestinal mucosa Anatomy 0.000 description 2
• 210000000936 intestine Anatomy 0.000 description 2
• 229940084651 iressa Drugs 0.000 description 2
• 208000002551 irritable bowel syndrome Diseases 0.000 description 2
• 238000002955 isolation Methods 0.000 description 2
• FABUFPQFXZVHFB-PVYNADRNSA-N ixabepilone Chemical compound C/C([C@@H]1C[C@@H]2O[C@]2(C)CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)N1)O)C)=C\C1=CSC(C)=N1 FABUFPQFXZVHFB-PVYNADRNSA-N 0.000 description 2
• 229940025735 jevtana Drugs 0.000 description 2
• 239000008101 lactose Substances 0.000 description 2
• 239000008141 laxative Substances 0.000 description 2
• 229940125722 laxative agent Drugs 0.000 description 2
• 235000010445 lecithin Nutrition 0.000 description 2
• 239000000787 lecithin Substances 0.000 description 2
• 229940067606 lecithin Drugs 0.000 description 2
• GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 description 2
• 229960004942 lenalidomide Drugs 0.000 description 2
• MPVGZUGXCQEXTM-UHFFFAOYSA-N linifanib Chemical compound CC1=CC=C(F)C(NC(=O)NC=2C=CC(=CC=2)C=2C=3C(N)=NNC=3C=CC=2)=C1 MPVGZUGXCQEXTM-UHFFFAOYSA-N 0.000 description 2
• 239000008297 liquid dosage form Substances 0.000 description 2
• 210000001165 lymph node Anatomy 0.000 description 2
• ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 2
• 239000001095 magnesium carbonate Substances 0.000 description 2
• 229910000021 magnesium carbonate Inorganic materials 0.000 description 2
• 239000000395 magnesium oxide Substances 0.000 description 2
• CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 2
• AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 2
• 229940049920 malate Drugs 0.000 description 2
• BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 2
• 238000007726 management method Methods 0.000 description 2
• 201000006512 mast cell neoplasm Diseases 0.000 description 2
• 231100000647 material safety data sheet Toxicity 0.000 description 2
• 229960001924 melphalan Drugs 0.000 description 2
• SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 description 2
• LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
• 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
• 239000008108 microcrystalline cellulose Substances 0.000 description 2
• 229940016286 microcrystalline cellulose Drugs 0.000 description 2
• 229960004857 mitomycin Drugs 0.000 description 2
• 231100000062 no-observed-adverse-effect level Toxicity 0.000 description 2
• 229940085033 nolvadex Drugs 0.000 description 2
• 229960002700 octreotide Drugs 0.000 description 2
• 235000008390 olive oil Nutrition 0.000 description 2
• 230000002018 overexpression Effects 0.000 description 2
• 229960001972 panitumumab Drugs 0.000 description 2
• 238000007911 parenteral administration Methods 0.000 description 2
• 239000002245 particle Substances 0.000 description 2
• 230000007170 pathology Effects 0.000 description 2
• WBXPDJSOTKVWSJ-ZDUSSCGKSA-L pemetrexed(2-) Chemical compound C=1NC=2NC(N)=NC(=O)C=2C=1CCC1=CC=C(C(=O)N[C@@H](CCC([O-])=O)C([O-])=O)C=C1 WBXPDJSOTKVWSJ-ZDUSSCGKSA-L 0.000 description 2
• 239000000825 pharmaceutical preparation Substances 0.000 description 2
• 102000020233 phosphotransferase Human genes 0.000 description 2
• 239000006187 pill Substances 0.000 description 2
• 229920005862 polyol Polymers 0.000 description 2
• 150000003077 polyols Chemical class 0.000 description 2
• 229940100467 polyvinyl acetate phthalate Drugs 0.000 description 2
• 238000002203 pretreatment Methods 0.000 description 2
• 239000006041 probiotic Substances 0.000 description 2
• 235000018291 probiotics Nutrition 0.000 description 2
• 230000002035 prolonged effect Effects 0.000 description 2
• 230000000069 prophylactic effect Effects 0.000 description 2
• 238000011321 prophylaxis Methods 0.000 description 2
• QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
• 238000001959 radiotherapy Methods 0.000 description 2
• 229960004432 raltitrexed Drugs 0.000 description 2
• 238000013102 re-test Methods 0.000 description 2
• 102000027426 receptor tyrosine kinases Human genes 0.000 description 2
• 108091008598 receptor tyrosine kinases Proteins 0.000 description 2
• 229960003452 romidepsin Drugs 0.000 description 2
• 210000002966 serum Anatomy 0.000 description 2
• 239000008159 sesame oil Substances 0.000 description 2
• 235000011803 sesame oil Nutrition 0.000 description 2
• 230000019491 signal transduction Effects 0.000 description 2
• RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 2
• 235000012239 silicon dioxide Nutrition 0.000 description 2
• GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 2
• 238000001694 spray drying Methods 0.000 description 2
• 239000008107 starch Substances 0.000 description 2
• 238000007619 statistical method Methods 0.000 description 2
• 229940090374 stivarga Drugs 0.000 description 2
• 229940034785 sutent Drugs 0.000 description 2
• 239000003765 sweetening agent Substances 0.000 description 2
• 230000009885 systemic effect Effects 0.000 description 2
• 229940063683 taxotere Drugs 0.000 description 2
• 229940061353 temodar Drugs 0.000 description 2
• 229940100411 torisel Drugs 0.000 description 2
• 231100000419 toxicity Toxicity 0.000 description 2
• 230000001988 toxicity Effects 0.000 description 2
• 230000001052 transient effect Effects 0.000 description 2
• 229940094060 tykerb Drugs 0.000 description 2
• 230000035899 viability Effects 0.000 description 2
• BPQMGSKTAYIVFO-UHFFFAOYSA-N vismodegib Chemical compound ClC1=CC(S(=O)(=O)C)=CC=C1C(=O)NC1=CC=C(Cl)C(C=2N=CC=CC=2)=C1 BPQMGSKTAYIVFO-UHFFFAOYSA-N 0.000 description 2
• 229940069559 votrient Drugs 0.000 description 2
• 230000003442 weekly effect Effects 0.000 description 2
• 230000036642 wellbeing Effects 0.000 description 2
• 229940049068 xalkori Drugs 0.000 description 2
• 229940053867 xeloda Drugs 0.000 description 2
• 229940036061 zaltrap Drugs 0.000 description 2
• 229940033942 zoladex Drugs 0.000 description 2
• XMOCLSLCDHWDHP-SWLSCSKDSA-N (+)-Epigallocatechin Natural products C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2O)=CC(O)=C(O)C(O)=C1 XMOCLSLCDHWDHP-SWLSCSKDSA-N 0.000 description 1
• PFTAWBLQPZVEMU-DZGCQCFKSA-N (+)-catechin Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-DZGCQCFKSA-N 0.000 description 1
