UA113158C2

UA113158C2 - Фармацевтична таблетка

Фармацевтична таблетка Download PDF

Info

Publication number: UA113158C2
Authority: UA; Ukraine
Prior art keywords: compound; tablet; amount; tablets; excipients
Prior art date: 2010-12-20

Application number

UAA201309128A

Other languages

English (en)

Ukrainian (uk)

Priority date

2010-12-20

Filing date

2011-12-20

Publication date

2016-12-26

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46314827&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UA113158(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2011-12-20 Application filed filed Critical

2016-12-26 Publication of UA113158C2 publication Critical patent/UA113158C2/uk

Links

IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims abstract description 48
238000000034 method Methods 0.000 claims abstract description 25
239000012453 solvate Substances 0.000 claims abstract description 20
METKIMKYRPQLGS-UHFFFAOYSA-N atenolol Chemical compound CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-UHFFFAOYSA-N 0.000 claims abstract description 3
238000011282 treatment Methods 0.000 claims description 58
239000000203 mixture Substances 0.000 claims description 53
239000003814 drug Substances 0.000 claims description 32
206010028980 Neoplasm Diseases 0.000 claims description 31
229940079593 drug Drugs 0.000 claims description 31
239000002245 particle Substances 0.000 claims description 31
239000007888 film coating Substances 0.000 claims description 24
238000009501 film coating Methods 0.000 claims description 24
239000000546 pharmaceutical excipient Substances 0.000 claims description 24
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 19
201000011510 cancer Diseases 0.000 claims description 18
UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 claims description 14
FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 8
229930195725 Mannitol Natural products 0.000 claims description 8
239000000594 mannitol Substances 0.000 claims description 8
235000010355 mannitol Nutrition 0.000 claims description 8
238000003825 pressing Methods 0.000 claims description 8
229920000168 Microcrystalline cellulose Polymers 0.000 claims description 7
235000019813 microcrystalline cellulose Nutrition 0.000 claims description 7
239000008108 microcrystalline cellulose Substances 0.000 claims description 7
229940016286 microcrystalline cellulose Drugs 0.000 claims description 7
DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 6
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 4
229920000881 Modified starch Polymers 0.000 claims description 4
239000001913 cellulose Substances 0.000 claims description 4
229940126601 medicinal product Drugs 0.000 claims description 4
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 3
229920002774 Maltodextrin Polymers 0.000 claims description 3
239000005913 Maltodextrin Substances 0.000 claims description 3
229920002472 Starch Polymers 0.000 claims description 3
239000008101 lactose Substances 0.000 claims description 3
229940035034 maltodextrin Drugs 0.000 claims description 3
235000019698 starch Nutrition 0.000 claims description 3
FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 2
FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 2
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
239000001506 calcium phosphate Substances 0.000 claims description 2
239000000832 lactitol Substances 0.000 claims description 2
VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 claims description 2
229960003451 lactitol Drugs 0.000 claims description 2
235000010448 lactitol Nutrition 0.000 claims description 2
238000002156 mixing Methods 0.000 claims description 2
229920003124 powdered cellulose Polymers 0.000 claims description 2
235000019814 powdered cellulose Nutrition 0.000 claims description 2
239000000600 sorbitol Substances 0.000 claims description 2
235000010356 sorbitol Nutrition 0.000 claims description 2
239000008107 starch Substances 0.000 claims description 2
235000019739 Dicalciumphosphate Nutrition 0.000 claims 1
NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 claims 1
229940038472 dicalcium phosphate Drugs 0.000 claims 1
229910000390 dicalcium phosphate Inorganic materials 0.000 claims 1
-1 2-fluoro-4-iodophenylamino Chemical group 0.000 abstract description 28
238000002360 preparation method Methods 0.000 abstract description 4
238000002560 therapeutic procedure Methods 0.000 abstract 1
239000003826 tablet Substances 0.000 description 110
150000001875 compounds Chemical class 0.000 description 93
229940126062 Compound A Drugs 0.000 description 91
NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 91
239000002552 dosage form Substances 0.000 description 57
230000000694 effects Effects 0.000 description 54
239000007787 solid Substances 0.000 description 53
239000003112 inhibitor Substances 0.000 description 38
239000002775 capsule Substances 0.000 description 36
239000003795 chemical substances by application Substances 0.000 description 29
239000007884 disintegrant Substances 0.000 description 26
241000700159 Rattus Species 0.000 description 23
239000002904 solvent Substances 0.000 description 23
239000002246 antineoplastic agent Substances 0.000 description 22
241000282472 Canis lupus familiaris Species 0.000 description 20
239000011230 binding agent Substances 0.000 description 18
239000000314 lubricant Substances 0.000 description 18
239000000243 solution Substances 0.000 description 18
150000003839 salts Chemical class 0.000 description 17
108091000080 Phosphotransferase Proteins 0.000 description 15
