JP2016516800A - フコシル化が少ない抗egfr抗体による抗がん処置 - Google Patents
フコシル化が少ない抗egfr抗体による抗がん処置 Download PDFInfo
- Publication number
- JP2016516800A JP2016516800A JP2016508192A JP2016508192A JP2016516800A JP 2016516800 A JP2016516800 A JP 2016516800A JP 2016508192 A JP2016508192 A JP 2016508192A JP 2016508192 A JP2016508192 A JP 2016508192A JP 2016516800 A JP2016516800 A JP 2016516800A
- Authority
- JP
- Japan
- Prior art keywords
- egfr
- egfr antibody
- fucose
- antibody
- cancer
- Prior art date
- 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.)
- Withdrawn
Links
- 230000033581 fucosylation Effects 0.000 title abstract description 18
- 238000011394 anticancer treatment Methods 0.000 title description 7
- SHZGCJCMOBCMKK-DHVFOXMCSA-N L-fucopyranose Chemical compound C[C@@H]1OC(O)[C@@H](O)[C@H](O)[C@@H]1O SHZGCJCMOBCMKK-DHVFOXMCSA-N 0.000 claims abstract description 250
- SHZGCJCMOBCMKK-UHFFFAOYSA-N D-mannomethylose Natural products CC1OC(O)C(O)C(O)C1O SHZGCJCMOBCMKK-UHFFFAOYSA-N 0.000 claims abstract description 239
- PNNNRSAQSRJVSB-SLPGGIOYSA-N Fucose Natural products C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C=O PNNNRSAQSRJVSB-SLPGGIOYSA-N 0.000 claims abstract description 232
- 230000002411 adverse Effects 0.000 claims abstract description 188
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 168
- 230000002829 reductive effect Effects 0.000 claims abstract description 167
- 201000010099 disease Diseases 0.000 claims abstract description 166
- 230000001613 neoplastic effect Effects 0.000 claims abstract description 134
- 230000013595 glycosylation Effects 0.000 claims abstract description 112
- 238000006206 glycosylation reaction Methods 0.000 claims abstract description 112
- 241000282414 Homo sapiens Species 0.000 claims abstract description 111
- 230000000694 effects Effects 0.000 claims abstract description 36
- 230000001419 dependent effect Effects 0.000 claims abstract description 11
- 230000001413 cellular effect Effects 0.000 claims abstract description 10
- 230000007402 cytotoxic response Effects 0.000 claims abstract description 10
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims abstract 72
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims abstract 72
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims abstract 71
- 238000011282 treatment Methods 0.000 claims description 331
- 206010028980 Neoplasm Diseases 0.000 claims description 209
- 206010040914 Skin reaction Diseases 0.000 claims description 208
- 231100000430 skin reaction Toxicity 0.000 claims description 208
- 230000035483 skin reaction Effects 0.000 claims description 208
- 210000004027 cell Anatomy 0.000 claims description 153
- 201000011510 cancer Diseases 0.000 claims description 128
- 229940121647 egfr inhibitor Drugs 0.000 claims description 106
- 208000010201 Exanthema Diseases 0.000 claims description 100
- 201000005884 exanthem Diseases 0.000 claims description 100
- 206010037844 rash Diseases 0.000 claims description 100
- 229960005395 cetuximab Drugs 0.000 claims description 83
- 206010027476 Metastases Diseases 0.000 claims description 72
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 68
- 231100000046 skin rash Toxicity 0.000 claims description 68
- 229940082789 erbitux Drugs 0.000 claims description 67
- 206010067484 Adverse reaction Diseases 0.000 claims description 66
- 230000006838 adverse reaction Effects 0.000 claims description 66
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 65
- 206010000496 acne Diseases 0.000 claims description 65
- 238000000034 method Methods 0.000 claims description 64
- 230000027455 binding Effects 0.000 claims description 60
- 230000010056 antibody-dependent cellular cytotoxicity Effects 0.000 claims description 53
- 230000001225 therapeutic effect Effects 0.000 claims description 51
- 239000002246 antineoplastic agent Substances 0.000 claims description 50
- 229940127089 cytotoxic agent Drugs 0.000 claims description 44
- 210000003714 granulocyte Anatomy 0.000 claims description 41
- 229960001972 panitumumab Drugs 0.000 claims description 41
- 230000001939 inductive effect Effects 0.000 claims description 39
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 36
- 206010038389 Renal cancer Diseases 0.000 claims description 34
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 34
- 201000010982 kidney cancer Diseases 0.000 claims description 34
- 150000001413 amino acids Chemical group 0.000 claims description 33
- 230000009401 metastasis Effects 0.000 claims description 33
- 230000004913 activation Effects 0.000 claims description 32
- 206010017758 gastric cancer Diseases 0.000 claims description 32
- 201000011549 stomach cancer Diseases 0.000 claims description 32
- 210000002540 macrophage Anatomy 0.000 claims description 31
- 230000003211 malignant effect Effects 0.000 claims description 31
- 102100029193 Low affinity immunoglobulin gamma Fc region receptor III-A Human genes 0.000 claims description 28
- 239000003795 chemical substances by application Substances 0.000 claims description 27
- 206010009944 Colon cancer Diseases 0.000 claims description 23
- SQVRNKJHWKZAKO-UHFFFAOYSA-N beta-N-Acetyl-D-neuraminic acid Natural products CC(=O)NC1C(O)CC(O)(C(O)=O)OC1C(O)C(O)CO SQVRNKJHWKZAKO-UHFFFAOYSA-N 0.000 claims description 21
- 208000030808 Clear cell renal carcinoma Diseases 0.000 claims description 20
- 206010021027 Hypomagnesaemia Diseases 0.000 claims description 20
- 206010073251 clear cell renal cell carcinoma Diseases 0.000 claims description 20
- 201000011330 nonpapillary renal cell carcinoma Diseases 0.000 claims description 20
- OVRNDRQMDRJTHS-UHFFFAOYSA-N N-acelyl-D-glucosamine Natural products CC(=O)NC1C(O)OC(CO)C(O)C1O OVRNDRQMDRJTHS-UHFFFAOYSA-N 0.000 claims description 19
- OVRNDRQMDRJTHS-RTRLPJTCSA-N N-acetyl-D-glucosamine Chemical compound CC(=O)N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-RTRLPJTCSA-N 0.000 claims description 19
- MBLBDJOUHNCFQT-LXGUWJNJSA-N N-acetylglucosamine Natural products CC(=O)N[C@@H](C=O)[C@@H](O)[C@H](O)[C@H](O)CO MBLBDJOUHNCFQT-LXGUWJNJSA-N 0.000 claims description 19
- 208000002193 Pain Diseases 0.000 claims description 19
- 230000028993 immune response Effects 0.000 claims description 19
- 230000036407 pain Effects 0.000 claims description 19
- 239000003814 drug Substances 0.000 claims description 18
- 229930182830 galactose Natural products 0.000 claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims description 18
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 17
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 17
- 238000001959 radiotherapy Methods 0.000 claims description 17
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 16
- 229960002949 fluorouracil Drugs 0.000 claims description 16
- 229960004768 irinotecan Drugs 0.000 claims description 16
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound 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 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims description 16
- 101000917858 Homo sapiens Low affinity immunoglobulin gamma Fc region receptor III-A Proteins 0.000 claims description 15
- 125000005629 sialic acid group Chemical group 0.000 claims description 15
- 102000004127 Cytokines Human genes 0.000 claims description 14
- 108090000695 Cytokines Proteins 0.000 claims description 14
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 14
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims description 14
- SQVRNKJHWKZAKO-OQPLDHBCSA-N sialic acid Chemical compound CC(=O)N[C@@H]1[C@@H](O)C[C@@](O)(C(O)=O)OC1[C@H](O)[C@H](O)CO SQVRNKJHWKZAKO-OQPLDHBCSA-N 0.000 claims description 14
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 14
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 13
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 13
- 208000029742 colonic neoplasm Diseases 0.000 claims description 13
- 201000004101 esophageal cancer Diseases 0.000 claims description 13
- 201000005202 lung cancer Diseases 0.000 claims description 13
- 208000020816 lung neoplasm Diseases 0.000 claims description 13
- 230000035772 mutation Effects 0.000 claims description 13
- 210000000822 natural killer cell Anatomy 0.000 claims description 13
- 238000001356 surgical procedure Methods 0.000 claims description 13
- 206010012735 Diarrhoea Diseases 0.000 claims description 12
- 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 claims description 12
- 101710099301 Low affinity immunoglobulin gamma Fc region receptor III-A Proteins 0.000 claims description 12
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 12
- 208000026310 Breast neoplasm Diseases 0.000 claims description 11
- QIGJYVCQYDKYDW-SDOYDPJRSA-N alpha-D-galactosyl-(1->3)-D-galactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@H]1[C@@H](O)[C@@H](CO)OC(O)[C@@H]1O QIGJYVCQYDKYDW-SDOYDPJRSA-N 0.000 claims description 11
- 230000006698 induction Effects 0.000 claims description 11
- 206010006187 Breast cancer Diseases 0.000 claims description 10
- 206010033128 Ovarian cancer Diseases 0.000 claims description 10
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 10
- 238000006243 chemical reaction Methods 0.000 claims description 10
- 230000001394 metastastic effect Effects 0.000 claims description 10
- 208000037819 metastatic cancer Diseases 0.000 claims description 10
- 208000011575 metastatic malignant neoplasm Diseases 0.000 claims description 10
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 10
- 238000009097 single-agent therapy Methods 0.000 claims description 10
- 210000002784 stomach Anatomy 0.000 claims description 10
- 206010040844 Skin exfoliation Diseases 0.000 claims description 9
- 208000025865 Ulcer Diseases 0.000 claims description 9
- 208000009956 adenocarcinoma Diseases 0.000 claims description 9
- 238000009098 adjuvant therapy Methods 0.000 claims description 9
- 150000001720 carbohydrates Chemical group 0.000 claims description 9
- 230000035618 desquamation Effects 0.000 claims description 9
- 229940079593 drug Drugs 0.000 claims description 9