• PFTAWBLQPZVEMU-ZFWWWQNUSA-N (+)-epicatechin Natural products C1([C@@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-ZFWWWQNUSA-N 0.000 description 1
• PFTAWBLQPZVEMU-UKRRQHHQSA-N (-)-epicatechin Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-UKRRQHHQSA-N 0.000 description 1
• QIJRTFXNRTXDIP-UHFFFAOYSA-N (1-carboxy-2-sulfanylethyl)azanium;chloride;hydrate Chemical compound O.Cl.SCC(N)C(O)=O QIJRTFXNRTXDIP-UHFFFAOYSA-N 0.000 description 1
• WCWUXEGQKLTGDX-LLVKDONJSA-N (2R)-1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methyl-6-pyrrolo[2,1-f][1,2,4]triazinyl]oxy]-2-propanol Chemical compound C1=C2NC(C)=CC2=C(F)C(OC2=NC=NN3C=C(C(=C32)C)OC[C@H](O)C)=C1 WCWUXEGQKLTGDX-LLVKDONJSA-N 0.000 description 1
• MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 1
• UUBHZHZSIKRVIV-KCXSXWJSSA-N (2e,6e,10e)-3,7,11,15-tetramethylhexadeca-2,4,6,10,14-pentaenoic acid Chemical compound CC(C)=CCC\C(C)=C\CC\C(C)=C\C=C\C(\C)=C\C(O)=O UUBHZHZSIKRVIV-KCXSXWJSSA-N 0.000 description 1
• OPCHFPHZPIURNA-MFERNQICSA-N (2s)-2,5-bis(3-aminopropylamino)-n-[2-(dioctadecylamino)acetyl]pentanamide Chemical compound CCCCCCCCCCCCCCCCCCN(CC(=O)NC(=O)[C@H](CCCNCCCN)NCCCN)CCCCCCCCCCCCCCCCCC OPCHFPHZPIURNA-MFERNQICSA-N 0.000 description 1
• KCOYQXZDFIIGCY-CZIZESTLSA-N (3e)-4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1,3-dihydrobenzimidazol-2-ylidene]quinolin-2-one Chemical compound C1CN(C)CCN1C1=CC=C(N\C(N2)=C/3C(=C4C(F)=CC=CC4=NC\3=O)N)C2=C1 KCOYQXZDFIIGCY-CZIZESTLSA-N 0.000 description 1
• GVJHHUAWPYXKBD-IEOSBIPESA-N (R)-alpha-Tocopherol Natural products OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
• QMMJWQMCMRUYTG-UHFFFAOYSA-N 1,2,4,5-tetrachloro-3-(trifluoromethyl)benzene Chemical compound FC(F)(F)C1=C(Cl)C(Cl)=CC(Cl)=C1Cl QMMJWQMCMRUYTG-UHFFFAOYSA-N 0.000 description 1
• 229940058015 1,3-butylene glycol Drugs 0.000 description 1
• WPHKIQPVPYJNAX-UHFFFAOYSA-N 1-[4-[4-amino-7-[1-(2-hydroxyethyl)pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl]phenyl]-3-(3-fluorophenyl)urea Chemical compound C1=2SC=C(C=3C=CC(NC(=O)NC=4C=C(F)C=CC=4)=CC=3)C=2C(N)=NC=C1C=1C=NN(CCO)C=1 WPHKIQPVPYJNAX-UHFFFAOYSA-N 0.000 description 1
• BJHCYTJNPVGSBZ-YXSASFKJSA-N 1-[4-[6-amino-5-[(Z)-methoxyiminomethyl]pyrimidin-4-yl]oxy-2-chlorophenyl]-3-ethylurea Chemical compound CCNC(=O)Nc1ccc(Oc2ncnc(N)c2\C=N/OC)cc1Cl BJHCYTJNPVGSBZ-YXSASFKJSA-N 0.000 description 1
• FSPQCTGGIANIJZ-UHFFFAOYSA-N 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1C(=O)NC1=C(C(N)=O)C(CCCC2)=C2S1 FSPQCTGGIANIJZ-UHFFFAOYSA-N 0.000 description 1
• JNODDICFTDYODH-UHFFFAOYSA-N 2-hydroxytetrahydrofuran Chemical compound OC1CCCO1 JNODDICFTDYODH-UHFFFAOYSA-N 0.000 description 1
• NHFDRBXTEDBWCZ-ZROIWOOFSA-N 3-[2,4-dimethyl-5-[(z)-(2-oxo-1h-indol-3-ylidene)methyl]-1h-pyrrol-3-yl]propanoic acid Chemical compound OC(=O)CCC1=C(C)NC(\C=C/2C3=CC=CC=C3NC\2=O)=C1C NHFDRBXTEDBWCZ-ZROIWOOFSA-N 0.000 description 1
• AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-VTZDEGQISA-N 0.000 description 1
• MDOJTZQKHMAPBK-UHFFFAOYSA-N 4-iodo-3-nitrobenzamide Chemical compound NC(=O)C1=CC=C(I)C([N+]([O-])=O)=C1 MDOJTZQKHMAPBK-UHFFFAOYSA-N 0.000 description 1
• YUDPTGPSBJVHCN-DZQJYWQESA-N 4-methylumbelliferyl beta-D-galactoside Chemical compound C1=CC=2C(C)=CC(=O)OC=2C=C1O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O YUDPTGPSBJVHCN-DZQJYWQESA-N 0.000 description 1
• VVIAGPKUTFNRDU-UHFFFAOYSA-N 6S-folinic acid Natural products C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-UHFFFAOYSA-N 0.000 description 1
• 102000057234 Acyl transferases Human genes 0.000 description 1
• 108700016155 Acyl transferases Proteins 0.000 description 1
• ORILYTVJVMAKLC-UHFFFAOYSA-N Adamantane Natural products C1C(C2)CC3CC1CC2C3 ORILYTVJVMAKLC-UHFFFAOYSA-N 0.000 description 1
• 108010012934 Albumin-Bound Paclitaxel Proteins 0.000 description 1
• 229920000856 Amylose Polymers 0.000 description 1
• 102100022014 Angiopoietin-1 receptor Human genes 0.000 description 1
• 235000003276 Apios tuberosa Nutrition 0.000 description 1
• 244000105624 Arachis hypogaea Species 0.000 description 1
• 235000010777 Arachis hypogaea Nutrition 0.000 description 1
• 235000010744 Arachis villosulicarpa Nutrition 0.000 description 1
• 102000004625 Aspartate Aminotransferases Human genes 0.000 description 1
• 108010003415 Aspartate Aminotransferases Proteins 0.000 description 1
• 229930003347 Atropine Natural products 0.000 description 1
• 102100035080 BDNF/NT-3 growth factors receptor Human genes 0.000 description 1
• 241000349750 Baphia nitida Species 0.000 description 1
• DWRXFEITVBNRMK-UHFFFAOYSA-N Beta-D-1-Arabinofuranosylthymine Natural products O=C1NC(=O)C(C)=CN1C1C(O)C(O)C(CO)O1 DWRXFEITVBNRMK-UHFFFAOYSA-N 0.000 description 1
• HWSISDHAHRVNMT-UHFFFAOYSA-N Bismuth subnitrate Chemical compound O[NH+]([O-])O[Bi](O[N+]([O-])=O)O[N+]([O-])=O HWSISDHAHRVNMT-UHFFFAOYSA-N 0.000 description 1
• 108091007914 CDKs Proteins 0.000 description 1
• 101150050673 CHK1 gene Proteins 0.000 description 1
• 241000824799 Canis lupus dingo Species 0.000 description 1
• 208000005623 Carcinogenesis Diseases 0.000 description 1
• 240000007857 Castanea sativa Species 0.000 description 1
• 235000014037 Castanea sativa Nutrition 0.000 description 1
• 240000008886 Ceratonia siliqua Species 0.000 description 1
• 235000013912 Ceratonia siliqua Nutrition 0.000 description 1
• 108091006146 Channels Proteins 0.000 description 1
• 102000009016 Cholera Toxin Human genes 0.000 description 1
• 108010049048 Cholera Toxin Proteins 0.000 description 1
• 206010009900 Colitis ulcerative Diseases 0.000 description 1
• 229920002261 Corn starch Polymers 0.000 description 1
• 208000011231 Crohn disease Diseases 0.000 description 1
• 229920002785 Croscarmellose sodium Polymers 0.000 description 1
• 239000004971 Cross linker Substances 0.000 description 1
• 241000741487 Croton draconoides Species 0.000 description 1
• 201000003883 Cystic fibrosis Diseases 0.000 description 1
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
• 102000053602 DNA Human genes 0.000 description 1
• 239000012625 DNA intercalator Substances 0.000 description 1
• 208000005156 Dehydration Diseases 0.000 description 1
• SUZLHDUTVMZSEV-UHFFFAOYSA-N Deoxycoleonol Natural products C12C(=O)CC(C)(C=C)OC2(C)C(OC(=O)C)C(O)C2C1(C)C(O)CCC2(C)C SUZLHDUTVMZSEV-UHFFFAOYSA-N 0.000 description 1