239000012535 impurity Substances 0.000 description 15
102000020233 phosphotransferase Human genes 0.000 description 15
229920000642 polymer Polymers 0.000 description 15
239000000126 substance Substances 0.000 description 15
206010065553 Bone marrow failure Diseases 0.000 description 14
108020004414 DNA Proteins 0.000 description 14
241000282414 Homo sapiens Species 0.000 description 14
239000007924 injection Substances 0.000 description 14
238000002347 injection Methods 0.000 description 14
239000007909 solid dosage form Substances 0.000 description 14
230000009471 action Effects 0.000 description 12
230000022131 cell cycle Effects 0.000 description 12
230000005764 inhibitory process Effects 0.000 description 12
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical class O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 11
239000013543 active substance Substances 0.000 description 11
210000004027 cell Anatomy 0.000 description 11
238000004807 desolvation Methods 0.000 description 11
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 11
239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 11
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 11
230000004060 metabolic process Effects 0.000 description 11
239000000725 suspension Substances 0.000 description 11
WYWHKKSPHMUBEB-UHFFFAOYSA-N tioguanine Chemical compound N1C(N)=NC(=S)C2=C1N=CN2 WYWHKKSPHMUBEB-UHFFFAOYSA-N 0.000 description 11
DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 10
229940034982 antineoplastic agent Drugs 0.000 description 10
239000011248 coating agent Substances 0.000 description 10
238000000576 coating method Methods 0.000 description 10
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 10
235000019333 sodium laurylsulphate Nutrition 0.000 description 10
230000001225 therapeutic effect Effects 0.000 description 10
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 9
AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 8
102000009465 Growth Factor Receptors Human genes 0.000 description 8
108010009202 Growth Factor Receptors Proteins 0.000 description 8
206010025323 Lymphomas Diseases 0.000 description 8
NIJJYAXOARWZEE-UHFFFAOYSA-N Valproic acid Chemical compound CCCC(C(O)=O)CCC NIJJYAXOARWZEE-UHFFFAOYSA-N 0.000 description 8
RJURFGZVJUQBHK-UHFFFAOYSA-N actinomycin D Natural products CC1OC(=O)C(C(C)C)N(C)C(=O)CN(C)C(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)NC4C(=O)NC(C(N5CCCC5C(=O)N(C)CC(=O)N(C)C(C(C)C)C(=O)OC4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-UHFFFAOYSA-N 0.000 description 8
229940127089 cytotoxic agent Drugs 0.000 description 8
238000004519 manufacturing process Methods 0.000 description 8
239000012907 medicinal substance Substances 0.000 description 8
239000008194 pharmaceutical composition Substances 0.000 description 8
230000019491 signal transduction Effects 0.000 description 8
241000863480 Vinca Species 0.000 description 7
230000015572 biosynthetic process Effects 0.000 description 7
230000030833 cell death Effects 0.000 description 7
DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 7
229940088597 hormone Drugs 0.000 description 7
239000005556 hormone Substances 0.000 description 7
201000002364 leukopenia Diseases 0.000 description 7
231100001022 leukopenia Toxicity 0.000 description 7
229960001855 mannitol Drugs 0.000 description 7
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 7
239000004014 plasticizer Substances 0.000 description 7
BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 description 7
KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 description 6
206010000830 Acute leukaemia Diseases 0.000 description 6
206010006187 Breast cancer Diseases 0.000 description 6
229920002785 Croscarmellose sodium Polymers 0.000 description 6
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 description 6
108090000323 DNA Topoisomerases Proteins 0.000 description 6
102000003915 DNA Topoisomerases Human genes 0.000 description 6
230000006820 DNA synthesis Effects 0.000 description 6
208000017604 Hodgkin disease Diseases 0.000 description 6
101001091371 Homo sapiens Kallikrein-8 Proteins 0.000 description 6
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
102000001253 Protein Kinase Human genes 0.000 description 6
DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 6
229930013930 alkaloid Natural products 0.000 description 6
229960004316 cisplatin Drugs 0.000 description 6
229940075614 colloidal silicon dioxide Drugs 0.000 description 6
229960001681 croscarmellose sodium Drugs 0.000 description 6
235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 6
229960000684 cytarabine Drugs 0.000 description 6
238000011161 development Methods 0.000 description 6
230000018109 developmental process Effects 0.000 description 6
150000004141 diterpene derivatives Chemical class 0.000 description 6
229960002949 fluorouracil Drugs 0.000 description 6
230000006870 function Effects 0.000 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 description 6
229960005277 gemcitabine Drugs 0.000 description 6
229960003943 hypromellose Drugs 0.000 description 6
229960004768 irinotecan Drugs 0.000 description 6
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 description 6
230000003285 pharmacodynamic effect Effects 0.000 description 6
239000000049 pigment Substances 0.000 description 6
238000012545 processing Methods 0.000 description 6
108060006633 protein kinase Proteins 0.000 description 6
230000011664 signaling Effects 0.000 description 6
230000001629 suppression Effects 0.000 description 6
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 description 6