- 210000003979 eosinophil Anatomy 0.000 claims description 9
- OSVMTWJCGUFAOD-KZQROQTASA-N formestane Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1O OSVMTWJCGUFAOD-KZQROQTASA-N 0.000 claims description 9
- 150000002256 galaktoses Chemical class 0.000 claims description 9
- 150000004676 glycans Chemical class 0.000 claims description 9
- 210000000440 neutrophil Anatomy 0.000 claims description 9
- 230000036961 partial effect Effects 0.000 claims description 9
- 206010020751 Hypersensitivity Diseases 0.000 claims description 8
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 8
- 238000002648 combination therapy Methods 0.000 claims description 8
- 210000002865 immune cell Anatomy 0.000 claims description 8
- 239000003446 ligand Substances 0.000 claims description 8
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 8
- 229960001756 oxaliplatin Drugs 0.000 claims description 8
- 210000004303 peritoneum Anatomy 0.000 claims description 8
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims description 7
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 7
- 230000006907 apoptotic process Effects 0.000 claims description 7
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 7
- 201000002528 pancreatic cancer Diseases 0.000 claims description 7
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 7
- 201000010279 papillary renal cell carcinoma Diseases 0.000 claims description 7
- 229910052697 platinum Inorganic materials 0.000 claims description 7
- 210000004224 pleura Anatomy 0.000 claims description 7
- 238000009101 premedication Methods 0.000 claims description 7
- 208000024891 symptom Diseases 0.000 claims description 7
- 230000036269 ulceration Effects 0.000 claims description 7
- 230000003442 weekly effect Effects 0.000 claims description 7
- PJMNEPMSGCRSRC-IEVKOWOJSA-N 4-androstene-3,6,17-trione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=O)C2=C1 PJMNEPMSGCRSRC-IEVKOWOJSA-N 0.000 claims description 6
- 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 claims description 6
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 6
- 201000009030 Carcinoma Diseases 0.000 claims description 6
- 102000004190 Enzymes Human genes 0.000 claims description 6
- 108090000790 Enzymes Proteins 0.000 claims description 6
- 208000019025 Hypokalemia Diseases 0.000 claims description 6
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims description 6
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 6
- 206010025538 Malignant ascites Diseases 0.000 claims description 6
- FDJKUWYYUZCUJX-KVNVFURPSA-N N-glycolylneuraminic acid Chemical compound OC[C@H](O)[C@H](O)[C@@H]1O[C@](O)(C(O)=O)C[C@H](O)[C@H]1NC(=O)CO FDJKUWYYUZCUJX-KVNVFURPSA-N 0.000 claims description 6
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 6
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims description 6
- 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 claims description 6
- 238000006471 dimerization reaction Methods 0.000 claims description 6
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims description 6
- 229960004679 doxorubicin Drugs 0.000 claims description 6
- CTSPAMFJBXKSOY-UHFFFAOYSA-N ellipticine Chemical compound N1=CC=C2C(C)=C(NC=3C4=CC=CC=3)C4=C(C)C2=C1 CTSPAMFJBXKSOY-UHFFFAOYSA-N 0.000 claims description 6
- 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 claims description 6
- 235000008191 folinic acid Nutrition 0.000 claims description 6
- 239000011672 folinic acid Substances 0.000 claims description 6
- 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 claims description 6
- 229960005277 gemcitabine Drugs 0.000 claims description 6
- ATHLLZUXVPNPAW-UHFFFAOYSA-N lamellarin d Chemical compound C1=C(O)C(OC)=CC(C2=C3C4=CC(OC)=C(O)C=C4C=CN3C3=C2C=2C=C(OC)C(O)=CC=2OC3=O)=C1 ATHLLZUXVPNPAW-UHFFFAOYSA-N 0.000 claims description 6
- 229960004891 lapatinib Drugs 0.000 claims description 6
- 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 6
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims description 6
- 229960001691 leucovorin Drugs 0.000 claims description 6
- 229960001156 mitoxantrone Drugs 0.000 claims description 6
- 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 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims description 6
- 208000024896 potassium deficiency disease Diseases 0.000 claims description 6
- 206010038038 rectal cancer Diseases 0.000 claims description 6
- 201000001275 rectum cancer Diseases 0.000 claims description 6
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims description 6
- 239000004474 valine Substances 0.000 claims description 6
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims description 5
- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 claims description 5
- 206010012441 Dermatitis bullous Diseases 0.000 claims description 5
- 206010012455 Dermatitis exfoliative Diseases 0.000 claims description 5
- 206010014733 Endometrial cancer Diseases 0.000 claims description 5
- MPJKWIXIYCLVCU-UHFFFAOYSA-N Folinic acid Natural products NC1=NC2=C(N(C=O)C(CNc3ccc(cc3)C(=O)NC(CCC(=O)O)CC(=O)O)CN2)C(=O)N1 MPJKWIXIYCLVCU-UHFFFAOYSA-N 0.000 claims description 5
- 206010033733 Papule Diseases 0.000 claims description 5
- 208000003251 Pruritus Diseases 0.000 claims description 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 5
- 208000030961 allergic reaction Diseases 0.000 claims description 5
- 229960000397 bevacizumab Drugs 0.000 claims description 5
- 201000010881 cervical cancer Diseases 0.000 claims description 5
- 229960004316 cisplatin Drugs 0.000 claims description 5
- 230000009089 cytolysis Effects 0.000 claims description 5
- 230000006378 damage Effects 0.000 claims description 5
- 229960000975 daunorubicin Drugs 0.000 claims description 5
- STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin 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(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims description 5
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 5
- 210000004072 lung Anatomy 0.000 claims description 5
- HRGDZIGMBDGFTC-UHFFFAOYSA-N platinum(2+) Chemical compound [Pt+2] HRGDZIGMBDGFTC-UHFFFAOYSA-N 0.000 claims description 5
- 230000003389 potentiating effect Effects 0.000 claims description 5
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 4
- 208000036764 Adenocarcinoma of the esophagus Diseases 0.000 claims description 4
- 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 claims 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 claims description 4
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 4
- 208000019487 Clear cell papillary renal cell carcinoma Diseases 0.000 claims description 4
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 4
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims description 4
- 208000032271 Malignant tumor of penis Diseases 0.000 claims description 4
- 208000002471 Penile Neoplasms Diseases 0.000 claims description 4
- 206010034299 Penile cancer Diseases 0.000 claims description 4
- 230000001754 anti-pyretic effect Effects 0.000 claims description 4
- 229960000455 brentuximab vedotin Drugs 0.000 claims description 4
- 229960004117 capecitabine Drugs 0.000 claims description 4
- 229960004562 carboplatin Drugs 0.000 claims description 4
- 210000000981 epithelium Anatomy 0.000 claims description 4
- 229960001433 erlotinib Drugs 0.000 claims description 4
- 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 4
- 208000028653 esophageal adenocarcinoma Diseases 0.000 claims description 4
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims description 4
- 229960004421 formestane Drugs 0.000 claims description 4
- 229960002584 gefitinib Drugs 0.000 claims description 4
- 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 4
- 201000010536 head and neck cancer Diseases 0.000 claims description 4
- 238000009099 neoadjuvant therapy Methods 0.000 claims description 4
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 4
- 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 4
- 238000012360 testing method Methods 0.000 claims description 4
- 229960000303 topotecan Drugs 0.000 claims description 4
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims description 4
- SSJXIUAHEKJCMH-PHDIDXHHSA-N (1r,2r)-cyclohexane-1,2-diamine Chemical compound N[C@@H]1CCCC[C@H]1N SSJXIUAHEKJCMH-PHDIDXHHSA-N 0.000 claims description 3
- WDXXEUARVHTWQF-DLBZAZTESA-N 3-hydroxy-2-[(1r,6r)-3-methyl-6-prop-1-en-2-ylcyclohex-2-en-1-yl]-5-pentylcyclohexa-2,5-diene-1,4-dione Chemical compound O=C1C(CCCCC)=CC(=O)C([C@H]2[C@@H](CCC(C)=C2)C(C)=C)=C1O WDXXEUARVHTWQF-DLBZAZTESA-N 0.000 claims description 3
- CLPFFLWZZBQMAO-UHFFFAOYSA-N 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile Chemical compound C1=CC(C#N)=CC=C1C1N2C=NC=C2CCC1 CLPFFLWZZBQMAO-UHFFFAOYSA-N 0.000 claims description 3
- 241000321096 Adenoides Species 0.000 claims description 3
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims description 3
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 3
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims description 3
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 3
- ZIXGXMMUKPLXBB-UHFFFAOYSA-N Guatambuinine Natural products N1C2=CC=CC=C2C2=C1C(C)=C1C=CN=C(C)C1=C2 ZIXGXMMUKPLXBB-UHFFFAOYSA-N 0.000 claims description 3
- XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 claims description 3
- XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 claims description 3
- 102100037850 Interferon gamma Human genes 0.000 claims description 3
- 108010074328 Interferon-gamma Proteins 0.000 claims description 3
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims description 3
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 3
- WPPTYUSIXLFOKZ-BYOOWSCBSA-N O([C@H]1[C@H]2[C@@](C([C@H](OC(=O)C3CC3)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=C(C)C)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 Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](OC(=O)C3CC3)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=C(C)C)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 WPPTYUSIXLFOKZ-BYOOWSCBSA-N 0.000 claims description 3