• 206010012335 Dependence Diseases 0.000 description 1
• FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
• 206010012742 Diarrhoea infectious Diseases 0.000 description 1
• 206010061819 Disease recurrence Diseases 0.000 description 1
• 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 description 1
• 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 description 1
• 101150029707 ERBB2 gene Proteins 0.000 description 1
• HEAUOKZIVMZVQL-VWLOTQADSA-N Elagolix Chemical compound COC1=CC=CC(C=2C(N(C[C@H](NCCCC(O)=O)C=3C=CC=CC=3)C(=O)N(CC=3C(=CC=CC=3F)C(F)(F)F)C=2C)=O)=C1F HEAUOKZIVMZVQL-VWLOTQADSA-N 0.000 description 1
• 206010014733 Endometrial cancer Diseases 0.000 description 1
• 206010014759 Endometrial neoplasm Diseases 0.000 description 1
• HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 description 1
• 241001481760 Erethizon dorsatum Species 0.000 description 1
• 241000588724 Escherichia coli Species 0.000 description 1
• JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 description 1
• 229920003138 Eudragit® L 30 D-55 Polymers 0.000 description 1
• 229920003134 Eudragit® polymer Polymers 0.000 description 1
• 241000221017 Euphorbiaceae Species 0.000 description 1
• CITFYDYEWQIEPX-UHFFFAOYSA-N Flavanol Natural products O1C2=CC(OCC=C(C)C)=CC(O)=C2C(=O)C(O)C1C1=CC=C(O)C=C1 CITFYDYEWQIEPX-UHFFFAOYSA-N 0.000 description 1
• 108700031843 GRB7 Adaptor Proteins 0.000 description 1
• 101150052409 GRB7 gene Proteins 0.000 description 1
• 206010061968 Gastric neoplasm Diseases 0.000 description 1
• 206010070840 Gastrointestinal tract irritation Diseases 0.000 description 1
• 108010010803 Gelatin Proteins 0.000 description 1
• 241000206672 Gelidium Species 0.000 description 1
• 208000032320 Germ cell tumor of testis Diseases 0.000 description 1
• 208000009139 Gilbert Disease Diseases 0.000 description 1
• 208000022412 Gilbert syndrome Diseases 0.000 description 1
• WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
• 206010056559 Graft infection Diseases 0.000 description 1
• 208000009329 Graft vs Host Disease Diseases 0.000 description 1
• 102000009465 Growth Factor Receptors Human genes 0.000 description 1
• 108010009202 Growth Factor Receptors Proteins 0.000 description 1
• 229940125497 HER2 kinase inhibitor Drugs 0.000 description 1
• 102000002812 Heat-Shock Proteins Human genes 0.000 description 1
• 108010004889 Heat-Shock Proteins Proteins 0.000 description 1
• 208000032843 Hemorrhage Diseases 0.000 description 1
• 102000003745 Hepatocyte Growth Factor Human genes 0.000 description 1
• 108090000100 Hepatocyte Growth Factor Proteins 0.000 description 1
• 108010033040 Histones Proteins 0.000 description 1
• 101000753291 Homo sapiens Angiopoietin-1 receptor Proteins 0.000 description 1
• 101000596896 Homo sapiens BDNF/NT-3 growth factors receptor Proteins 0.000 description 1
• 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 description 1
• RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 description 1
• 208000001953 Hypotension Diseases 0.000 description 1
• 206010021639 Incontinence Diseases 0.000 description 1
• 206010061218 Inflammation Diseases 0.000 description 1
• 102000003746 Insulin Receptor Human genes 0.000 description 1
• 108010001127 Insulin Receptor Proteins 0.000 description 1
• 239000011786 L-ascorbyl-6-palmitate Substances 0.000 description 1
• QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 description 1
• OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 1
• UCEQXRCJXIVODC-PMACEKPBSA-N LSM-1131 Chemical compound C1CCC2=CC=CC3=C2N1C=C3[C@@H]1C(=O)NC(=O)[C@H]1C1=CNC2=CC=CC=C12 UCEQXRCJXIVODC-PMACEKPBSA-N 0.000 description 1
• 102000001291 MAP Kinase Kinase Kinase Human genes 0.000 description 1
• 108060006687 MAP kinase kinase kinase Proteins 0.000 description 1
• 102100028198 Macrophage colony-stimulating factor 1 receptor Human genes 0.000 description 1
• 101710150918 Macrophage colony-stimulating factor 1 receptor Proteins 0.000 description 1
• 208000002720 Malnutrition Diseases 0.000 description 1
• 241000124008 Mammalia Species 0.000 description 1
• 229930195725 Mannitol Natural products 0.000 description 1
• 206010059282 Metastases to central nervous system Diseases 0.000 description 1
• VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
• 102000029749 Microtubule Human genes 0.000 description 1
• 108091022875 Microtubule Proteins 0.000 description 1
• 101100091501 Mus musculus Ros1 gene Proteins 0.000 description 1
• 241000699670 Mus sp. Species 0.000 description 1
• GXCLVBGFBYZDAG-UHFFFAOYSA-N N-[2-(1H-indol-3-yl)ethyl]-N-methylprop-2-en-1-amine Chemical compound CN(CCC1=CNC2=C1C=CC=C2)CC=C GXCLVBGFBYZDAG-UHFFFAOYSA-N 0.000 description 1
• 102000014736 Notch Human genes 0.000 description 1
• 108010070047 Notch Receptors Proteins 0.000 description 1
• 240000007817 Olea europaea Species 0.000 description 1
• 239000008896 Opium Substances 0.000 description 1
• 239000012828 PI3K inhibitor Substances 0.000 description 1
• 208000002606 Paramyxoviridae Infections Diseases 0.000 description 1
• 235000019483 Peanut oil Nutrition 0.000 description 1
• 102000057297 Pepsin A Human genes 0.000 description 1
• 108090000284 Pepsin A Proteins 0.000 description 1
• 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 description 1
• 108010038512 Platelet-Derived Growth Factor Proteins 0.000 description 1
• 102000010780 Platelet-Derived Growth Factor Human genes 0.000 description 1
• 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 description 1
• 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
• 239000004952 Polyamide Substances 0.000 description 1
• 229940079156 Proteasome inhibitor Drugs 0.000 description 1
• 102000001253 Protein Kinase Human genes 0.000 description 1
• 102000055027 Protein Methyltransferases Human genes 0.000 description 1
• 108700040121 Protein Methyltransferases Proteins 0.000 description 1
• 102000052575 Proto-Oncogene Human genes 0.000 description 1
• 108700020978 Proto-Oncogene Proteins 0.000 description 1
• 241000308676 Pterocarpus officinalis Species 0.000 description 1
• 102100029981 Receptor tyrosine-protein kinase erbB-4 Human genes 0.000 description 1
• 101710100963 Receptor tyrosine-protein kinase erbB-4 Proteins 0.000 description 1