206010043554 thrombocytopenia Diseases 0.000 description 6
URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 6
FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 description 5
108010006654 Bleomycin Proteins 0.000 description 5
208000026310 Breast neoplasm Diseases 0.000 description 5
COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 5
DLGOEMSEDOSKAD-UHFFFAOYSA-N Carmustine Chemical compound ClCCNC(=O)N(N=O)CCCl DLGOEMSEDOSKAD-UHFFFAOYSA-N 0.000 description 5
108010092160 Dactinomycin Proteins 0.000 description 5
GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 description 5
PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 5
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 5
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 description 5
229930012538 Paclitaxel Natural products 0.000 description 5
102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 5
108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 5
OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical class N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 description 5
229940127093 camptothecin Drugs 0.000 description 5
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 description 5
238000011260 co-administration Methods 0.000 description 5
238000007907 direct compression Methods 0.000 description 5
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
238000004090 dissolution Methods 0.000 description 5
238000007908 dry granulation Methods 0.000 description 5
230000012010 growth Effects 0.000 description 5
UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 5
230000002401 inhibitory effect Effects 0.000 description 5
230000003993 interaction Effects 0.000 description 5
235000019359 magnesium stearate Nutrition 0.000 description 5
239000000463 material Substances 0.000 description 5
GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 description 5
229960000485 methotrexate Drugs 0.000 description 5
229960001592 paclitaxel Drugs 0.000 description 5
238000002638 palliative care Methods 0.000 description 5
102000004169 proteins and genes Human genes 0.000 description 5
108090000623 proteins and genes Proteins 0.000 description 5
238000011160 research Methods 0.000 description 5
238000003860 storage Methods 0.000 description 5
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 description 5
229960001278 teniposide Drugs 0.000 description 5
238000012360 testing method Methods 0.000 description 5
229960003087 tioguanine Drugs 0.000 description 5
229960000303 topotecan Drugs 0.000 description 5
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 description 5
231100000041 toxicology testing Toxicity 0.000 description 5
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 description 4
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
201000009030 Carcinoma Diseases 0.000 description 4
CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 description 4
102000053602 DNA Human genes 0.000 description 4
239000001856 Ethyl cellulose Substances 0.000 description 4
ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 4
239000000579 Gonadotropin-Releasing Hormone Substances 0.000 description 4
208000010747 Hodgkins lymphoma Diseases 0.000 description 4
241000282412 Homo Species 0.000 description 4
241001465754 Metazoa Species 0.000 description 4
ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 description 4
206010033128 Ovarian cancer Diseases 0.000 description 4
229940079156 Proteasome inhibitor Drugs 0.000 description 4
101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 description 4
102000004243 Tubulin Human genes 0.000 description 4
108090000704 Tubulin Proteins 0.000 description 4
RJURFGZVJUQBHK-IIXSONLDSA-N actinomycin D Chemical compound C[C@H]1OC(=O)[C@H](C(C)C)N(C)C(=O)CN(C)C(=O)[C@@H]2CCCN2C(=O)[C@@H](C(C)C)NC(=O)[C@H]1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)N[C@@H]4C(=O)N[C@@H](C(N5CCC[C@H]5C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-IIXSONLDSA-N 0.000 description 4
230000004913 activation Effects 0.000 description 4
239000004480 active ingredient Substances 0.000 description 4
239000008186 active pharmaceutical agent Substances 0.000 description 4
230000002411 adverse Effects 0.000 description 4
229940100198 alkylating agent Drugs 0.000 description 4
239000002168 alkylating agent Substances 0.000 description 4
230000033115 angiogenesis Effects 0.000 description 4
238000010171 animal model 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
210000004369 blood Anatomy 0.000 description 4
239000008280 blood Substances 0.000 description 4
210000001185 bone marrow Anatomy 0.000 description 4
229960004562 carboplatin Drugs 0.000 description 4
229960005243 carmustine Drugs 0.000 description 4
229960004630 chlorambucil Drugs 0.000 description 4
JCKYGMPEJWAADB-UHFFFAOYSA-N chlorambucil Chemical compound OC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 JCKYGMPEJWAADB-UHFFFAOYSA-N 0.000 description 4
229960004397 cyclophosphamide Drugs 0.000 description 4
229960003901 dacarbazine Drugs 0.000 description 4
229960000640 dactinomycin Drugs 0.000 description 4
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 description 4
229960000975 daunorubicin Drugs 0.000 description 4
238000000354 decomposition reaction Methods 0.000 description 4
229960003668 docetaxel Drugs 0.000 description 4
229960004679 doxorubicin Drugs 0.000 description 4
229940088679 drug related substance Drugs 0.000 description 4
235000019325 ethyl cellulose Nutrition 0.000 description 4
229920001249 ethyl cellulose Polymers 0.000 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 description 4