- 206010037888 Rash pustular Diseases 0.000 claims description 3
- SUYXJDLXGFPMCQ-INIZCTEOSA-N SJ000287331 Natural products CC1=c2cnccc2=C(C)C2=Nc3ccccc3[C@H]12 SUYXJDLXGFPMCQ-INIZCTEOSA-N 0.000 claims description 3
- 208000003252 Signet Ring Cell Carcinoma Diseases 0.000 claims description 3
- 229940123237 Taxane Drugs 0.000 claims description 3
- WFWLQNSHRPWKFK-UHFFFAOYSA-N Tegafur Chemical compound O=C1NC(=O)C(F)=CN1C1OCCC1 WFWLQNSHRPWKFK-UHFFFAOYSA-N 0.000 claims description 3
- 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 claims description 3
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims description 3
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 3
- 208000000260 Warts Diseases 0.000 claims description 3
- 230000003213 activating effect Effects 0.000 claims description 3
- 210000002534 adenoid Anatomy 0.000 claims description 3
- 201000000452 adenoid squamous cell carcinoma Diseases 0.000 claims description 3
- 229960003437 aminoglutethimide Drugs 0.000 claims description 3
- ROBVIMPUHSLWNV-UHFFFAOYSA-N aminoglutethimide Chemical compound C=1C=C(N)C=CC=1C1(CC)CCC(=O)NC1=O ROBVIMPUHSLWNV-UHFFFAOYSA-N 0.000 claims description 3
- XCPGHVQEEXUHNC-UHFFFAOYSA-N amsacrine Chemical compound COC1=CC(NS(C)(=O)=O)=CC=C1NC1=C(C=CC=C2)C2=NC2=CC=CC=C12 XCPGHVQEEXUHNC-UHFFFAOYSA-N 0.000 claims description 3
- 229960001220 amsacrine Drugs 0.000 claims description 3
- 229960002932 anastrozole Drugs 0.000 claims description 3
- 229940045799 anthracyclines and related substance Drugs 0.000 claims description 3
- 239000002221 antipyretic Substances 0.000 claims description 3
- 229940078010 arimidex Drugs 0.000 claims description 3
- 229940087620 aromasin Drugs 0.000 claims description 3
- 239000003886 aromatase inhibitor Substances 0.000 claims description 3
- 229940046844 aromatase inhibitors Drugs 0.000 claims description 3
- GIXWDMTZECRIJT-UHFFFAOYSA-N aurintricarboxylic acid Chemical compound C1=CC(=O)C(C(=O)O)=CC1=C(C=1C=C(C(O)=CC=1)C(O)=O)C1=CC=C(O)C(C(O)=O)=C1 GIXWDMTZECRIJT-UHFFFAOYSA-N 0.000 claims description 3
- 229940127093 camptothecin Drugs 0.000 claims description 3
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims description 3
- 230000004663 cell proliferation Effects 0.000 claims description 3
- 229960004397 cyclophosphamide Drugs 0.000 claims description 3
- 229960000684 cytarabine Drugs 0.000 claims description 3
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims description 3
- 102000015694 estrogen receptors Human genes 0.000 claims description 3
- 108010038795 estrogen receptors Proteins 0.000 claims description 3
- 229950011548 fadrozole Drugs 0.000 claims description 3
- 229940087476 femara Drugs 0.000 claims description 3
- ODKNJVUHOIMIIZ-RRKCRQDMSA-N floxuridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(F)=C1 ODKNJVUHOIMIIZ-RRKCRQDMSA-N 0.000 claims description 3
- 229960000961 floxuridine Drugs 0.000 claims description 3
- 201000010175 gallbladder cancer Diseases 0.000 claims description 3
- 201000006585 gastric adenocarcinoma Diseases 0.000 claims description 3
- 230000002496 gastric effect Effects 0.000 claims description 3
- 229940022353 herceptin Drugs 0.000 claims description 3
- 229960000908 idarubicin Drugs 0.000 claims description 3
- 229940121354 immunomodulator Drugs 0.000 claims description 3
- 238000001802 infusion Methods 0.000 claims description 3
- 239000003112 inhibitor Substances 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 230000003993 interaction Effects 0.000 claims description 3
- 210000003734 kidney Anatomy 0.000 claims description 3
- 150000002596 lactones Chemical class 0.000 claims description 3
- 229960003881 letrozole Drugs 0.000 claims description 3
- 201000007270 liver cancer Diseases 0.000 claims description 3
- 208000014018 liver neoplasm Diseases 0.000 claims description 3
- 229960000485 methotrexate Drugs 0.000 claims description 3
- ZDZOTLJHXYCWBA-BSEPLHNVSA-N molport-006-823-826 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-BSEPLHNVSA-N 0.000 claims description 3
- 201000010879 mucinous adenocarcinoma Diseases 0.000 claims description 3
- 229950010203 nimotuzumab Drugs 0.000 claims description 3
- 238000002638 palliative care Methods 0.000 claims description 3
- 208000004019 papillary adenocarcinoma Diseases 0.000 claims description 3
- 229960005079 pemetrexed Drugs 0.000 claims 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 claims description 3
- 229960002087 pertuzumab Drugs 0.000 claims description 3
- 208000013368 pseudoglandular squamous cell carcinoma Diseases 0.000 claims description 3
- 125000000561 purinyl group Chemical class N1=C(N=C2N=CNC2=C1)* 0.000 claims description 3
- 208000029561 pustule Diseases 0.000 claims description 3
- 150000003230 pyrimidines Chemical class 0.000 claims description 3
- 229960004432 raltitrexed Drugs 0.000 claims description 3
- 230000000306 recurrent effect Effects 0.000 claims description 3
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims description 3
- 201000008123 signet ring cell adenocarcinoma Diseases 0.000 claims description 3
- 201000010153 skin papilloma Diseases 0.000 claims description 3
- 230000009885 systemic effect Effects 0.000 claims description 3
- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 claims description 3
- 229960001278 teniposide Drugs 0.000 claims description 3
- BPEWUONYVDABNZ-DZBHQSCQSA-N testolactone Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(OC(=O)CC4)[C@@H]4[C@@H]3CCC2=C1 BPEWUONYVDABNZ-DZBHQSCQSA-N 0.000 claims description 3
- 229960005353 testolactone Drugs 0.000 claims description 3
- 229960000575 trastuzumab Drugs 0.000 claims description 3
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims description 3
- 201000007423 tubular adenocarcinoma Diseases 0.000 claims description 3
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 3
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 3
- 150000004917 tyrosine kinase inhibitor derivatives Chemical group 0.000 claims description 3
- 206010046766 uterine cancer Diseases 0.000 claims description 3
- 229960000653 valrubicin Drugs 0.000 claims description 3
- ZOCKGBMQLCSHFP-KQRAQHLDSA-N valrubicin Chemical compound O([C@H]1C[C@](CC2=C(O)C=3C(=O)C4=CC=CC(OC)=C4C(=O)C=3C(O)=C21)(O)C(=O)COC(=O)CCCC)[C@H]1C[C@H](NC(=O)C(F)(F)F)[C@H](O)[C@H](C)O1 ZOCKGBMQLCSHFP-KQRAQHLDSA-N 0.000 claims description 3
- 229960002066 vinorelbine Drugs 0.000 claims description 3
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 claims description 3
- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 claims description 2
- 206010001150 Adenocarcinoma gastric Diseases 0.000 claims description 2
- 206010057649 Endometrial sarcoma Diseases 0.000 claims description 2
- UKCVAQGKEOJTSR-UHFFFAOYSA-N Fadrozole hydrochloride Chemical compound Cl.C1=CC(C#N)=CC=C1C1N2C=NC=C2CCC1 UKCVAQGKEOJTSR-UHFFFAOYSA-N 0.000 claims description 2
- 102000018713 Histocompatibility Antigens Class II Human genes 0.000 claims description 2
- 108010027412 Histocompatibility Antigens Class II Proteins 0.000 claims description 2
- 102000004889 Interleukin-6 Human genes 0.000 claims description 2
- 108090001005 Interleukin-6 Proteins 0.000 claims description 2
- 108090001007 Interleukin-8 Proteins 0.000 claims description 2
- 102000004890 Interleukin-8 Human genes 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 102000043129 MHC class I family Human genes 0.000 claims description 2
- 108091054437 MHC class I family Proteins 0.000 claims description 2
- 206010030137 Oesophageal adenocarcinoma Diseases 0.000 claims description 2
- 239000004098 Tetracycline Substances 0.000 claims description 2
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims description 2
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims description 2
- 239000013543 active substance Substances 0.000 claims description 2
- 239000000739 antihistaminic agent Substances 0.000 claims description 2
- 229940045686 antimetabolites antineoplastic purine analogs Drugs 0.000 claims description 2
- 229940045688 antineoplastic antimetabolites pyrimidine analogues Drugs 0.000 claims description 2
- 229940125716 antipyretic agent Drugs 0.000 claims description 2
- 230000000903 blocking effect Effects 0.000 claims description 2
- 230000037396 body weight Effects 0.000 claims description 2
- 230000003013 cytotoxicity Effects 0.000 claims description 2
- 231100000135 cytotoxicity Toxicity 0.000 claims description 2
- 229960000255 exemestane Drugs 0.000 claims description 2
- 208000004526 exfoliative dermatitis Diseases 0.000 claims description 2
- 239000004052 folic acid antagonist Substances 0.000 claims description 2
- 201000007492 gastroesophageal junction adenocarcinoma Diseases 0.000 claims description 2
- 229960003297 gemtuzumab ozogamicin Drugs 0.000 claims description 2
- 210000004907 gland Anatomy 0.000 claims description 2
- 239000012642 immune effector Substances 0.000 claims description 2
- 102000009634 interleukin-1 receptor antagonist activity proteins Human genes 0.000 claims description 2
- 108040001669 interleukin-1 receptor antagonist activity proteins Proteins 0.000 claims description 2
- 239000002502 liposome Substances 0.000 claims description 2
- 201000005243 lung squamous cell carcinoma Diseases 0.000 claims description 2
- 230000004060 metabolic process Effects 0.000 claims description 2
- 229960000214 pralatrexate Drugs 0.000 claims description 2
- OGSBUKJUDHAQEA-WMCAAGNKSA-N pralatrexate Chemical compound C1=NC2=NC(N)=NC(N)=C2N=C1CC(CC#C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OGSBUKJUDHAQEA-WMCAAGNKSA-N 0.000 claims description 2
- 229960002180 tetracycline Drugs 0.000 claims description 2
- 229930101283 tetracycline Natural products 0.000 claims description 2
- 235000019364 tetracycline Nutrition 0.000 claims description 2
- 150000003522 tetracyclines Chemical class 0.000 claims description 2
- 239000003053 toxin Substances 0.000 claims description 2