• 101710151245 Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 description 1
• 208000035999 Recurrence Diseases 0.000 description 1
• 208000001647 Renal Insufficiency Diseases 0.000 description 1
• 235000004443 Ricinus communis Nutrition 0.000 description 1
• 235000019485 Safflower oil Nutrition 0.000 description 1
• MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
• 102100036077 Serine/threonine-protein kinase pim-1 Human genes 0.000 description 1
• 101710184310 Serine/threonine-protein kinase pim-1 Proteins 0.000 description 1
• 229920001800 Shellac Polymers 0.000 description 1
• VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
• DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
• 238000000692 Student's t-test Methods 0.000 description 1
• 229930006000 Sucrose Natural products 0.000 description 1
• FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
• 102000002938 Thrombospondin Human genes 0.000 description 1
• 108060008245 Thrombospondin Proteins 0.000 description 1
• GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
• 238000008050 Total Bilirubin Reagent Methods 0.000 description 1
• DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 1
• 102000014384 Type C Phospholipases Human genes 0.000 description 1
• 108010079194 Type C Phospholipases Proteins 0.000 description 1
• 201000006704 Ulcerative Colitis Diseases 0.000 description 1
• 108091008605 VEGF receptors Proteins 0.000 description 1
• 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 description 1
• 108010053096 Vascular Endothelial Growth Factor Receptor-1 Proteins 0.000 description 1
• 102000016548 Vascular Endothelial Growth Factor Receptor-1 Human genes 0.000 description 1
• 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 description 1
• 108010053100 Vascular Endothelial Growth Factor Receptor-3 Proteins 0.000 description 1
• 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 1
• 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 1
• 102100033179 Vascular endothelial growth factor receptor 3 Human genes 0.000 description 1
• 241000700605 Viruses Species 0.000 description 1
• 210000001015 abdomen Anatomy 0.000 description 1
• 230000002159 abnormal effect Effects 0.000 description 1
• 229940028652 abraxane Drugs 0.000 description 1
• 238000009825 accumulation Methods 0.000 description 1
• 229940022663 acetate Drugs 0.000 description 1
• IYKJEILNJZQJPU-UHFFFAOYSA-N acetic acid;butanedioic acid Chemical compound CC(O)=O.OC(=O)CCC(O)=O IYKJEILNJZQJPU-UHFFFAOYSA-N 0.000 description 1
• GAMPNQJDUFQVQO-UHFFFAOYSA-N acetic acid;phthalic acid Chemical class CC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O GAMPNQJDUFQVQO-UHFFFAOYSA-N 0.000 description 1
• 239000012190 activator Substances 0.000 description 1
• 230000009692 acute damage Effects 0.000 description 1
• 239000002671 adjuvant Substances 0.000 description 1
• 239000008272 agar Substances 0.000 description 1
• 238000011366 aggressive therapy Methods 0.000 description 1
• 235000010443 alginic acid Nutrition 0.000 description 1
• 239000000783 alginic acid Substances 0.000 description 1
• 229920000615 alginic acid Polymers 0.000 description 1
• 229960001126 alginic acid Drugs 0.000 description 1
• 150000004781 alginic acids Chemical class 0.000 description 1
• 208000026935 allergic disease Diseases 0.000 description 1
• 230000003281 allosteric effect Effects 0.000 description 1
• 229940087168 alpha tocopherol Drugs 0.000 description 1
• 229910052782 aluminium Inorganic materials 0.000 description 1
• XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
• BWZOPYPOZJBVLQ-UHFFFAOYSA-K aluminium glycinate Chemical compound O[Al+]O.NCC([O-])=O BWZOPYPOZJBVLQ-UHFFFAOYSA-K 0.000 description 1
• 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
• 229940024545 aluminum hydroxide Drugs 0.000 description 1
• JIFPTBLGXRKRAO-UHFFFAOYSA-K aluminum;magnesium;hydroxide;sulfate Chemical compound [OH-].[Mg+2].[Al+3].[O-]S([O-])(=O)=O JIFPTBLGXRKRAO-UHFFFAOYSA-K 0.000 description 1
• SEIGJEJVIMIXIU-UHFFFAOYSA-J aluminum;sodium;carbonate;dihydroxide Chemical compound [Na+].O[Al+]O.[O-]C([O-])=O SEIGJEJVIMIXIU-UHFFFAOYSA-J 0.000 description 1
• 230000003321 amplification Effects 0.000 description 1
• 229960002932 anastrozole Drugs 0.000 description 1
• 239000002870 angiogenesis inducing agent Substances 0.000 description 1
• 125000000129 anionic group Chemical group 0.000 description 1
• 229930014669 anthocyanidin Natural products 0.000 description 1
• 235000008758 anthocyanidins Nutrition 0.000 description 1
• 230000003466 anti-cipated effect Effects 0.000 description 1
• 230000000843 anti-fungal effect Effects 0.000 description 1
• 230000002141 anti-parasite Effects 0.000 description 1
• 230000000798 anti-retroviral effect Effects 0.000 description 1
• 229940125714 antidiarrheal agent Drugs 0.000 description 1
• 239000003793 antidiarrheal agent Substances 0.000 description 1
• 229940121375 antifungal agent Drugs 0.000 description 1
• 229940041181 antineoplastic drug Drugs 0.000 description 1
• 229940124522 antiretrovirals Drugs 0.000 description 1
• 229940121357 antivirals Drugs 0.000 description 1
• 238000013459 approach Methods 0.000 description 1
• 239000008365 aqueous carrier Substances 0.000 description 1
• 239000007864 aqueous solution Substances 0.000 description 1
• 235000010323 ascorbic acid Nutrition 0.000 description 1
• 229960005070 ascorbic acid Drugs 0.000 description 1
• 239000011668 ascorbic acid Substances 0.000 description 1
• 235000010385 ascorbyl palmitate Nutrition 0.000 description 1
• MOTJMGVDPWRKOC-QPVYNBJUSA-N atrasentan Chemical compound C1([C@H]2[C@@H]([C@H](CN2CC(=O)N(CCCC)CCCC)C=2C=C3OCOC3=CC=2)C(O)=O)=CC=C(OC)C=C1 MOTJMGVDPWRKOC-QPVYNBJUSA-N 0.000 description 1
• 229950010993 atrasentan Drugs 0.000 description 1
• RKUNBYITZUJHSG-SPUOUPEWSA-N atropine Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-SPUOUPEWSA-N 0.000 description 1
• 229960000396 atropine Drugs 0.000 description 1
• 239000011324 bead Substances 0.000 description 1
• 239000000440 bentonite Substances 0.000 description 1
• 229910000278 bentonite Inorganic materials 0.000 description 1
• SVPXDRXYRYOSEX-UHFFFAOYSA-N bentoquatam Chemical compound O.O=[Si]=O.O=[Al]O[Al]=O SVPXDRXYRYOSEX-UHFFFAOYSA-N 0.000 description 1