229960005420 etoposide Drugs 0.000 description 4
239000000945 filler Substances 0.000 description 4
238000009472 formulation Methods 0.000 description 4
XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 description 4
229940035638 gonadotropin-releasing hormone Drugs 0.000 description 4
238000004128 high performance liquid chromatography Methods 0.000 description 4
CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical group O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 description 4
239000003446 ligand Substances 0.000 description 4
229960001924 melphalan Drugs 0.000 description 4
SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 description 4
229960001428 mercaptopurine Drugs 0.000 description 4
230000011278 mitosis Effects 0.000 description 4
102000037979 non-receptor tyrosine kinases Human genes 0.000 description 4
108091008046 non-receptor tyrosine kinases Proteins 0.000 description 4
229910052697 platinum Inorganic materials 0.000 description 4
239000000843 powder Substances 0.000 description 4
125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 4
239000003207 proteasome inhibitor Substances 0.000 description 4
108091008598 receptor tyrosine kinases Proteins 0.000 description 4
102000027426 receptor tyrosine kinases Human genes 0.000 description 4
102000005962 receptors Human genes 0.000 description 4
108020003175 receptors Proteins 0.000 description 4
230000004044 response Effects 0.000 description 4
230000035939 shock Effects 0.000 description 4
238000003786 synthesis reaction Methods 0.000 description 4
229960000604 valproic acid Drugs 0.000 description 4
JXLYSJRDGCGARV-CFWMRBGOSA-N vinblastine Chemical compound C([C@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-CFWMRBGOSA-N 0.000 description 4
229960003048 vinblastine Drugs 0.000 description 4
OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 description 4
229960004528 vincristine Drugs 0.000 description 4
OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 description 4
229960002066 vinorelbine Drugs 0.000 description 4
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 description 4
CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
108091007914 CDKs Proteins 0.000 description 3
229920002134 Carboxymethyl cellulose Polymers 0.000 description 3
102000003903 Cyclin-dependent kinases Human genes 0.000 description 3
108090000266 Cyclin-dependent kinases Proteins 0.000 description 3
102000004190 Enzymes Human genes 0.000 description 3
108090000790 Enzymes Proteins 0.000 description 3
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
102000029749 Microtubule Human genes 0.000 description 3
108091022875 Microtubule Proteins 0.000 description 3
102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 description 3
108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 description 3
206010028116 Mucosal inflammation Diseases 0.000 description 3
201000010927 Mucositis Diseases 0.000 description 3
208000034578 Multiple myelomas Diseases 0.000 description 3
206010028813 Nausea Diseases 0.000 description 3
208000015914 Non-Hodgkin lymphomas Diseases 0.000 description 3
108700020796 Oncogene Proteins 0.000 description 3
206010035226 Plasma cell myeloma Diseases 0.000 description 3
LCTONWCANYUPML-UHFFFAOYSA-M Pyruvate Chemical compound CC(=O)C([O-])=O LCTONWCANYUPML-UHFFFAOYSA-M 0.000 description 3
108091005682 Receptor kinases Proteins 0.000 description 3
MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 3
QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 3
208000024313 Testicular Neoplasms Diseases 0.000 description 3
206010057644 Testis cancer Diseases 0.000 description 3
JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 description 3
206010047700 Vomiting Diseases 0.000 description 3
238000010521 absorption reaction Methods 0.000 description 3
238000009825 accumulation Methods 0.000 description 3
229930183665 actinomycin Natural products 0.000 description 3
208000007502 anemia Diseases 0.000 description 3
230000000118 anti-neoplastic effect Effects 0.000 description 3
230000000692 anti-sense effect Effects 0.000 description 3
230000008901 benefit Effects 0.000 description 3
230000004071 biological effect Effects 0.000 description 3
229960001561 bleomycin Drugs 0.000 description 3
229960002092 busulfan Drugs 0.000 description 3
235000010948 carboxy methyl cellulose Nutrition 0.000 description 3
239000001768 carboxy methyl cellulose Substances 0.000 description 3
230000004663 cell proliferation Effects 0.000 description 3
235000010980 cellulose Nutrition 0.000 description 3
229920002678 cellulose Polymers 0.000 description 3
230000008859 change Effects 0.000 description 3
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
239000008199 coating composition Substances 0.000 description 3
239000003086 colorant Substances 0.000 description 3
230000001419 dependent effect Effects 0.000 description 3
201000010099 disease Diseases 0.000 description 3
239000006185 dispersion Substances 0.000 description 3
238000009826 distribution Methods 0.000 description 3
239000003937 drug carrier Substances 0.000 description 3
238000005516 engineering process Methods 0.000 description 3
CJMJLDQKTOJACI-BGQAIRJTSA-N ergotamine d-tartrate Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.C([C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@@](C(N21)=O)(C)NC(=O)[C@H]1CN([C@H]2C(C=3C=CC=C4NC=C(C=34)C2)=C1)C)C1=CC=CC=C1.C([C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@@](C(N21)=O)(C)NC(=O)[C@H]1CN([C@H]2C(C=3C=CC=C4NC=C(C=34)C2)=C1)C)C1=CC=CC=C1 CJMJLDQKTOJACI-BGQAIRJTSA-N 0.000 description 3