- 231100000765 toxin Toxicity 0.000 claims description 2
- 108700012359 toxins Proteins 0.000 claims description 2
- 229960001771 vorozole Drugs 0.000 claims description 2
- XLMPPFTZALNBFS-INIZCTEOSA-N vorozole Chemical compound C1([C@@H](C2=CC=C3N=NN(C3=C2)C)N2N=CN=C2)=CC=C(Cl)C=C1 XLMPPFTZALNBFS-INIZCTEOSA-N 0.000 claims description 2
- SQVRNKJHWKZAKO-LUWBGTNYSA-N N-acetylneuraminic acid Chemical compound CC(=O)N[C@@H]1[C@@H](O)CC(O)(C(O)=O)O[C@H]1[C@H](O)[C@H](O)CO SQVRNKJHWKZAKO-LUWBGTNYSA-N 0.000 claims 4
- 229940060155 neuac Drugs 0.000 claims 4
- CERZMXAJYMMUDR-UHFFFAOYSA-N neuraminic acid Natural products NC1C(O)CC(O)(C(O)=O)OC1C(O)C(O)CO CERZMXAJYMMUDR-UHFFFAOYSA-N 0.000 claims 4
- 101100193693 Kirsten murine sarcoma virus K-RAS gene Proteins 0.000 claims 2
- 206010064390 Tumour invasion Diseases 0.000 claims 2
- 230000009400 cancer invasion Effects 0.000 claims 2
- 102100025248 C-X-C motif chemokine 10 Human genes 0.000 claims 1
- 101710098275 C-X-C motif chemokine 10 Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010042566 Superinfection Diseases 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000003432 anti-folate effect Effects 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 229940127074 antifolate Drugs 0.000 claims 1
- 210000003651 basophil Anatomy 0.000 claims 1
- 208000035269 cancer or benign tumor Diseases 0.000 claims 1
- 190000008236 carboplatin Chemical compound 0.000 claims 1
- 230000001461 cytolytic effect Effects 0.000 claims 1
- 229940011871 estrogen Drugs 0.000 claims 1
- 239000000262 estrogen Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 208000003849 large cell carcinoma Diseases 0.000 claims 1
- 230000000877 morphologic effect Effects 0.000 claims 1
- 238000011231 neoadjuvant-adjuvant treatment Methods 0.000 claims 1
- 229940075993 receptor modulator Drugs 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 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 claims 1
- 230000001976 improved effect Effects 0.000 abstract description 13
- 238000011275 oncology therapy Methods 0.000 abstract description 10
- 230000001093 anti-cancer Effects 0.000 abstract description 9
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 102000001301 EGF receptor Human genes 0.000 description 228
- 108060006698 EGF receptor Proteins 0.000 description 227
- 125000003275 alpha amino acid group Chemical group 0.000 description 67
- 125000000837 carbohydrate group Chemical group 0.000 description 42
- 239000000203 mixture Substances 0.000 description 30
- 108010047041 Complementarity Determining Regions Proteins 0.000 description 27
- 230000009467 reduction Effects 0.000 description 27
- 230000004044 response Effects 0.000 description 25
- 239000000427 antigen Substances 0.000 description 23
- 108091007433 antigens Proteins 0.000 description 23
- 102000036639 antigens Human genes 0.000 description 23
- WQZGKKKJIJFFOK-PHYPRBDBSA-N alpha-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 description 22
- 230000000875 corresponding effect Effects 0.000 description 22
- 230000014509 gene expression Effects 0.000 description 22
- 235000001014 amino acid Nutrition 0.000 description 21
- 210000004369 blood Anatomy 0.000 description 21
- 239000008280 blood Substances 0.000 description 21
- 230000003902 lesion Effects 0.000 description 19
- 101710113436 GTPase KRas Proteins 0.000 description 18
- 150000001875 compounds Chemical class 0.000 description 18
- 239000012530 fluid Substances 0.000 description 17
- 230000007423 decrease Effects 0.000 description 16
- 238000002560 therapeutic procedure Methods 0.000 description 16
- 230000008901 benefit Effects 0.000 description 15
- 230000004083 survival effect Effects 0.000 description 14
- 238000007901 in situ hybridization Methods 0.000 description 13
- 239000004055 small Interfering RNA Substances 0.000 description 13
- 239000012634 fragment Substances 0.000 description 12
- 210000004881 tumor cell Anatomy 0.000 description 11
- 206010003445 Ascites Diseases 0.000 description 10
- 101150039808 Egfr gene Proteins 0.000 description 10
- 206010051792 Infusion related reaction Diseases 0.000 description 10
- 108020004459 Small interfering RNA Proteins 0.000 description 10
- 210000002966 serum Anatomy 0.000 description 10
- 108010022366 Carcinoembryonic Antigen Proteins 0.000 description 9
- 102100025475 Carcinoembryonic antigen-related cell adhesion molecule 5 Human genes 0.000 description 9
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 9
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 9
- 238000003556 assay Methods 0.000 description 9
- 108700021358 erbB-1 Genes Proteins 0.000 description 9
- 239000011777 magnesium Substances 0.000 description 9
- 229910052749 magnesium Inorganic materials 0.000 description 9
- 108090000623 proteins and genes Proteins 0.000 description 9
- 102000005962 receptors Human genes 0.000 description 9
- 108020003175 receptors Proteins 0.000 description 9
- INZOTETZQBPBCE-NYLDSJSYSA-N 3-sialyl lewis Chemical compound O[C@H]1[C@H](O)[C@H](O)[C@H](C)O[C@H]1O[C@H]([C@H](O)CO)[C@@H]([C@@H](NC(C)=O)C=O)O[C@H]1[C@H](O)[C@@H](O[C@]2(O[C@H]([C@H](NC(C)=O)[C@@H](O)C2)[C@H](O)[C@H](O)CO)C(O)=O)[C@@H](O)[C@@H](CO)O1 INZOTETZQBPBCE-NYLDSJSYSA-N 0.000 description 8
- 229940024606 amino acid Drugs 0.000 description 8
- 230000012010 growth Effects 0.000 description 8
- 230000036541 health Effects 0.000 description 8
- 230000001965 increasing effect Effects 0.000 description 8
- 239000000523 sample Substances 0.000 description 8
- 241000283984 Rodentia Species 0.000 description 7
- 238000002512 chemotherapy Methods 0.000 description 7
- 210000005260 human cell Anatomy 0.000 description 7
- 238000003364 immunohistochemistry Methods 0.000 description 7
- 238000000338 in vitro Methods 0.000 description 7
- 230000005764 inhibitory process Effects 0.000 description 7
- 230000001404 mediated effect Effects 0.000 description 7
- 230000002265 prevention Effects 0.000 description 7
- 229940124597 therapeutic agent Drugs 0.000 description 7
- OVRNDRQMDRJTHS-FMDGEEDCSA-N N-acetyl-beta-D-glucosamine Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-FMDGEEDCSA-N 0.000 description 6
- 208000002151 Pleural effusion Diseases 0.000 description 6
- 206010066901 Treatment failure Diseases 0.000 description 6
- 235000014633 carbohydrates Nutrition 0.000 description 6
- 210000004602 germ cell Anatomy 0.000 description 6
- 208000015181 infectious disease Diseases 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 6
- 230000007246 mechanism Effects 0.000 description 6
- NFGXHKASABOEEW-UHFFFAOYSA-N 1-methylethyl 11-methoxy-3,7,11-trimethyl-2,4-dodecadienoate Chemical compound COC(C)(C)CCCC(C)CC=CC(C)=CC(=O)OC(C)C NFGXHKASABOEEW-UHFFFAOYSA-N 0.000 description 5
- WQZGKKKJIJFFOK-QTVWNMPRSA-N D-mannopyranose Chemical compound OC[C@H]1OC(O)[C@@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-QTVWNMPRSA-N 0.000 description 5
- 102000009109 Fc receptors Human genes 0.000 description 5
- 108010087819 Fc receptors Proteins 0.000 description 5
- 108010073807 IgG Receptors Proteins 0.000 description 5
- 206010069755 K-ras gene mutation Diseases 0.000 description 5
- 102000006747 Transforming Growth Factor alpha Human genes 0.000 description 5
- 101800004564 Transforming growth factor alpha Proteins 0.000 description 5
- 230000000259 anti-tumor effect Effects 0.000 description 5
- 238000009175 antibody therapy Methods 0.000 description 5
- 210000003567 ascitic fluid Anatomy 0.000 description 5
- 210000000601 blood cell Anatomy 0.000 description 5
- 229940088598 enzyme Drugs 0.000 description 5
- 230000006870 function Effects 0.000 description 5
- 230000006872 improvement Effects 0.000 description 5
- 230000004048 modification Effects 0.000 description 5
- 238000012986 modification Methods 0.000 description 5
- 230000011664 signaling Effects 0.000 description 5
- 210000001519 tissue Anatomy 0.000 description 5
- 206010052358 Colorectal cancer metastatic Diseases 0.000 description 4
- 206010063045 Effusion Diseases 0.000 description 4
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 4
- 102000009490 IgG Receptors Human genes 0.000 description 4
- 108010054477 Immunoglobulin Fab Fragments Proteins 0.000 description 4
- 102000001706 Immunoglobulin Fab Fragments Human genes 0.000 description 4
- 206010050513 Metastatic renal cell carcinoma Diseases 0.000 description 4
- 230000004988 N-glycosylation Effects 0.000 description 4
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 4
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 4
- 206010041067 Small cell lung cancer Diseases 0.000 description 4
- 108091027967 Small hairpin RNA Proteins 0.000 description 4
- 230000009471 action Effects 0.000 description 4
- 125000000539 amino acid group Chemical group 0.000 description 4
- 230000000202 analgesic effect Effects 0.000 description 4
- 230000000340 anti-metabolite Effects 0.000 description 4
- 229940100197 antimetabolite Drugs 0.000 description 4
- 239000002256 antimetabolite Substances 0.000 description 4
- 238000013459 approach Methods 0.000 description 4
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 description 4
- 210000004978 chinese hamster ovary cell Anatomy 0.000 description 4
- 238000010494 dissociation reaction Methods 0.000 description 4
- 230000005593 dissociations Effects 0.000 description 4
- 239000012636 effector Substances 0.000 description 4
- 230000009368 gene silencing by RNA Effects 0.000 description 4
- 239000008187 granular material Substances 0.000 description 4
- 238000011534 incubation Methods 0.000 description 4
- 238000002347 injection Methods 0.000 description 4
- 239000007924 injection Substances 0.000 description 4
- 239000003550 marker Substances 0.000 description 4
- 229950006780 n-acetylglucosamine Drugs 0.000 description 4
- 239000011591 potassium Substances 0.000 description 4
- 229910052700 potassium Inorganic materials 0.000 description 4
- 102000004169 proteins and genes Human genes 0.000 description 4
- 238000011160 research Methods 0.000 description 4