• 229960002903 benzyl benzoate Drugs 0.000 description 1
• WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
• IQFYYKKMVGJFEH-UHFFFAOYSA-N beta-L-thymidine Natural products O=C1NC(=O)C(C)=CN1C1OC(CO)C(O)C1 IQFYYKKMVGJFEH-UHFFFAOYSA-N 0.000 description 1
• 239000011230 binding agent Substances 0.000 description 1
• 230000004071 biological effect Effects 0.000 description 1
• 230000033228 biological regulation Effects 0.000 description 1
• 238000001815 biotherapy Methods 0.000 description 1
• 229910052797 bismuth Inorganic materials 0.000 description 1
• JCXGWMGPZLAOME-UHFFFAOYSA-N bismuth atom Chemical compound [Bi] JCXGWMGPZLAOME-UHFFFAOYSA-N 0.000 description 1
• 229960001482 bismuth subnitrate Drugs 0.000 description 1
• ZREIPSZUJIFJNP-UHFFFAOYSA-K bismuth subsalicylate Chemical compound C1=CC=C2O[Bi](O)OC(=O)C2=C1 ZREIPSZUJIFJNP-UHFFFAOYSA-K 0.000 description 1
• 229960000782 bismuth subsalicylate Drugs 0.000 description 1
• 230000000740 bleeding effect Effects 0.000 description 1
• 229960001467 bortezomib Drugs 0.000 description 1
• 239000006172 buffering agent Substances 0.000 description 1
• 239000001273 butane Substances 0.000 description 1
• 235000019437 butane-1,3-diol Nutrition 0.000 description 1
• 235000019282 butylated hydroxyanisole Nutrition 0.000 description 1
• 229960003563 calcium carbonate Drugs 0.000 description 1
• 235000012241 calcium silicate Nutrition 0.000 description 1
• 229940088954 camptosar Drugs 0.000 description 1
• 230000036952 cancer formation Effects 0.000 description 1
• 239000001768 carboxy methyl cellulose Substances 0.000 description 1
• 231100000504 carcinogenesis Toxicity 0.000 description 1
• 239000003183 carcinogenic agent Substances 0.000 description 1
• 239000004359 castor oil Substances 0.000 description 1
• 230000015556 catabolic process Effects 0.000 description 1
• 150000001765 catechin Chemical class 0.000 description 1
• 230000010261 cell growth Effects 0.000 description 1
• 210000000170 cell membrane Anatomy 0.000 description 1
• 230000004663 cell proliferation Effects 0.000 description 1
• 229960005395 cetuximab Drugs 0.000 description 1
• 239000002738 chelating agent Substances 0.000 description 1
• 230000001055 chewing effect Effects 0.000 description 1
• 150000005827 chlorofluoro hydrocarbons Chemical class 0.000 description 1
• 229950001002 cianidanol Drugs 0.000 description 1
• DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 1
• 229960004316 cisplatin Drugs 0.000 description 1
• 239000004927 clay Substances 0.000 description 1
• 239000007931 coated granule Substances 0.000 description 1
• 229940110456 cocoa butter Drugs 0.000 description 1
• 235000019868 cocoa butter Nutrition 0.000 description 1
• 238000012321 colectomy Methods 0.000 description 1
• OHCQJHSOBUTRHG-UHFFFAOYSA-N colforsin Natural products OC12C(=O)CC(C)(C=C)OC1(C)C(OC(=O)C)C(O)C1C2(C)C(O)CCC1(C)C OHCQJHSOBUTRHG-UHFFFAOYSA-N 0.000 description 1
• 206010009887 colitis Diseases 0.000 description 1
• 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
• 238000004891 communication Methods 0.000 description 1
• 238000013270 controlled release Methods 0.000 description 1
• 235000005687 corn oil Nutrition 0.000 description 1
• 239000002285 corn oil Substances 0.000 description 1
• 239000008120 corn starch Substances 0.000 description 1
• 239000002385 cottonseed oil Substances 0.000 description 1
• 229940109239 creatinine Drugs 0.000 description 1
• 229960001681 croscarmellose sodium Drugs 0.000 description 1
• 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
• 238000002425 crystallisation Methods 0.000 description 1
• 230000008025 crystallization Effects 0.000 description 1
• 230000001186 cumulative effect Effects 0.000 description 1
• 229960001305 cysteine hydrochloride Drugs 0.000 description 1
• 238000006731 degradation reaction Methods 0.000 description 1
• 230000001934 delay Effects 0.000 description 1
• 230000001419 dependent effect Effects 0.000 description 1
• 238000011161 development Methods 0.000 description 1
• 238000003745 diagnosis Methods 0.000 description 1
• 235000014113 dietary fatty acids Nutrition 0.000 description 1
• 229940015828 dihydroxyaluminum sodium carbonate Drugs 0.000 description 1
• 239000002270 dispersing agent Substances 0.000 description 1
• 230000009429 distress Effects 0.000 description 1
• 239000003534 dna topoisomerase inhibitor Substances 0.000 description 1
• 229950005778 dovitinib Drugs 0.000 description 1
• 239000009136 dragon's blood Substances 0.000 description 1
• 239000008298 dragée Substances 0.000 description 1
• 230000036267 drug metabolism Effects 0.000 description 1
• 230000008406 drug-drug interaction Effects 0.000 description 1
• 208000001848 dysentery Diseases 0.000 description 1
• 230000002526 effect on cardiovascular system Effects 0.000 description 1
• 229950004823 elagolix Drugs 0.000 description 1
• 239000003792 electrolyte Substances 0.000 description 1
• 230000008030 elimination Effects 0.000 description 1
• 238000003379 elimination reaction Methods 0.000 description 1
• 239000000839 emulsion Substances 0.000 description 1
• 201000003914 endometrial carcinoma Diseases 0.000 description 1
• 239000002662 enteric coated tablet Substances 0.000 description 1
• 230000000688 enterotoxigenic effect Effects 0.000 description 1
• LPTRNLNOHUVQMS-UHFFFAOYSA-N epicatechin Natural products Cc1cc(O)cc2OC(C(O)Cc12)c1ccc(O)c(O)c1 LPTRNLNOHUVQMS-UHFFFAOYSA-N 0.000 description 1
• 229960001904 epirubicin Drugs 0.000 description 1
• 230000008472 epithelial growth Effects 0.000 description 1
• 229940082789 erbitux Drugs 0.000 description 1
• 150000002148 esters Chemical class 0.000 description 1
• 229940093499 ethyl acetate Drugs 0.000 description 1
• 239000003925 fat Substances 0.000 description 1
• 235000019197 fats Nutrition 0.000 description 1
• 239000000194 fatty acid Substances 0.000 description 1
• 229930195729 fatty acid Natural products 0.000 description 1
• 239000000945 filler Substances 0.000 description 1
• 150000005835 flavan-3,4-diols Chemical class 0.000 description 1
• 150000002206 flavan-3-ols Chemical class 0.000 description 1
• 235000011987 flavanols Nutrition 0.000 description 1
• 229930003935 flavonoid Natural products 0.000 description 1
• 235000017173 flavonoids Nutrition 0.000 description 1