238000002474 experimental method Methods 0.000 description 3
230000014509 gene expression Effects 0.000 description 3
231100000025 genetic toxicology Toxicity 0.000 description 3
230000001738 genotoxic effect Effects 0.000 description 3
235000013773 glyceryl triacetate Nutrition 0.000 description 3
230000001900 immune effect Effects 0.000 description 3
229960000367 inositol Drugs 0.000 description 3
231100000682 maximum tolerated dose Toxicity 0.000 description 3
230000007246 mechanism Effects 0.000 description 3
229920000609 methyl cellulose Polymers 0.000 description 3
235000010981 methylcellulose Nutrition 0.000 description 3
239000001923 methylcellulose Substances 0.000 description 3
210000004688 microtubule Anatomy 0.000 description 3
230000008693 nausea Effects 0.000 description 3
208000004235 neutropenia Diseases 0.000 description 3
208000002154 non-small cell lung carcinoma Diseases 0.000 description 3
239000006187 pill Substances 0.000 description 3
229920001223 polyethylene glycol Polymers 0.000 description 3
230000000861 pro-apoptotic effect Effects 0.000 description 3
CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 3
238000011519 second-line treatment Methods 0.000 description 3
201000003120 testicular cancer Diseases 0.000 description 3
210000001519 tissue Anatomy 0.000 description 3
231100000419 toxicity Toxicity 0.000 description 3
230000001988 toxicity Effects 0.000 description 3
229960002622 triacetin Drugs 0.000 description 3
210000004881 tumor cell Anatomy 0.000 description 3
208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 3
230000008673 vomiting Effects 0.000 description 3
WMBWREPUVVBILR-WIYYLYMNSA-N (-)-Epigallocatechin-3-o-gallate Chemical compound O([C@@H]1CC2=C(O)C=C(C=C2O[C@@H]1C=1C=C(O)C(O)=C(O)C=1)O)C(=O)C1=CC(O)=C(O)C(O)=C1 WMBWREPUVVBILR-WIYYLYMNSA-N 0.000 description 2
WZFUQSJFWNHZHM-UHFFFAOYSA-N 2-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)CC(=O)N1CC2=C(CC1)NN=N2 WZFUQSJFWNHZHM-UHFFFAOYSA-N 0.000 description 2
OBKXEAXTFZPCHS-UHFFFAOYSA-N 4-phenylbutyric acid Chemical compound OC(=O)CCCC1=CC=CC=C1 OBKXEAXTFZPCHS-UHFFFAOYSA-N 0.000 description 2
208000031261 Acute myeloid leukaemia Diseases 0.000 description 2
201000004384 Alopecia Diseases 0.000 description 2
102100022014 Angiopoietin-1 receptor Human genes 0.000 description 2
108020000948 Antisense Oligonucleotides Proteins 0.000 description 2
KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 2
VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
102000016736 Cyclin Human genes 0.000 description 2
108050006400 Cyclin Proteins 0.000 description 2
229940123780 DNA topoisomerase I inhibitor Drugs 0.000 description 2
WMBWREPUVVBILR-UHFFFAOYSA-N GCG Natural products C=1C(O)=C(O)C(O)=CC=1C1OC2=CC(O)=CC(O)=C2CC1OC(=O)C1=CC(O)=C(O)C(O)=C1 WMBWREPUVVBILR-UHFFFAOYSA-N 0.000 description 2
206010064147 Gastrointestinal inflammation Diseases 0.000 description 2
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
101000753291 Homo sapiens Angiopoietin-1 receptor Proteins 0.000 description 2
239000004354 Hydroxyethyl cellulose Substances 0.000 description 2
229920000663 Hydroxyethyl cellulose Polymers 0.000 description 2
229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 2
208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 description 2
230000005723 MEK inhibition Effects 0.000 description 2
CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 description 2
208000033776 Myeloid Acute Leukemia Diseases 0.000 description 2
HRNLUBSXIHFDHP-UHFFFAOYSA-N N-(2-aminophenyl)-4-[[[4-(3-pyridinyl)-2-pyrimidinyl]amino]methyl]benzamide Chemical compound NC1=CC=CC=C1NC(=O)C(C=C1)=CC=C1CNC1=NC=CC(C=2C=NC=CC=2)=N1 HRNLUBSXIHFDHP-UHFFFAOYSA-N 0.000 description 2
AMQJEAYHLZJPGS-UHFFFAOYSA-N N-Pentanol Chemical compound CCCCCO AMQJEAYHLZJPGS-UHFFFAOYSA-N 0.000 description 2
108091034117 Oligonucleotide Proteins 0.000 description 2
206010061535 Ovarian neoplasm Diseases 0.000 description 2
DLRVVLDZNNYCBX-UHFFFAOYSA-N Polydextrose Polymers OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(O)O1 DLRVVLDZNNYCBX-UHFFFAOYSA-N 0.000 description 2
229920002565 Polyethylene Glycol 400 Polymers 0.000 description 2
206010060862 Prostate cancer Diseases 0.000 description 2
102000003923 Protein Kinase C Human genes 0.000 description 2
108090000315 Protein Kinase C Proteins 0.000 description 2
102000004278 Receptor Protein-Tyrosine Kinases Human genes 0.000 description 2
108090000873 Receptor Protein-Tyrosine Kinases Proteins 0.000 description 2
UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 description 2
241001116498 Taxus baccata Species 0.000 description 2
206010043275 Teratogenicity Diseases 0.000 description 2
RMMPZDDLWLALLJ-UHFFFAOYSA-N Thermophillin Chemical compound COC1=CC(=O)C(OC)=CC1=O RMMPZDDLWLALLJ-UHFFFAOYSA-N 0.000 description 2
239000000365 Topoisomerase I Inhibitor Substances 0.000 description 2
ZFOZVQLOBQUTQQ-UHFFFAOYSA-N Tributyl citrate Chemical compound CCCCOC(=O)CC(O)(C(=O)OCCCC)CC(=O)OCCCC ZFOZVQLOBQUTQQ-UHFFFAOYSA-N 0.000 description 2
RTKIYFITIVXBLE-UHFFFAOYSA-N Trichostatin A Natural products ONC(=O)C=CC(C)=CC(C)C(=O)C1=CC=C(N(C)C)C=C1 RTKIYFITIVXBLE-UHFFFAOYSA-N 0.000 description 2
230000001594 aberrant effect Effects 0.000 description 2
239000002253 acid Substances 0.000 description 2
230000001464 adherent effect Effects 0.000 description 2
239000002671 adjuvant Substances 0.000 description 2
235000010443 alginic acid Nutrition 0.000 description 2
229920000615 alginic acid Polymers 0.000 description 2
229940045714 alkyl sulfonate alkylating agent Drugs 0.000 description 2