- 229960004641 rituximab Drugs 0.000 description 4
- 241000894007 species Species 0.000 description 4
- 230000006641 stabilisation Effects 0.000 description 4
- 238000011105 stabilization Methods 0.000 description 4
- 230000004614 tumor growth Effects 0.000 description 4
- 230000009278 visceral effect Effects 0.000 description 4
- 230000004544 DNA amplification Effects 0.000 description 3
- 201000004624 Dermatitis Diseases 0.000 description 3
- 206010061818 Disease progression Diseases 0.000 description 3
- 108010019236 Fucosyltransferases Proteins 0.000 description 3
- 102000006471 Fucosyltransferases Human genes 0.000 description 3
- 108010062427 GDP-mannose 4,6-dehydratase Proteins 0.000 description 3
- 102000002312 GDPmannose 4,6-dehydratase Human genes 0.000 description 3
- 102000010445 Lactoferrin Human genes 0.000 description 3
- 108010063045 Lactoferrin Proteins 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- SQVRNKJHWKZAKO-PFQGKNLYSA-N N-acetyl-beta-neuraminic acid Chemical compound CC(=O)N[C@@H]1[C@@H](O)C[C@@](O)(C(O)=O)O[C@H]1[C@H](O)[C@H](O)CO SQVRNKJHWKZAKO-PFQGKNLYSA-N 0.000 description 3
- 108091000080 Phosphotransferase Proteins 0.000 description 3
- 206010039491 Sarcoma Diseases 0.000 description 3
- 206010059516 Skin toxicity Diseases 0.000 description 3
- 238000009825 accumulation Methods 0.000 description 3
- 208000026935 allergic disease Diseases 0.000 description 3
- 230000006037 cell lysis Effects 0.000 description 3
- 230000000973 chemotherapeutic effect Effects 0.000 description 3
- 230000000295 complement effect Effects 0.000 description 3
- 231100000433 cytotoxic Toxicity 0.000 description 3
- 239000002254 cytotoxic agent Substances 0.000 description 3
- 230000001472 cytotoxic effect Effects 0.000 description 3
- 230000003247 decreasing effect Effects 0.000 description 3
- 230000005750 disease progression Effects 0.000 description 3
- 229940000406 drug candidate Drugs 0.000 description 3
- 210000000416 exudates and transudate Anatomy 0.000 description 3
- 230000000977 initiatory effect Effects 0.000 description 3
- 230000003834 intracellular effect Effects 0.000 description 3
- 238000010253 intravenous injection Methods 0.000 description 3
- CSSYQJWUGATIHM-IKGCZBKSSA-N l-phenylalanyl-l-lysyl-l-cysteinyl-l-arginyl-l-arginyl-l-tryptophyl-l-glutaminyl-l-tryptophyl-l-arginyl-l-methionyl-l-lysyl-l-lysyl-l-leucylglycyl-l-alanyl-l-prolyl-l-seryl-l-isoleucyl-l-threonyl-l-cysteinyl-l-valyl-l-arginyl-l-arginyl-l-alanyl-l-phenylal Chemical compound C([C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CS)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)C1=CC=CC=C1 CSSYQJWUGATIHM-IKGCZBKSSA-N 0.000 description 3
- 229940078795 lactoferrin Drugs 0.000 description 3
- 235000021242 lactoferrin Nutrition 0.000 description 3
- 230000000670 limiting effect Effects 0.000 description 3
- 210000004185 liver Anatomy 0.000 description 3
- 238000011866 long-term treatment Methods 0.000 description 3
- 210000004379 membrane Anatomy 0.000 description 3
- 239000012528 membrane Substances 0.000 description 3
- 230000017074 necrotic cell death Effects 0.000 description 3
- 238000009116 palliative therapy Methods 0.000 description 3
- 102000020233 phosphotransferase Human genes 0.000 description 3
- 238000010837 poor prognosis Methods 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 235000018102 proteins Nutrition 0.000 description 3
- -1 radioisotopes Substances 0.000 description 3
- 239000003642 reactive oxygen metabolite Substances 0.000 description 3
- 238000002271 resection Methods 0.000 description 3
- 230000019491 signal transduction Effects 0.000 description 3
- 229910052709 silver Inorganic materials 0.000 description 3
- 239000004332 silver Substances 0.000 description 3
- 231100000438 skin toxicity Toxicity 0.000 description 3
- 230000000638 stimulation Effects 0.000 description 3
- 210000000115 thoracic cavity Anatomy 0.000 description 3
- 229960005267 tositumomab Drugs 0.000 description 3
- 239000000439 tumor marker Substances 0.000 description 3
- VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 description 3
- NMWKYTGJWUAZPZ-WWHBDHEGSA-N (4S)-4-[[(4R,7S,10S,16S,19S,25S,28S,31R)-31-[[(2S)-2-[[(1R,6R,9S,12S,18S,21S,24S,27S,30S,33S,36S,39S,42R,47R,53S,56S,59S,62S,65S,68S,71S,76S,79S,85S)-47-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-oxobutanoyl]amino]-3-carboxypropanoyl]amino]-18-(4-aminobutyl)-27,68-bis(3-amino-3-oxopropyl)-36,71,76-tribenzyl-39-(3-carbamimidamidopropyl)-24-(2-carboxyethyl)-21,56-bis(carboxymethyl)-65,85-bis[(1R)-1-hydroxyethyl]-59-(hydroxymethyl)-62,79-bis(1H-imidazol-4-ylmethyl)-9-methyl-33-(2-methylpropyl)-8,11,17,20,23,26,29,32,35,38,41,48,54,57,60,63,66,69,72,74,77,80,83,86-tetracosaoxo-30-propan-2-yl-3,4,44,45-tetrathia-7,10,16,19,22,25,28,31,34,37,40,49,55,58,61,64,67,70,73,75,78,81,84,87-tetracosazatetracyclo[40.31.14.012,16.049,53]heptaoctacontane-6-carbonyl]amino]-3-methylbutanoyl]amino]-7-(3-carbamimidamidopropyl)-25-(hydroxymethyl)-19-[(4-hydroxyphenyl)methyl]-28-(1H-imidazol-4-ylmethyl)-10-methyl-6,9,12,15,18,21,24,27,30-nonaoxo-16-propan-2-yl-1,2-dithia-5,8,11,14,17,20,23,26,29-nonazacyclodotriacontane-4-carbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-3-carboxy-1-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid Chemical compound CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc4c[nH]cn4)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H]4CCCN4C(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc4c[nH]cn4)NC(=O)[C@H](Cc4ccccc4)NC3=O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)C(C)C)[C@@H](C)O)C(C)C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1)C(=O)N[C@@H](C)C(O)=O NMWKYTGJWUAZPZ-WWHBDHEGSA-N 0.000 description 2
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 2
- RTQWWZBSTRGEAV-PKHIMPSTSA-N 2-[[(2s)-2-[bis(carboxymethyl)amino]-3-[4-(methylcarbamoylamino)phenyl]propyl]-[2-[bis(carboxymethyl)amino]propyl]amino]acetic acid Chemical compound CNC(=O)NC1=CC=C(C[C@@H](CN(CC(C)N(CC(O)=O)CC(O)=O)CC(O)=O)N(CC(O)=O)CC(O)=O)C=C1 RTQWWZBSTRGEAV-PKHIMPSTSA-N 0.000 description 2
- 206010069754 Acquired gene mutation Diseases 0.000 description 2
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 description 2
- 208000003174 Brain Neoplasms Diseases 0.000 description 2
- 102000019034 Chemokines Human genes 0.000 description 2
- 108010012236 Chemokines Proteins 0.000 description 2
- 208000003322 Coinfection Diseases 0.000 description 2
- 238000002965 ELISA Methods 0.000 description 2
- 206010015218 Erythema multiforme Diseases 0.000 description 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 2
- 108700023372 Glycosyltransferases Proteins 0.000 description 2
- 102000051366 Glycosyltransferases Human genes 0.000 description 2
- 101000819490 Homo sapiens Alpha-(1,6)-fucosyltransferase Proteins 0.000 description 2
- 101000851181 Homo sapiens Epidermal growth factor receptor Proteins 0.000 description 2
- 101001010819 Homo sapiens Receptor tyrosine-protein kinase erbB-3 Proteins 0.000 description 2
- 101001010823 Homo sapiens Receptor tyrosine-protein kinase erbB-4 Proteins 0.000 description 2
- 108010001336 Horseradish Peroxidase Proteins 0.000 description 2
- 208000022120 Jeavons syndrome Diseases 0.000 description 2
- 208000007433 Lymphatic Metastasis Diseases 0.000 description 2
- 229930126263 Maytansine Natural products 0.000 description 2
- 206010027458 Metastases to lung Diseases 0.000 description 2
- 206010051676 Metastases to peritoneum Diseases 0.000 description 2
- 206010027463 Metastases to pleura Diseases 0.000 description 2
- 206010063569 Metastatic squamous cell carcinoma Diseases 0.000 description 2
- 108700011259 MicroRNAs Proteins 0.000 description 2
- 229930012538 Paclitaxel Natural products 0.000 description 2
- 108090000526 Papain Proteins 0.000 description 2
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 2
- 239000004365 Protease Substances 0.000 description 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 2
- 238000012228 RNA interference-mediated gene silencing Methods 0.000 description 2
- 108091030071 RNAI Proteins 0.000 description 2
- 206010040047 Sepsis Diseases 0.000 description 2
- 210000001015 abdomen Anatomy 0.000 description 2
- 210000000683 abdominal cavity Anatomy 0.000 description 2
- 229960000548 alemtuzumab Drugs 0.000 description 2
- 229940100198 alkylating agent Drugs 0.000 description 2
- 239000002168 alkylating agent Substances 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- DKVSUQWCZQBWCP-QAGGRKNESA-N androsta-1,4,6-triene-3,17-dione Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3C=CC2=C1 DKVSUQWCZQBWCP-QAGGRKNESA-N 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 125000000613 asparagine group Chemical group N[C@@H](CC(N)=O)C(=O)* 0.000 description 2
- 229940120638 avastin Drugs 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 238000001815 biotherapy Methods 0.000 description 2
- 201000010983 breast ductal carcinoma Diseases 0.000 description 2
- 238000009566 cancer vaccine Methods 0.000 description 2
- 229940022399 cancer vaccine Drugs 0.000 description 2
- 230000021164 cell adhesion Effects 0.000 description 2
- 230000030833 cell death Effects 0.000 description 2
- 210000000038 chest Anatomy 0.000 description 2
- 201000010276 collecting duct carcinoma Diseases 0.000 description 2
- 238000011284 combination treatment Methods 0.000 description 2
- 230000002596 correlated effect Effects 0.000 description 2
- 239000000824 cytostatic agent Substances 0.000 description 2
- 230000002950 deficient Effects 0.000 description 2
- 238000001514 detection method Methods 0.000 description 2
- 208000024334 diffuse gastric cancer Diseases 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 239000012893 effector ligand Substances 0.000 description 2
- 238000011984 electrochemiluminescence immunoassay Methods 0.000 description 2
- 210000003238 esophagus Anatomy 0.000 description 2
- 238000001943 fluorescence-activated cell sorting Methods 0.000 description 2
- 101150023212 fut8 gene Proteins 0.000 description 2