• 150000002215 flavonoids Chemical class 0.000 description 1
• HVQAJTFOCKOKIN-UHFFFAOYSA-N flavonol Natural products O1C2=CC=CC=C2C(=O)C(O)=C1C1=CC=CC=C1 HVQAJTFOCKOKIN-UHFFFAOYSA-N 0.000 description 1
• 150000002216 flavonol derivatives Chemical class 0.000 description 1
• 235000011957 flavonols Nutrition 0.000 description 1
• NWKFECICNXDNOQ-UHFFFAOYSA-N flavylium Chemical compound C1=CC=CC=C1C1=CC=C(C=CC=C2)C2=[O+]1 NWKFECICNXDNOQ-UHFFFAOYSA-N 0.000 description 1
• 150000005699 fluoropyrimidines Chemical class 0.000 description 1
• 108010003374 fms-Like Tyrosine Kinase 3 Proteins 0.000 description 1
• 239000006260 foam Substances 0.000 description 1
• VVIAGPKUTFNRDU-ABLWVSNPSA-N folinic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-ABLWVSNPSA-N 0.000 description 1
• 235000008191 folinic acid Nutrition 0.000 description 1
• 239000011672 folinic acid Substances 0.000 description 1
• 235000013355 food flavoring agent Nutrition 0.000 description 1
• 235000012631 food intake Nutrition 0.000 description 1
• 235000003599 food sweetener Nutrition 0.000 description 1
• 239000008273 gelatin Substances 0.000 description 1
• 229920000159 gelatin Polymers 0.000 description 1
• 235000019322 gelatine Nutrition 0.000 description 1
• 235000011852 gelatine desserts Nutrition 0.000 description 1
• 239000008103 glucose Substances 0.000 description 1
• 150000002334 glycols Chemical class 0.000 description 1
• 208000024908 graft versus host disease Diseases 0.000 description 1
• 230000012010 growth Effects 0.000 description 1
• 230000003862 health status Effects 0.000 description 1
• 229930195733 hydrocarbon Natural products 0.000 description 1
• 150000002430 hydrocarbons Chemical class 0.000 description 1
• 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 description 1
• 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 description 1
• 208000013403 hyperactivity Diseases 0.000 description 1
• 230000036543 hypotension Effects 0.000 description 1
• 229950000568 ilorasertib Drugs 0.000 description 1
• 239000005414 inactive ingredient Substances 0.000 description 1
• 239000000411 inducer Substances 0.000 description 1
• 230000006698 induction Effects 0.000 description 1
• 239000003701 inert diluent Substances 0.000 description 1
• 208000015181 infectious disease Diseases 0.000 description 1
• 230000008595 infiltration Effects 0.000 description 1
• 238000001764 infiltration Methods 0.000 description 1
• 230000004054 inflammatory process Effects 0.000 description 1
• 206010022000 influenza Diseases 0.000 description 1
• 229950002133 iniparib Drugs 0.000 description 1
• 230000000977 initiatory effect Effects 0.000 description 1
• 230000000266 injurious effect Effects 0.000 description 1
• 230000008991 intestinal motility Effects 0.000 description 1
• 238000010255 intramuscular injection Methods 0.000 description 1
• 238000001990 intravenous administration Methods 0.000 description 1
• 238000010253 intravenous injection Methods 0.000 description 1
• 238000011835 investigation Methods 0.000 description 1
• 229960005386 ipilimumab Drugs 0.000 description 1
• 230000002427 irreversible effect Effects 0.000 description 1
• 239000013038 irreversible inhibitor Substances 0.000 description 1
• 230000007794 irritation Effects 0.000 description 1
• 229940011083 istodax Drugs 0.000 description 1
• 229960002014 ixabepilone Drugs 0.000 description 1
• 229940111707 ixempra Drugs 0.000 description 1
• 201000006370 kidney failure Diseases 0.000 description 1
• MJIHNNLFOKEZEW-UHFFFAOYSA-N lansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1 MJIHNNLFOKEZEW-UHFFFAOYSA-N 0.000 description 1
• 230000002045 lasting effect Effects 0.000 description 1
• 229960001691 leucovorin Drugs 0.000 description 1
• 230000000670 limiting effect Effects 0.000 description 1
• 229950002216 linifanib Drugs 0.000 description 1
• 210000004185 liver Anatomy 0.000 description 1
• 238000001325 log-rank test Methods 0.000 description 1
• 238000007477 logistic regression Methods 0.000 description 1
• 239000007937 lozenge Substances 0.000 description 1
• 229940124302 mTOR inhibitor Drugs 0.000 description 1
• 210000002540 macrophage Anatomy 0.000 description 1
• 229960004018 magaldrate Drugs 0.000 description 1
• 229960001708 magnesium carbonate Drugs 0.000 description 1
• 229960000816 magnesium hydroxide Drugs 0.000 description 1
• 229960000869 magnesium oxide Drugs 0.000 description 1
• 229940057948 magnesium stearate Drugs 0.000 description 1
• 238000012423 maintenance Methods 0.000 description 1
• 230000036210 malignancy Effects 0.000 description 1
• 230000001071 malnutrition Effects 0.000 description 1
• 235000000824 malnutrition Nutrition 0.000 description 1
• 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 description 1
• 239000000594 mannitol Substances 0.000 description 1
• 235000010355 mannitol Nutrition 0.000 description 1
• 239000011159 matrix material Substances 0.000 description 1
• 238000005259 measurement Methods 0.000 description 1
• 230000007246 mechanism Effects 0.000 description 1
• 230000001404 mediated effect Effects 0.000 description 1
• 230000007721 medicinal effect Effects 0.000 description 1
• 229910052751 metal Inorganic materials 0.000 description 1
• 239000002184 metal Substances 0.000 description 1
• 230000001394 metastastic effect Effects 0.000 description 1
• 206010061289 metastatic neoplasm Diseases 0.000 description 1
• 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
• 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
• 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
• 229960002216 methylparaben Drugs 0.000 description 1
• 239000004530 micro-emulsion Substances 0.000 description 1
• 208000008275 microscopic colitis Diseases 0.000 description 1
• 239000004005 microsphere Substances 0.000 description 1
• 210000004688 microtubule Anatomy 0.000 description 1
• BMGQWWVMWDBQGC-IIFHNQTCSA-N midostaurin Chemical compound CN([C@H]1[C@H]([C@]2(C)O[C@@H](N3C4=CC=CC=C4C4=C5C(=O)NCC5=C5C6=CC=CC=C6N2C5=C43)C1)OC)C(=O)C1=CC=CC=C1 BMGQWWVMWDBQGC-IIFHNQTCSA-N 0.000 description 1
• 229950010895 midostaurin Drugs 0.000 description 1
• KKZJGLLVHKMTCM-UHFFFAOYSA-N mitoxantrone Chemical compound O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCCNCCO)=CC=C2NCCNCCO KKZJGLLVHKMTCM-UHFFFAOYSA-N 0.000 description 1