150000008052 alkyl sulfonates Chemical class 0.000 description 2
230000029936 alkylation Effects 0.000 description 2
238000005804 alkylation reaction Methods 0.000 description 2
231100000360 alopecia Toxicity 0.000 description 2
238000004458 analytical method Methods 0.000 description 2
239000004037 angiogenesis inhibitor Substances 0.000 description 2
229940121369 angiogenesis inhibitor Drugs 0.000 description 2
208000022531 anorexia Diseases 0.000 description 2
239000005557 antagonist Substances 0.000 description 2
230000001399 anti-metabolic effect Effects 0.000 description 2
229940044684 anti-microtubule agent Drugs 0.000 description 2
229940045719 antineoplastic alkylating agent nitrosoureas Drugs 0.000 description 2
239000003972 antineoplastic antibiotic Substances 0.000 description 2
229940041181 antineoplastic drug Drugs 0.000 description 2
239000000074 antisense oligonucleotide Substances 0.000 description 2
238000012230 antisense oligonucleotides Methods 0.000 description 2
WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 2
229960001467 bortezomib Drugs 0.000 description 2
GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 description 2
210000000481 breast Anatomy 0.000 description 2
201000008275 breast carcinoma Diseases 0.000 description 2
CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical class [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 2
OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
239000008112 carboxymethyl-cellulose Substances 0.000 description 2
229920003086 cellulose ether Polymers 0.000 description 2
239000012829 chemotherapy agent Substances 0.000 description 2
MVPPADPHJFYWMZ-UHFFFAOYSA-N chlorobenzene Chemical compound ClC1=CC=CC=C1 MVPPADPHJFYWMZ-UHFFFAOYSA-N 0.000 description 2
238000004587 chromatography analysis Methods 0.000 description 2
230000001427 coherent effect Effects 0.000 description 2
229920001577 copolymer Polymers 0.000 description 2
231100000433 cytotoxic Toxicity 0.000 description 2
230000001472 cytotoxic effect Effects 0.000 description 2
GYOZYWVXFNDGLU-XLPZGREQSA-N dTMP Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)C1 GYOZYWVXFNDGLU-XLPZGREQSA-N 0.000 description 2
206010061428 decreased appetite Diseases 0.000 description 2
239000002274 desiccant Substances 0.000 description 2
FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical compound CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 description 2
239000003085 diluting agent Substances 0.000 description 2
208000035475 disorder Diseases 0.000 description 2
229960002563 disulfiram Drugs 0.000 description 2
231100000371 dose-limiting toxicity Toxicity 0.000 description 2
229940030275 epigallocatechin gallate Drugs 0.000 description 2
230000029142 excretion Effects 0.000 description 2
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 description 2
229960000961 floxuridine Drugs 0.000 description 2
230000002496 gastric effect Effects 0.000 description 2
208000018925 gastrointestinal mucositis Diseases 0.000 description 2
235000011187 glycerol Nutrition 0.000 description 2
239000001087 glyceryl triacetate Substances 0.000 description 2
239000008187 granular material Substances 0.000 description 2
230000010224 hepatic metabolism Effects 0.000 description 2
229940121372 histone deacetylase inhibitor Drugs 0.000 description 2
239000003276 histone deacetylase inhibitor Substances 0.000 description 2
239000002944 hormone and hormone analog Substances 0.000 description 2
230000036571 hydration Effects 0.000 description 2
238000006703 hydration reaction Methods 0.000 description 2
235000019447 hydroxyethyl cellulose Nutrition 0.000 description 2
235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
239000001863 hydroxypropyl cellulose Substances 0.000 description 2
230000006698 induction Effects 0.000 description 2
NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
238000011835 investigation Methods 0.000 description 2
PHTQWCKDNZKARW-UHFFFAOYSA-N isoamylol Chemical compound CC(C)CCO PHTQWCKDNZKARW-UHFFFAOYSA-N 0.000 description 2
210000003734 kidney Anatomy 0.000 description 2
229960001375 lactose Drugs 0.000 description 2
230000000670 limiting effect Effects 0.000 description 2
239000007937 lozenge Substances 0.000 description 2
229950002736 marizomib Drugs 0.000 description 2
230000001394 metastastic effect Effects 0.000 description 2
206010061289 metastatic neoplasm Diseases 0.000 description 2
229950007812 mocetinostat Drugs 0.000 description 2
229910052757 nitrogen Inorganic materials 0.000 description 2
231100000062 no-observed-adverse-effect level Toxicity 0.000 description 2
102000039446 nucleic acids Human genes 0.000 description 2
108020004707 nucleic acids Proteins 0.000 description 2
150000007523 nucleic acids Chemical class 0.000 description 2
230000001590 oxidative effect Effects 0.000 description 2
238000004806 packaging method and process Methods 0.000 description 2
229960005184 panobinostat Drugs 0.000 description 2
FWZRWHZDXBDTFK-ZHACJKMWSA-N panobinostat Chemical compound CC1=NC2=CC=C[CH]C2=C1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FWZRWHZDXBDTFK-ZHACJKMWSA-N 0.000 description 2
230000035699 permeability Effects 0.000 description 2
239000001267 polyvinylpyrrolidone Substances 0.000 description 2
229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 description 2
229960004618 prednisone Drugs 0.000 description 2
230000002265 prevention Effects 0.000 description 2
230000008569 process Effects 0.000 description 2
235000013772 propylene glycol Nutrition 0.000 description 2