- 230000003862 health status Effects 0.000 description 2
- 238000005734 heterodimerization reaction Methods 0.000 description 2
- 102000057750 human ERBB3 Human genes 0.000 description 2
- 102000053810 human ERBB4 Human genes 0.000 description 2
- 229960001001 ibritumomab tiuxetan Drugs 0.000 description 2
- 230000005847 immunogenicity Effects 0.000 description 2
- 238000009169 immunotherapy Methods 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 230000007803 itching Effects 0.000 description 2
- 231100000518 lethal Toxicity 0.000 description 2
- 230000001665 lethal effect Effects 0.000 description 2
- 238000012153 long-term therapy Methods 0.000 description 2
- 125000000311 mannosyl group Chemical group C1([C@@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 2
- WKPWGQKGSOKKOO-RSFHAFMBSA-N maytansine Chemical compound CO[C@@H]([C@@]1(O)C[C@](OC(=O)N1)([C@H]([C@@H]1O[C@@]1(C)[C@@H](OC(=O)[C@H](C)N(C)C(C)=O)CC(=O)N1C)C)[H])\C=C\C=C(C)\CC2=CC(OC)=C(Cl)C1=C2 WKPWGQKGSOKKOO-RSFHAFMBSA-N 0.000 description 2
- 230000010534 mechanism of action Effects 0.000 description 2
- 230000002503 metabolic effect Effects 0.000 description 2
- 239000002679 microRNA Substances 0.000 description 2
- 208000025113 myeloid leukemia Diseases 0.000 description 2
- 208000026721 nail disease Diseases 0.000 description 2
- 210000005036 nerve Anatomy 0.000 description 2
- 210000004882 non-tumor cell Anatomy 0.000 description 2
- 238000005457 optimization Methods 0.000 description 2
- 230000002018 overexpression Effects 0.000 description 2
- 229940055729 papain Drugs 0.000 description 2
- 235000019834 papain Nutrition 0.000 description 2
- 229960005489 paracetamol Drugs 0.000 description 2
- 210000003819 peripheral blood mononuclear cell Anatomy 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 238000009520 phase I clinical trial Methods 0.000 description 2
- 238000009521 phase II clinical trial Methods 0.000 description 2
- 229920001184 polypeptide Polymers 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 102000004196 processed proteins & peptides Human genes 0.000 description 2
- 108090000765 processed proteins & peptides Proteins 0.000 description 2
- 238000012545 processing Methods 0.000 description 2
- 102000003998 progesterone receptors Human genes 0.000 description 2
- 108090000468 progesterone receptors Proteins 0.000 description 2
- 230000005855 radiation Effects 0.000 description 2
- 102000027426 receptor tyrosine kinases Human genes 0.000 description 2
- 108091008598 receptor tyrosine kinases Proteins 0.000 description 2
- 238000003259 recombinant expression Methods 0.000 description 2
- 238000005549 size reduction Methods 0.000 description 2
- 208000000587 small cell lung carcinoma Diseases 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 230000037439 somatic mutation Effects 0.000 description 2
- 230000009870 specific binding Effects 0.000 description 2
- 238000010186 staining Methods 0.000 description 2
- 238000011301 standard therapy Methods 0.000 description 2
- 230000003319 supportive effect Effects 0.000 description 2
- 206010044412 transitional cell carcinoma Diseases 0.000 description 2
- 210000001835 viscera Anatomy 0.000 description 2
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 description 1
- 102000040650 (ribonucleotides)n+m Human genes 0.000 description 1
- CDAWCLOXVUBKRW-UHFFFAOYSA-N 2-aminophenol Chemical class NC1=CC=CC=C1O CDAWCLOXVUBKRW-UHFFFAOYSA-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
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 description 1
- 102100021266 Alpha-(1,6)-fucosyltransferase Human genes 0.000 description 1
- 102000015404 Amino Acid Receptors Human genes 0.000 description 1
- 108010025177 Amino Acid Receptors Proteins 0.000 description 1
- 206010002199 Anaphylactic shock Diseases 0.000 description 1
- 101100067974 Arabidopsis thaliana POP2 gene Proteins 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 208000006478 Cecal Neoplasms Diseases 0.000 description 1
- 102000016289 Cell Adhesion Molecules Human genes 0.000 description 1
- 108010067225 Cell Adhesion Molecules Proteins 0.000 description 1
- 206010008479 Chest Pain Diseases 0.000 description 1
- 206010055114 Colon cancer metastatic Diseases 0.000 description 1
- 108091035707 Consensus sequence Proteins 0.000 description 1
- 206010010774 Constipation Diseases 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 229940122204 Cyclooxygenase inhibitor Drugs 0.000 description 1
- 206010012456 Dermatitis exfoliative generalised Diseases 0.000 description 1
- 238000009007 Diagnostic Kit Methods 0.000 description 1
- 208000000059 Dyspnea Diseases 0.000 description 1
- 206010013975 Dyspnoeas Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 102100023387 Endoribonuclease Dicer Human genes 0.000 description 1
- 101800003838 Epidermal growth factor Proteins 0.000 description 1
- 102400001368 Epidermal growth factor Human genes 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
- 108010021468 Fc gamma receptor IIA Proteins 0.000 description 1
- 108010021472 Fc gamma receptor IIB Proteins 0.000 description 1
- 241000233866 Fungi Species 0.000 description 1
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 description 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 description 1
- 102000003886 Glycoproteins Human genes 0.000 description 1
- 108090000288 Glycoproteins Proteins 0.000 description 1
- 102000001398 Granzyme Human genes 0.000 description 1
- 108060005986 Granzyme Proteins 0.000 description 1
- 229940122957 Histamine H2 receptor antagonist Drugs 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 101100118549 Homo sapiens EGFR gene Proteins 0.000 description 1
- 101000917839 Homo sapiens Low affinity immunoglobulin gamma Fc region receptor III-B Proteins 0.000 description 1
- 101000581981 Homo sapiens Neural cell adhesion molecule 1 Proteins 0.000 description 1
- 208000001953 Hypotension Diseases 0.000 description 1
- 102100026120 IgG receptor FcRn large subunit p51 Human genes 0.000 description 1
- 101710177940 IgG receptor FcRn large subunit p51 Proteins 0.000 description 1
- 108060003951 Immunoglobulin Proteins 0.000 description 1
- 108010067060 Immunoglobulin Variable Region Proteins 0.000 description 1
- 102000017727 Immunoglobulin Variable Region Human genes 0.000 description 1
- 238000012404 In vitro experiment Methods 0.000 description 1
- 208000020060 Increased inflammatory response Diseases 0.000 description 1
- 125000002842 L-seryl group Chemical group O=C([*])[C@](N([H])[H])([H])C([H])([H])O[H] 0.000 description 1
- 125000000769 L-threonyl group Chemical group [H]N([H])[C@]([H])(C(=O)[*])[C@](O[H])(C([H])([H])[H])[H] 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
- 239000005517 L01XE01 - Imatinib Substances 0.000 description 1
- 239000003798 L01XE11 - Pazopanib Substances 0.000 description 1
- 102100029204 Low affinity immunoglobulin gamma Fc region receptor II-a Human genes 0.000 description 1
- 102100029205 Low affinity immunoglobulin gamma Fc region receptor II-b Human genes 0.000 description 1
- 206010026673 Malignant Pleural Effusion Diseases 0.000 description 1
- 206010027452 Metastases to bone Diseases 0.000 description 1
- 206010059282 Metastases to central nervous system Diseases 0.000 description 1
- 206010027457 Metastases to liver Diseases 0.000 description 1
- 206010027459 Metastases to lymph nodes Diseases 0.000 description 1
- 206010027465 Metastases to skin Diseases 0.000 description 1
- 206010063916 Metastatic gastric cancer Diseases 0.000 description 1
- 241001529936 Murinae Species 0.000 description 1
- SUHQNCLNRUAGOO-UHFFFAOYSA-N N-glycoloyl-neuraminic acid Natural products OCC(O)C(O)C(O)C(NC(=O)CO)C(O)CC(=O)C(O)=O SUHQNCLNRUAGOO-UHFFFAOYSA-N 0.000 description 1
- FDJKUWYYUZCUJX-UHFFFAOYSA-N N-glycolyl-beta-neuraminic acid Natural products OCC(O)C(O)C1OC(O)(C(O)=O)CC(O)C1NC(=O)CO FDJKUWYYUZCUJX-UHFFFAOYSA-N 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 206010028885 Necrotising fasciitis Diseases 0.000 description 1
- 206010061309 Neoplasm progression Diseases 0.000 description 1
- 208000028389 Nerve injury Diseases 0.000 description 1
- 102100027347 Neural cell adhesion molecule 1 Human genes 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 238000010222 PCR analysis Methods 0.000 description 1
- KHGNFPUMBJSZSM-UHFFFAOYSA-N Perforine Natural products COC1=C2CCC(O)C(CCC(C)(C)O)(OC)C2=NC2=C1C=CO2 KHGNFPUMBJSZSM-UHFFFAOYSA-N 0.000 description 1
- 206010054827 Peritoneal lesion Diseases 0.000 description 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- 101150040459 RAS gene Proteins 0.000 description 1
- 208000001647 Renal Insufficiency Diseases 0.000 description 1
- 208000008938 Rhabdoid tumor Diseases 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- 101100123851 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) HER1 gene Proteins 0.000 description 1
- 238000012300 Sequence Analysis Methods 0.000 description 1
- 206010040893 Skin necrosis Diseases 0.000 description 1
- 238000002105 Southern blotting Methods 0.000 description 1
- 206010042674 Swelling Diseases 0.000 description 1
- 208000024770 Thyroid neoplasm Diseases 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 229940122803 Vinca alkaloid Drugs 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 206010000269 abscess Diseases 0.000 description 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 description 1
- 150000008061 acetanilides Chemical class 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000006978 adaptation Effects 0.000 description 1
- 238000011374 additional therapy Methods 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 208000037842 advanced-stage tumor Diseases 0.000 description 1
- 229930013930 alkaloid Natural products 0.000 description 1
- 230000000172 allergic effect Effects 0.000 description 1
- 102000012086 alpha-L-Fucosidase Human genes 0.000 description 1
- 108010061314 alpha-L-Fucosidase Proteins 0.000 description 1