• 229960001156 mitoxantrone Drugs 0.000 description 1
• 238000012544 monitoring process Methods 0.000 description 1
• CQDGTJPVBWZJAZ-UHFFFAOYSA-N monoethyl carbonate Chemical compound CCOC(O)=O CQDGTJPVBWZJAZ-UHFFFAOYSA-N 0.000 description 1
• 229940124303 multikinase inhibitor Drugs 0.000 description 1
• RDSACQWTXKSHJT-NSHDSACASA-N n-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2s)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 description 1
• IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 1
• OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 description 1
• 229930014626 natural product Natural products 0.000 description 1
• 230000017074 necrotic cell death Effects 0.000 description 1
• 208000025402 neoplasm of esophagus Diseases 0.000 description 1
• 230000009826 neoplastic cell growth Effects 0.000 description 1
• 230000003472 neutralizing effect Effects 0.000 description 1
• 239000002547 new drug Substances 0.000 description 1
• 229940080607 nexavar Drugs 0.000 description 1
• 231100001079 no serious adverse effect Toxicity 0.000 description 1
• 239000012457 nonaqueous media Substances 0.000 description 1
• 231100000252 nontoxic Toxicity 0.000 description 1
• 230000003000 nontoxic effect Effects 0.000 description 1
• 238000010606 normalization Methods 0.000 description 1
• 238000003199 nucleic acid amplification method Methods 0.000 description 1
• 239000002417 nutraceutical Substances 0.000 description 1
• 235000021436 nutraceutical agent Nutrition 0.000 description 1
• 208000015380 nutritional deficiency disease Diseases 0.000 description 1
• 229950003600 ombrabulin Drugs 0.000 description 1
• IXWNTLSTOZFSCM-YVACAVLKSA-N ombrabulin Chemical compound C1=C(NC(=O)[C@@H](N)CO)C(OC)=CC=C1\C=C/C1=CC(OC)=C(OC)C(OC)=C1 IXWNTLSTOZFSCM-YVACAVLKSA-N 0.000 description 1
• 229940127240 opiate Drugs 0.000 description 1
• 229960001027 opium Drugs 0.000 description 1
• 229940100688 oral solution Drugs 0.000 description 1
• 229950006354 orantinib Drugs 0.000 description 1
• 150000002895 organic esters Chemical class 0.000 description 1
• 239000003960 organic solvent Substances 0.000 description 1
• 230000002611 ovarian Effects 0.000 description 1
• 229960005184 panobinostat Drugs 0.000 description 1
• FWZRWHZDXBDTFK-ZHACJKMWSA-N panobinostat Chemical compound CC1=NC2=CC=C[CH]C2=C1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FWZRWHZDXBDTFK-ZHACJKMWSA-N 0.000 description 1
• 244000045947 parasite Species 0.000 description 1
• 230000000849 parathyroid Effects 0.000 description 1
• 230000007310 pathophysiology Effects 0.000 description 1
• 239000000312 peanut oil Substances 0.000 description 1
• 239000008188 pellet Substances 0.000 description 1
• 210000004197 pelvis Anatomy 0.000 description 1
• PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 description 1
• 229940111202 pepsin Drugs 0.000 description 1
• 229950010307 peretinoin Drugs 0.000 description 1
• 239000002304 perfume Substances 0.000 description 1
• 230000002688 persistence Effects 0.000 description 1
• WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
• 239000008363 phosphate buffer Substances 0.000 description 1
• 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
• 235000011007 phosphoric acid Nutrition 0.000 description 1
• 230000000865 phosphorylative effect Effects 0.000 description 1
• 230000036314 physical performance Effects 0.000 description 1
• 230000008288 physiological mechanism Effects 0.000 description 1
• 238000009160 phytotherapy Methods 0.000 description 1
• 239000000049 pigment Substances 0.000 description 1
• 229920002647 polyamide Polymers 0.000 description 1
• 229920001296 polysiloxane Polymers 0.000 description 1
• 229920002744 polyvinyl acetate phthalate Polymers 0.000 description 1
• 238000010837 poor prognosis Methods 0.000 description 1
• ZRHANBBTXQZFSP-UHFFFAOYSA-M potassium;4-amino-3,5,6-trichloropyridine-2-carboxylate Chemical compound [K+].NC1=C(Cl)C(Cl)=NC(C([O-])=O)=C1Cl ZRHANBBTXQZFSP-UHFFFAOYSA-M 0.000 description 1
• 229920001592 potato starch Polymers 0.000 description 1
• 238000001556 precipitation Methods 0.000 description 1
• 238000009597 pregnancy test Methods 0.000 description 1
• 230000002028 premature Effects 0.000 description 1
• 239000003755 preservative agent Substances 0.000 description 1
• 230000002265 prevention Effects 0.000 description 1
• 230000008569 process Effects 0.000 description 1
• 239000001294 propane Substances 0.000 description 1
• 239000003380 propellant Substances 0.000 description 1
• 239000000473 propyl gallate Substances 0.000 description 1
• 235000010388 propyl gallate Nutrition 0.000 description 1
• 229940075579 propyl gallate Drugs 0.000 description 1
• 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
• 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
• 235000013772 propylene glycol Nutrition 0.000 description 1
• 229960003415 propylparaben Drugs 0.000 description 1
• 239000003207 proteasome inhibitor Substances 0.000 description 1
• 229940121649 protein inhibitor Drugs 0.000 description 1
• 239000012268 protein inhibitor Substances 0.000 description 1
• 108060006633 protein kinase Proteins 0.000 description 1
• 230000005855 radiation Effects 0.000 description 1
• 150000003254 radicals Chemical class 0.000 description 1
• 108010077182 raf Kinases Proteins 0.000 description 1
• 102000009929 raf Kinases Human genes 0.000 description 1
• 229960002633 ramucirumab Drugs 0.000 description 1
• ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 description 1
• 230000000306 recurrent effect Effects 0.000 description 1
• 229950008933 refametinib Drugs 0.000 description 1
• 230000001105 regulatory effect Effects 0.000 description 1
• 230000001850 reproductive effect Effects 0.000 description 1
• 229940127558 rescue medication Drugs 0.000 description 1
• FECGNJPYVFEKOD-VMPITWQZSA-N resminostat Chemical compound C1=CC(CN(C)C)=CC=C1S(=O)(=O)N1C=C(\C=C\C(=O)NO)C=C1 FECGNJPYVFEKOD-VMPITWQZSA-N 0.000 description 1
• 229950002821 resminostat Drugs 0.000 description 1
• 230000000241 respiratory effect Effects 0.000 description 1
• 230000004044 response Effects 0.000 description 1
• 229950003238 rilotumumab Drugs 0.000 description 1
• 235000005713 safflower oil Nutrition 0.000 description 1