201000001514 prostate carcinoma Diseases 0.000 description 2
230000009467 reduction Effects 0.000 description 2
230000002829 reductive effect Effects 0.000 description 2
230000021014 regulation of cell growth Effects 0.000 description 2
230000001105 regulatory effect Effects 0.000 description 2
230000010076 replication Effects 0.000 description 2
238000012552 review Methods 0.000 description 2
229960003452 romidepsin Drugs 0.000 description 2
OHRURASPPZQGQM-GCCNXGTGSA-N romidepsin Chemical compound O1C(=O)[C@H](C(C)C)NC(=O)C(=C/C)/NC(=O)[C@H]2CSSCC\C=C\[C@@H]1CC(=O)N[C@H](C(C)C)C(=O)N2 OHRURASPPZQGQM-GCCNXGTGSA-N 0.000 description 2
OHRURASPPZQGQM-UHFFFAOYSA-N romidepsin Natural products O1C(=O)C(C(C)C)NC(=O)C(=CC)NC(=O)C2CSSCCC=CC1CC(=O)NC(C(C)C)C(=O)N2 OHRURASPPZQGQM-UHFFFAOYSA-N 0.000 description 2
108010091666 romidepsin Proteins 0.000 description 2
NGWSFRIPKNWYAO-UHFFFAOYSA-N salinosporamide A Natural products N1C(=O)C(CCCl)C2(C)OC(=O)C21C(O)C1CCCC=C1 NGWSFRIPKNWYAO-UHFFFAOYSA-N 0.000 description 2
NGWSFRIPKNWYAO-SHTIJGAHSA-N salinosporamide A Chemical compound C([C@@H]1[C@H](O)[C@]23C(=O)O[C@]2([C@H](C(=O)N3)CCCl)C)CCC=C1 NGWSFRIPKNWYAO-SHTIJGAHSA-N 0.000 description 2
239000000333 selective estrogen receptor modulator Substances 0.000 description 2
229940095743 selective estrogen receptor modulator Drugs 0.000 description 2
235000012239 silicon dioxide Nutrition 0.000 description 2
239000000377 silicon dioxide Substances 0.000 description 2
229960001866 silicon dioxide Drugs 0.000 description 2
239000004094 surface-active agent Substances 0.000 description 2
230000009885 systemic effect Effects 0.000 description 2
239000007916 tablet composition Substances 0.000 description 2
231100000211 teratogenicity Toxicity 0.000 description 2
230000002381 testicular Effects 0.000 description 2
AUZONCFQVSMFAP-UHFFFAOYSA-N tetraethylthiuram disulfide Natural products CCN(CC)C(=S)SSC(=S)N(CC)CC AUZONCFQVSMFAP-UHFFFAOYSA-N 0.000 description 2
231100000331 toxic Toxicity 0.000 description 2
230000002588 toxic effect Effects 0.000 description 2
150000004654 triazenes Chemical class 0.000 description 2
RTKIYFITIVXBLE-QEQCGCAPSA-N trichostatin A Chemical compound ONC(=O)/C=C/C(/C)=C/[C@@H](C)C(=O)C1=CC=C(N(C)C)C=C1 RTKIYFITIVXBLE-QEQCGCAPSA-N 0.000 description 2
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 2
229960000237 vorinostat Drugs 0.000 description 2
WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 description 2
JWOGUUIOCYMBPV-GMFLJSBRSA-N (3S,6S,9S,12R)-3-[(2S)-Butan-2-yl]-6-[(1-methoxyindol-3-yl)methyl]-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone Chemical compound N1C(=O)[C@H](CCCCCC(=O)CC)NC(=O)[C@H]2CCCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]1CC1=CN(OC)C2=CC=CC=C12 JWOGUUIOCYMBPV-GMFLJSBRSA-N 0.000 description 1
FPVKHBSQESCIEP-UHFFFAOYSA-N (8S)-3-(2-deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol Natural products C1C(O)C(CO)OC1N1C(NC=NCC2O)=C2N=C1 FPVKHBSQESCIEP-UHFFFAOYSA-N 0.000 description 1
LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 description 1
QRPSQQUYPMFERG-LFYBBSHMSA-N (e)-5-[3-(benzenesulfonamido)phenyl]-n-hydroxypent-2-en-4-ynamide Chemical compound ONC(=O)\C=C\C#CC1=CC=CC(NS(=O)(=O)C=2C=CC=CC=2)=C1 QRPSQQUYPMFERG-LFYBBSHMSA-N 0.000 description 1
108091032973 (ribonucleotides)n+m Proteins 0.000 description 1
LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 1
ZNQVEEAIQZEUHB-UHFFFAOYSA-N 2-ethoxyethanol Chemical compound CCOCCO ZNQVEEAIQZEUHB-UHFFFAOYSA-N 0.000 description 1
NEAQRZUHTPSBBM-UHFFFAOYSA-N 2-hydroxy-3,3-dimethyl-7-nitro-4h-isoquinolin-1-one Chemical class C1=C([N+]([O-])=O)C=C2C(=O)N(O)C(C)(C)CC2=C1 NEAQRZUHTPSBBM-UHFFFAOYSA-N 0.000 description 1
ZZVDXRCAGGQFAK-UHFFFAOYSA-N 2h-oxazaphosphinine Chemical class N1OC=CC=P1 ZZVDXRCAGGQFAK-UHFFFAOYSA-N 0.000 description 1
YVCVYCSAAZQOJI-JHQYFNNDSA-N 4'-demethylepipodophyllotoxin Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O)[C@@H]3[C@@H]2C(OC3)=O)=C1 YVCVYCSAAZQOJI-JHQYFNNDSA-N 0.000 description 1
NMUSYJAQQFHJEW-UHFFFAOYSA-N 5-Azacytidine Natural products O=C1N=C(N)N=CN1C1C(O)C(O)C(CO)O1 NMUSYJAQQFHJEW-UHFFFAOYSA-N 0.000 description 1
NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical compound O=C1N=C(N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 NMUSYJAQQFHJEW-KVTDHHQDSA-N 0.000 description 1
HFEKDTCAMMOLQP-RRKCRQDMSA-N 5-fluorodeoxyuridine monophosphate Chemical compound O1[C@H](COP(O)(O)=O)[C@@H](O)C[C@@H]1N1C(=O)NC(=O)C(F)=C1 HFEKDTCAMMOLQP-RRKCRQDMSA-N 0.000 description 1
YWLXLRUDGLRYDR-ZHPRIASZSA-N 5beta,20-epoxy-1,7beta,10beta,13alpha-tetrahydroxy-9-oxotax-11-ene-2alpha,4alpha-diyl 4-acetate 2-benzoate Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](O)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 YWLXLRUDGLRYDR-ZHPRIASZSA-N 0.000 description 1
JTDYUFSDZATMKU-UHFFFAOYSA-N 6-(1,3-dioxo-2-benzo[de]isoquinolinyl)-N-hydroxyhexanamide Chemical compound C1=CC(C(N(CCCCCC(=O)NO)C2=O)=O)=C3C2=CC=CC3=C1 JTDYUFSDZATMKU-UHFFFAOYSA-N 0.000 description 1
HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
102100033350 ATP-dependent translocase ABCB1 Human genes 0.000 description 1
QZCLKYGREBVARF-UHFFFAOYSA-N Acetyl tributyl citrate Chemical compound CCCCOC(=O)CC(C(=O)OCCCC)(OC(C)=O)CC(=O)OCCCC QZCLKYGREBVARF-UHFFFAOYSA-N 0.000 description 1
208000024893 Acute lymphoblastic leukemia Diseases 0.000 description 1
208000014697 Acute lymphocytic leukaemia Diseases 0.000 description 1
102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 description 1
108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 description 1
229920001817 Agar Polymers 0.000 description 1