- 230000003321 amplification Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- 150000001448 anilines Chemical class 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000003266 anti-allergic effect Effects 0.000 description 1
- 229940124650 anti-cancer therapies Drugs 0.000 description 1
- 230000002001 anti-metastasis Effects 0.000 description 1
- 230000000692 anti-sense effect Effects 0.000 description 1
- 238000011230 antibody-based therapy Methods 0.000 description 1
- 238000011319 anticancer therapy Methods 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 229940034982 antineoplastic agent Drugs 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 230000035578 autophosphorylation Effects 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 230000003796 beauty Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 238000001574 biopsy Methods 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 210000000746 body region Anatomy 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000006172 buffering agent Substances 0.000 description 1
- 229940112129 campath Drugs 0.000 description 1
- 230000005907 cancer growth Effects 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 201000003959 cecum carcinoma Diseases 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 230000012292 cell migration Effects 0.000 description 1
- 210000003855 cell nucleus Anatomy 0.000 description 1
- 230000005889 cellular cytotoxicity Effects 0.000 description 1
- 238000012412 chemical coupling Methods 0.000 description 1
- 239000007795 chemical reaction product Substances 0.000 description 1
- 210000000349 chromosome Anatomy 0.000 description 1
- 208000009060 clear cell adenocarcinoma Diseases 0.000 description 1
- 238000011278 co-treatment Methods 0.000 description 1
- 201000003970 colon lymphoma Diseases 0.000 description 1
- 230000004154 complement system Effects 0.000 description 1
- 239000000306 component Substances 0.000 description 1
- 238000002591 computed tomography Methods 0.000 description 1
- 238000012790 confirmation Methods 0.000 description 1
- 230000002920 convulsive effect Effects 0.000 description 1
- 230000009260 cross reactivity Effects 0.000 description 1
- 230000002380 cytological effect Effects 0.000 description 1
- 231100000599 cytotoxic agent Toxicity 0.000 description 1
- 229960003901 dacarbazine Drugs 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 230000003831 deregulation Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 238000002405 diagnostic procedure Methods 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 229910003460 diamond Inorganic materials 0.000 description 1
- 239000010432 diamond Substances 0.000 description 1
- CEJLBZWIKQJOAT-UHFFFAOYSA-N dichloroisocyanuric acid Chemical compound ClN1C(=O)NC(=O)N(Cl)C1=O CEJLBZWIKQJOAT-UHFFFAOYSA-N 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 239000000539 dimer Substances 0.000 description 1
- 230000007783 downstream signaling Effects 0.000 description 1
- 229940126534 drug product Drugs 0.000 description 1
- 235000006694 eating habits Nutrition 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 238000004836 empirical method Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 230000002357 endometrial effect Effects 0.000 description 1
- 238000001839 endoscopy Methods 0.000 description 1
- 238000009585 enzyme analysis Methods 0.000 description 1
- 229940116977 epidermal growth factor Drugs 0.000 description 1
- 229960001904 epirubicin Drugs 0.000 description 1
- 210000003236 esophagogastric junction Anatomy 0.000 description 1
- 239000002834 estrogen receptor modulator Substances 0.000 description 1
- 229960005420 etoposide Drugs 0.000 description 1
- 230000005713 exacerbation Effects 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 238000009093 first-line therapy Methods 0.000 description 1
- 229940014144 folate Drugs 0.000 description 1
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 description 1
- 235000019152 folic acid Nutrition 0.000 description 1
- 239000011724 folic acid Substances 0.000 description 1
- 239000010200 folin Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 229960000578 gemtuzumab Drugs 0.000 description 1
- 238000003197 gene knockdown Methods 0.000 description 1
- 238000003209 gene knockout Methods 0.000 description 1
- 101150106565 gmd gene Proteins 0.000 description 1
- 230000007407 health benefit Effects 0.000 description 1
- 230000005802 health problem Effects 0.000 description 1
- 239000000833 heterodimer Substances 0.000 description 1
- 239000000710 homodimer Substances 0.000 description 1
- 238000009396 hybridization Methods 0.000 description 1
- 230000036543 hypotension Effects 0.000 description 1
- 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 description 1
- 229960002411 imatinib Drugs 0.000 description 1
- 230000001900 immune effect Effects 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 102000018358 immunoglobulin Human genes 0.000 description 1
- 230000002055 immunohistochemical effect Effects 0.000 description 1
- 238000011532 immunohistochemical staining Methods 0.000 description 1
- 239000002955 immunomodulating agent Substances 0.000 description 1
- 238000000099 in vitro assay Methods 0.000 description 1
- 230000002458 infectious effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 201000002313 intestinal cancer Diseases 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 230000005865 ionizing radiation Effects 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 201000006370 kidney failure Diseases 0.000 description 1
- 230000002147 killing effect Effects 0.000 description 1
- 210000002429 large intestine Anatomy 0.000 description 1
- 210000000265 leukocyte Anatomy 0.000 description 1
- 238000000670 ligand binding assay Methods 0.000 description 1
- 108020001756 ligand binding domains Proteins 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 201000005249 lung adenocarcinoma Diseases 0.000 description 1
- 210000001365 lymphatic vessel Anatomy 0.000 description 1
- 239000008176 lyophilized powder Substances 0.000 description 1
- 238000002595 magnetic resonance imaging Methods 0.000 description 1
- 230000036210 malignancy Effects 0.000 description 1
- 210000004962 mammalian cell Anatomy 0.000 description 1
- 238000009607 mammography Methods 0.000 description 1
- 229940127554 medical product Drugs 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 230000005012 migration Effects 0.000 description 1
- 238000013508 migration Methods 0.000 description 1
- 231100001067 mild skin irritation Toxicity 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 238000002703 mutagenesis Methods 0.000 description 1
- 231100000350 mutagenesis Toxicity 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 201000007970 necrotizing fasciitis Diseases 0.000 description 1
- 230000008764 nerve damage Effects 0.000 description 1
- 208000004296 neuralgia Diseases 0.000 description 1
- 208000021722 neuropathic pain Diseases 0.000 description 1
- 229940121367 non-opioid analgesics Drugs 0.000 description 1
- 238000003199 nucleic acid amplification method Methods 0.000 description 1
- 102000039446 nucleic acids Human genes 0.000 description 1
- 108020004707 nucleic acids Proteins 0.000 description 1
- 150000007523 nucleic acids Chemical class 0.000 description 1
- 239000002773 nucleotide Chemical group 0.000 description 1
- 125000003729 nucleotide group Chemical group 0.000 description 1
- 229940127084 other anti-cancer agent Drugs 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 229960000639 pazopanib Drugs 0.000 description 1
- 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 description 1
- 229930192851 perforin Natural products 0.000 description 1
- 238000012831 peritoneal equilibrium test Methods 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 229940124531 pharmaceutical excipient Drugs 0.000 description 1
- 230000005195 poor health Effects 0.000 description 1
- 238000012636 positron electron tomography Methods 0.000 description 1
- 238000012877 positron emission topography Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000007425 progressive decline Effects 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 239000002089 prostaglandin antagonist Substances 0.000 description 1
- 239000002599 prostaglandin synthase inhibitor Substances 0.000 description 1
- 238000000159 protein binding assay Methods 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 108700042226 ras Genes Proteins 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000009877 rendering Methods 0.000 description 1
- 108091008146 restriction endonucleases Proteins 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 210000000614 rib Anatomy 0.000 description 1
- 102200006532 rs112445441 Human genes 0.000 description 1
- 102220053950 rs121913238 Human genes 0.000 description 1
- 102200006520 rs121913240 Human genes 0.000 description 1
- 102200006531 rs121913529 Human genes 0.000 description 1
- 102200006537 rs121913529 Human genes 0.000 description 1
- 102200006539 rs121913529 Human genes 0.000 description 1
- 102200006538 rs121913530 Human genes 0.000 description 1
- 102200006540 rs121913530 Human genes 0.000 description 1
- 102200006541 rs121913530 Human genes 0.000 description 1
- 102200006533 rs121913535 Human genes 0.000 description 1
- 102200007373 rs17851045 Human genes 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 238000002741 site-directed mutagenesis Methods 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 238000011272 standard treatment Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 150000004579 taxol derivatives Chemical class 0.000 description 1
- 150000003505 terpenes Chemical class 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 239000008181 tonicity modifier Substances 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 238000003151 transfection method Methods 0.000 description 1
- 230000032258 transport Effects 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 230000005751 tumor progression Effects 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