• 239000003813 safflower oil Substances 0.000 description 1
• 230000009291 secondary effect Effects 0.000 description 1
• 239000004208 shellac Substances 0.000 description 1
• ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 description 1
• 229940113147 shellac Drugs 0.000 description 1
• 235000013874 shellac Nutrition 0.000 description 1
• 230000011664 signaling Effects 0.000 description 1
• 229960002930 sirolimus Drugs 0.000 description 1
• QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 1
• 210000003491 skin Anatomy 0.000 description 1
• 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
• 235000017557 sodium bicarbonate Nutrition 0.000 description 1
• WBHQBSYUUJJSRZ-UHFFFAOYSA-M sodium bisulfate Chemical compound [Na+].OS([O-])(=O)=O WBHQBSYUUJJSRZ-UHFFFAOYSA-M 0.000 description 1
• 229910000342 sodium bisulfate Inorganic materials 0.000 description 1
• 229940100996 sodium bisulfate Drugs 0.000 description 1
• 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
• 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
• HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
• 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
• 229940001584 sodium metabisulfite Drugs 0.000 description 1
• 235000010262 sodium metabisulphite Nutrition 0.000 description 1
• 229940001482 sodium sulfite Drugs 0.000 description 1
• 235000010265 sodium sulphite Nutrition 0.000 description 1
• 238000012358 sourcing Methods 0.000 description 1
• 239000003549 soybean oil Substances 0.000 description 1
• 235000012424 soybean oil Nutrition 0.000 description 1
• 229940068117 sprycel Drugs 0.000 description 1
• 102000009076 src-Family Kinases Human genes 0.000 description 1
• 108010087686 src-Family Kinases Proteins 0.000 description 1
• 238000000528 statistical test Methods 0.000 description 1
• 239000008174 sterile solution Substances 0.000 description 1
• 150000003431 steroids Chemical class 0.000 description 1
• 238000003860 storage Methods 0.000 description 1
• 238000007920 subcutaneous administration Methods 0.000 description 1
• 238000010254 subcutaneous injection Methods 0.000 description 1
• 239000000758 substrate Substances 0.000 description 1
• 239000005720 sucrose Substances 0.000 description 1
• 235000000346 sugar Nutrition 0.000 description 1
• 150000008163 sugars Chemical class 0.000 description 1
• 229960002812 sunitinib malate Drugs 0.000 description 1
• 239000004094 surface-active agent Substances 0.000 description 1
• 238000001356 surgical procedure Methods 0.000 description 1
• 230000004083 survival effect Effects 0.000 description 1
• 239000000375 suspending agent Substances 0.000 description 1
• 208000011580 syndromic disease Diseases 0.000 description 1
• 230000002194 synthesizing effect Effects 0.000 description 1
• 239000006188 syrup Substances 0.000 description 1
• 235000020357 syrup Nutrition 0.000 description 1
• 238000012353 t test Methods 0.000 description 1
• 229920001864 tannin Polymers 0.000 description 1
• 239000001648 tannin Substances 0.000 description 1
• 235000018553 tannin Nutrition 0.000 description 1
• 230000008685 targeting Effects 0.000 description 1
• 239000011975 tartaric acid Substances 0.000 description 1
• 235000002906 tartaric acid Nutrition 0.000 description 1
• 229950001899 tasquinimod Drugs 0.000 description 1
• ONDYALNGTUAJDX-UHFFFAOYSA-N tasquinimod Chemical compound OC=1C=2C(OC)=CC=CC=2N(C)C(=O)C=1C(=O)N(C)C1=CC=C(C(F)(F)F)C=C1 ONDYALNGTUAJDX-UHFFFAOYSA-N 0.000 description 1
• 208000002918 testicular germ cell tumor Diseases 0.000 description 1
• 238000011287 therapeutic dose Methods 0.000 description 1
• 230000001225 therapeutic effect Effects 0.000 description 1
• 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 description 1
• 229940104230 thymidine Drugs 0.000 description 1
• 210000001685 thyroid gland Anatomy 0.000 description 1
• 229940098465 tincture Drugs 0.000 description 1
• 210000001519 tissue Anatomy 0.000 description 1
• 229960005196 titanium dioxide Drugs 0.000 description 1
• OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
• 229950005976 tivantinib Drugs 0.000 description 1
• 229960005048 toceranib Drugs 0.000 description 1
• AOBORMOPSGHCAX-DGHZZKTQSA-N tocofersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2O[C@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-DGHZZKTQSA-N 0.000 description 1
• 229960000984 tocofersolan Drugs 0.000 description 1
• 231100000331 toxic Toxicity 0.000 description 1
• 230000002588 toxic effect Effects 0.000 description 1
• 231100000041 toxicology testing Toxicity 0.000 description 1
• 239000003053 toxin Substances 0.000 description 1
• 231100000765 toxin Toxicity 0.000 description 1
• 108700012359 toxins Proteins 0.000 description 1
• 238000013518 transcription Methods 0.000 description 1
• 230000035897 transcription Effects 0.000 description 1
• 229960001612 trastuzumab emtansine Drugs 0.000 description 1
• 238000011269 treatment regimen Methods 0.000 description 1
• 108010075758 trebananib Proteins 0.000 description 1
• 229950001210 trebananib Drugs 0.000 description 1
• 229950007217 tremelimumab Drugs 0.000 description 1
• 239000001069 triethyl citrate Substances 0.000 description 1
• 235000013769 triethyl citrate Nutrition 0.000 description 1
• VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
• OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
• 241001529453 unidentified herpesvirus Species 0.000 description 1
• 235000015112 vegetable and seed oil Nutrition 0.000 description 1
• 235000019871 vegetable fat Nutrition 0.000 description 1
• 239000008158 vegetable oil Substances 0.000 description 1
• 230000002861 ventricular Effects 0.000 description 1
• 239000000080 wetting agent Substances 0.000 description 1
• 239000002023 wood Substances 0.000 description 1
• 239000000230 xanthan gum Substances 0.000 description 1
• 235000010493 xanthan gum Nutrition 0.000 description 1
• 229920001285 xanthan gum Polymers 0.000 description 1
• 229940082509 xanthan gum Drugs 0.000 description 1
• 229940055760 yervoy Drugs 0.000 description 1
• 239000011787 zinc oxide Substances 0.000 description 1
• 235000014692 zinc oxide Nutrition 0.000 description 1
• 239000002076 α-tocopherol Substances 0.000 description 1
• 235000004835 α-tocopherol Nutrition 0.000 description 1