- 238000002604 ultrasonography Methods 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 125000002987 valine group Chemical group [H]N([H])C([H])(C(*)=O)C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
- 238000012800 visualization Methods 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000001262 western blot Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/40—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6871—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting an enzyme
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/545—Medicinal preparations containing antigens or antibodies characterised by the dose, timing or administration schedule
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/55—Medicinal preparations containing antigens or antibodies characterised by the host/recipient, e.g. newborn with maternal antibodies
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/40—Immunoglobulins specific features characterized by post-translational modification
- C07K2317/41—Glycosylation, sialylation, or fucosylation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
- C07K2317/73—Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- C07K2317/732—Antibody-dependent cellular cytotoxicity [ADCC]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
- C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Radiology & Medical Imaging (AREA)
- Pathology (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13002106.6 | 2013-04-22 | ||
| EP13002106 | 2013-04-22 | ||
| EP13002108.2 | 2013-04-22 | ||
| EP13002108 | 2013-04-22 | ||
| PCT/EP2014/058118 WO2014173886A1 (en) | 2013-04-22 | 2014-04-22 | Anti-cancer treatments with anti-egfr antibodies having a low fucosylation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016516800A true JP2016516800A (ja) | 2016-06-09 |
| JP2016516800A5 JP2016516800A5 (enExample) | 2017-05-25 |
Family
ID=50729450
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016508192A Withdrawn JP2016516800A (ja) | 2013-04-22 | 2014-04-22 | フコシル化が少ない抗egfr抗体による抗がん処置 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20160068609A1 (enExample) |
| EP (1) | EP2989126A1 (enExample) |
| JP (1) | JP2016516800A (enExample) |
| KR (1) | KR20150144804A (enExample) |
| CN (1) | CN105229030A (enExample) |
| AU (1) | AU2014257650A1 (enExample) |
| BR (1) | BR112015025955A2 (enExample) |
| CA (1) | CA2908819A1 (enExample) |
| EA (1) | EA201591977A1 (enExample) |
| MX (1) | MX2015014773A (enExample) |
| SG (1) | SG11201507743XA (enExample) |
| WO (1) | WO2014173886A1 (enExample) |
| ZA (1) | ZA201507246B (enExample) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020100969A1 (ja) * | 2018-11-14 | 2020-05-22 | 学校法人金沢医科大学 | びまん性胃がんを治療するための医薬組成物 |
| JP2020516300A (ja) * | 2017-04-13 | 2020-06-11 | アデュロ・バイオテック・ホールディングス・ヨーロッパ・ベスローテン・フエンノートシャップAduro Biotech Holdings, Europe B.V. | 抗sirpアルファ抗体 |
| JP2020521780A (ja) * | 2017-05-29 | 2020-07-27 | ガママブス ファルマ | 癌関連免疫抑制阻害剤 |
| JP2023523006A (ja) * | 2020-04-24 | 2023-06-01 | メルス ナムローゼ フェンノートシャップ | Lgr5及びegfrに結合する抗体によるがんの治療 |
| JP2024537357A (ja) * | 2021-10-12 | 2024-10-10 | センター フォー エクセレンス イン モレキュラー セル サイエンス,チャイニーズ アカデミー オブ サイエンシーズ | 呼吸器合胞体ウイルスを中和する全ヒト抗体の設計および使用 |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10478498B2 (en) | 2014-06-20 | 2019-11-19 | Reform Biologics, Llc | Excipient compounds for biopolymer formulations |
| CN105820248A (zh) * | 2015-01-07 | 2016-08-03 | 上海张江生物技术有限公司 | 一种新型抗egfr单克隆抗体的制备方法及应用 |
| CN105399830B (zh) * | 2015-09-08 | 2019-11-19 | 北京天广实生物技术股份有限公司 | 抗egfr人源化单克隆抗体、其制备方法及用途 |
| US20170247458A1 (en) * | 2016-01-10 | 2017-08-31 | Sorrento Therapeutics, Inc. | Safety for Treating Cancers with a Glycosylated Chimeric Antibody to EGFR |
| HUE058745T2 (hu) * | 2016-04-27 | 2022-09-28 | Green Cross Corp | Hatóanyagként epidermális növekedési faktor receptorhoz specifikusan kötõdõ antitestet tartalmazó gyógyászati készítmény rák áttételének gátlására |
| WO2017205465A2 (en) * | 2016-05-24 | 2017-11-30 | Griswold Karl Edwin | Antibodies and methods of making same |
| WO2018013673A1 (en) * | 2016-07-13 | 2018-01-18 | Reform Biologics, Llc | Stabilizing excipients for therapeutic protein formulations |
| KR101884614B1 (ko) | 2016-10-11 | 2018-08-02 | 신일제약주식회사 | Fab 단편 및 이의 용도 |
| WO2018178122A1 (en) * | 2017-03-29 | 2018-10-04 | Glycotope Gmbh | Pd-l1 and ta-muc1 antibodies |
| US20210269530A1 (en) * | 2018-05-14 | 2021-09-02 | Harpoon Therapeutics, Inc. | Conditionally activated binding protein comprising a sterically occluded target binding domain |
| US12195544B2 (en) | 2018-09-21 | 2025-01-14 | Harpoon Therapeutics, Inc. | EGFR binding proteins and methods of use |
| CN112300278A (zh) * | 2019-07-25 | 2021-02-02 | 上海交通大学 | 抗人egfr嵌合抗体及其制备方法和用途 |
| WO2023154796A2 (en) * | 2022-02-09 | 2023-08-17 | Dragonfly Therapeutics, Inc. | Pharmaceutical formulations and therapeutic uses of multi-specific binding proteins that bind egfr, nkg2d, and cd16 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0104865A3 (en) | 1999-01-15 | 2004-07-28 | Genentech Inc | Polypeptide variants with altered effector function |
| DK2270147T4 (da) | 1999-04-09 | 2020-08-31 | Kyowa Kirin Co Ltd | Fremgangsmåde til at kontrollere aktiviteten af immunologisk funktionelt molekyle |
| ATE309385T1 (de) | 2000-06-28 | 2005-11-15 | Glycofi Inc | Verfahren für die herstellung modifizierter glykoproteine |
| WO2003035835A2 (en) | 2001-10-25 | 2003-05-01 | Genentech, Inc. | Glycoprotein compositions |
| EP1500400A4 (en) | 2002-04-09 | 2006-10-11 | Kyowa Hakko Kogyo Kk | MEDICAMENT CONTAINING ANTIBODY COMPOSITION |
| FR2858235B1 (fr) | 2003-07-31 | 2006-02-17 | Lab Francais Du Fractionnement | Utilisation d'anticorps optimises en adcc pour traiter les patients faibles repondeurs |
| EP1871805B1 (en) * | 2005-02-07 | 2019-09-25 | Roche Glycart AG | Antigen binding molecules that bind egfr, vectors encoding same, and uses thereof |
| KR101603632B1 (ko) | 2006-09-10 | 2016-03-16 | 글리코토페 게엠베하 | 항체 발현을 위한 골수성 백혈병 기원의 인간 세포의 용도 |
| WO2011101328A2 (en) * | 2010-02-18 | 2011-08-25 | Roche Glycart Ag | Treatment with a humanized igg class anti egfr antibody and an antibody against insulin like growth factor 1 receptor |
| CN103025760A (zh) * | 2010-08-10 | 2013-04-03 | 葛莱高托普有限公司 | 人源化egfr抗体 |
| EP2603528B1 (en) * | 2010-08-10 | 2016-10-12 | Glycotope GmbH | Fab-glycosylated antibodies |
-
2014
- 2014-04-22 JP JP2016508192A patent/JP2016516800A/ja not_active Withdrawn
- 2014-04-22 EA EA201591977A patent/EA201591977A1/ru unknown
- 2014-04-22 EP EP14724007.1A patent/EP2989126A1/en not_active Withdrawn
- 2014-04-22 BR BR112015025955A patent/BR112015025955A2/pt not_active IP Right Cessation
- 2014-04-22 CA CA2908819A patent/CA2908819A1/en not_active Abandoned
- 2014-04-22 AU AU2014257650A patent/AU2014257650A1/en not_active Abandoned
- 2014-04-22 KR KR1020157033309A patent/KR20150144804A/ko not_active Withdrawn
- 2014-04-22 SG SG11201507743XA patent/SG11201507743XA/en unknown
- 2014-04-22 MX MX2015014773A patent/MX2015014773A/es unknown
- 2014-04-22 WO PCT/EP2014/058118 patent/WO2014173886A1/en not_active Ceased
- 2014-04-22 US US14/784,470 patent/US20160068609A1/en not_active Abandoned
- 2014-04-22 CN CN201480021328.XA patent/CN105229030A/zh active Pending
-
2015
- 2015-09-30 ZA ZA2015/07246A patent/ZA201507246B/en unknown
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020516300A (ja) * | 2017-04-13 | 2020-06-11 | アデュロ・バイオテック・ホールディングス・ヨーロッパ・ベスローテン・フエンノートシャップAduro Biotech Holdings, Europe B.V. | 抗sirpアルファ抗体 |
| JP7160833B2 (ja) | 2017-04-13 | 2022-10-25 | サイロパ ビー.ブイ. | 抗sirpアルファ抗体 |
| JP2020521780A (ja) * | 2017-05-29 | 2020-07-27 | ガママブス ファルマ | 癌関連免疫抑制阻害剤 |
| JP2023073965A (ja) * | 2017-05-29 | 2023-05-26 | ガママブス ファルマ | 癌関連免疫抑制阻害剤 |
| JP7678493B2 (ja) | 2017-05-29 | 2025-05-16 | エクセリクシス, インク. | 癌関連免疫抑制阻害剤 |
| WO2020100969A1 (ja) * | 2018-11-14 | 2020-05-22 | 学校法人金沢医科大学 | びまん性胃がんを治療するための医薬組成物 |
| JPWO2020100969A1 (ja) * | 2018-11-14 | 2021-12-02 | 学校法人金沢医科大学 | びまん性胃がんを治療するための医薬組成物 |
| JP7493237B2 (ja) | 2018-11-14 | 2024-05-31 | 学校法人金沢医科大学 | びまん性胃がんを治療するための医薬組成物 |
| JP2023523006A (ja) * | 2020-04-24 | 2023-06-01 | メルス ナムローゼ フェンノートシャップ | Lgr5及びegfrに結合する抗体によるがんの治療 |
| JP2024537357A (ja) * | 2021-10-12 | 2024-10-10 | センター フォー エクセレンス イン モレキュラー セル サイエンス,チャイニーズ アカデミー オブ サイエンシーズ | 呼吸器合胞体ウイルスを中和する全ヒト抗体の設計および使用 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2989126A1 (en) | 2016-03-02 |
| ZA201507246B (en) | 2016-12-21 |
| US20160068609A1 (en) | 2016-03-10 |
| WO2014173886A1 (en) | 2014-10-30 |
| EA201591977A1 (ru) | 2016-06-30 |
| SG11201507743XA (en) | 2015-11-27 |
| KR20150144804A (ko) | 2015-12-28 |
| BR112015025955A2 (pt) | 2017-10-17 |
| CA2908819A1 (en) | 2014-10-30 |
| AU2014257650A1 (en) | 2015-11-12 |
| MX2015014773A (es) | 2016-03-04 |
| CN105229030A (zh) | 2016-01-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016516800A (ja) | フコシル化が少ない抗egfr抗体による抗がん処置 | |
| JP7494245B2 (ja) | Cd47及びegfrの二重標的化による癌治療 | |
| CN106459184B (zh) | 与抗cd38抗体联用的组合疗法 | |
| CN106456731B (zh) | 用于治疗急性成淋巴细胞性白血病的抗cd38抗体 | |
| CN108367011A (zh) | 使用tlr8激动剂治疗癌症 | |
| TW201827076A (zh) | 使用抗pd-l1抗體及抗雄激素治療癌症之方法 | |
| WO2022043895A2 (en) | Treatment of non-small lung cancer with egfr mutations | |
| AU2013291964B2 (en) | Novel therapeutic treatments with anti-HER2 antibodies having a low fucosylation | |
| KR20140130455A (ko) | Adcc-강화 항체를 사용한 암 치료용 예측 바이오마커 | |
| Ooki et al. | Novel immunotherapy for gastric cancer: targeting the CD47–SIRPα axis | |
| JP2025537137A (ja) | 抗ccr8抗体、化学療法及び免疫療法の組み合わせを使用する抗がん療法 | |
| TW201625301A (zh) | 藉由folr1標靶藥及葉酸代謝拮抗劑用於癌症患者之治療方法與醫藥 | |
| JP2024537091A (ja) | 少なくともegfrに結合する抗体を使用した、免疫チェックポイント阻害剤で治療された高いegfr発現を有するがんの治療 | |
| CN110177807B (zh) | 使用抗MUC1抗体和ErbB抑制剂的抗癌治疗 | |
| US20250215087A1 (en) | Combination therapy of kras inhibitor and treg depleting agent |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20170407 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20170407 |
|
| A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20171107 |