239000005995 Aluminium silicate Substances 0.000 description 1
102400000068 Angiostatin Human genes 0.000 description 1
108010079709 Angiostatins Proteins 0.000 description 1
101500021169 Aplysia californica Myomodulin-G Proteins 0.000 description 1
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 description 1
208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 description 1
208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 1
206010004446 Benign prostatic hyperplasia Diseases 0.000 description 1
206010005003 Bladder cancer Diseases 0.000 description 1
108010017384 Blood Proteins Proteins 0.000 description 1
102000004506 Blood Proteins Human genes 0.000 description 1
239000004135 Bone phosphate Substances 0.000 description 1
208000003174 Brain Neoplasms Diseases 0.000 description 1
102100022595 Broad substrate specificity ATP-binding cassette transporter ABCG2 Human genes 0.000 description 1
101100190541 Caenorhabditis elegans pink-1 gene Proteins 0.000 description 1
KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 description 1
102000053642 Catalytic RNA Human genes 0.000 description 1
108090000994 Catalytic RNA Proteins 0.000 description 1
102100025064 Cellular tumor antigen p53 Human genes 0.000 description 1
PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 description 1
208000010833 Chronic myeloid leukaemia Diseases 0.000 description 1
241000207199 Citrus Species 0.000 description 1
PTOAARAWEBMLNO-KVQBGUIXSA-N Cladribine Chemical compound C1=NC=2C(N)=NC(Cl)=NC=2N1[C@H]1C[C@H](O)[C@@H](CO)O1 PTOAARAWEBMLNO-KVQBGUIXSA-N 0.000 description 1
206010055114 Colon cancer metastatic Diseases 0.000 description 1
229920002261 Corn starch Polymers 0.000 description 1
102000018832 Cytochromes Human genes 0.000 description 1
108010052832 Cytochromes Proteins 0.000 description 1
231100001074 DNA strand break Toxicity 0.000 description 1
229940124087 DNA topoisomerase II inhibitor Drugs 0.000 description 1
FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
206010012735 Diarrhoea Diseases 0.000 description 1
ZQZFYGIXNQKOAV-OCEACIFDSA-N Droloxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=C(O)C=CC=1)\C1=CC=C(OCCN(C)C)C=C1 ZQZFYGIXNQKOAV-OCEACIFDSA-N 0.000 description 1
102000018386 EGF Family of Proteins Human genes 0.000 description 1
108010066486 EGF Family of Proteins Proteins 0.000 description 1
206010014733 Endometrial cancer Diseases 0.000 description 1
206010014759 Endometrial neoplasm Diseases 0.000 description 1
102400001047 Endostatin Human genes 0.000 description 1
108010079505 Endostatins Proteins 0.000 description 1
102000050554 Eph Family Receptors Human genes 0.000 description 1
108091008815 Eph receptors Proteins 0.000 description 1
102400001368 Epidermal growth factor Human genes 0.000 description 1
101800003838 Epidermal growth factor Proteins 0.000 description 1
OTMSDBZUPAUEDD-UHFFFAOYSA-N Ethane Chemical compound CC OTMSDBZUPAUEDD-UHFFFAOYSA-N 0.000 description 1
VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
239000005977 Ethylene Substances 0.000 description 1
LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
241000238558 Eucarida Species 0.000 description 1
108091008794 FGF receptors Proteins 0.000 description 1
102000007317 Farnesyltranstransferase Human genes 0.000 description 1
108010007508 Farnesyltranstransferase Proteins 0.000 description 1
102000044168 Fibroblast Growth Factor Receptor Human genes 0.000 description 1
102000016621 Focal Adhesion Protein-Tyrosine Kinases Human genes 0.000 description 1
108010067715 Focal Adhesion Protein-Tyrosine Kinases Proteins 0.000 description 1
102000012673 Follicle Stimulating Hormone Human genes 0.000 description 1
108010079345 Follicle Stimulating Hormone Proteins 0.000 description 1
108010069236 Goserelin Proteins 0.000 description 1
229920002907 Guar gum Polymers 0.000 description 1
SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 description 1
101000823298 Homo sapiens Broad substrate specificity ATP-binding cassette transporter ABCG2 Proteins 0.000 description 1
JJKOTMDDZAJTGQ-DQSJHHFOSA-N Idoxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN2CCCC2)=CC=1)/C1=CC=C(I)C=C1 JJKOTMDDZAJTGQ-DQSJHHFOSA-N 0.000 description 1
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
102100023915 Insulin Human genes 0.000 description 1
108090001061 Insulin Proteins 0.000 description 1
208000007766 Kaposi sarcoma Diseases 0.000 description 1
102000003855 L-lactate dehydrogenase Human genes 0.000 description 1
102100034671 L-lactate dehydrogenase A chain Human genes 0.000 description 1
108700023483 L-lactate dehydrogenases Proteins 0.000 description 1
GHSJKUNUIHUPDF-BYPYZUCNSA-N L-thialysine Chemical compound NCCSC[C@H](N)C(O)=O GHSJKUNUIHUPDF-BYPYZUCNSA-N 0.000 description 1
108010088350 Lactate Dehydrogenase 5 Proteins 0.000 description 1
208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 description 1
208000035561 Leukaemic infiltration brain Diseases 0.000 description 1
206010058467 Lung neoplasm malignant Diseases 0.000 description 1
108091054455 MAP kinase family Proteins 0.000 description 1
102000043136 MAP kinase family Human genes 0.000 description 1
229940124647 MEK inhibitor Drugs 0.000 description 1
241000282553 Macaca Species 0.000 description 1
102000007651 Macrophage Colony-Stimulating Factor Human genes 0.000 description 1
108010046938 Macrophage Colony-Stimulating Factor Proteins 0.000 description 1
241000124008 Mammalia Species 0.000 description 1
108010047230 Member 1 Subfamily B ATP Binding Cassette Transporter Proteins 0.000 description 1
241001102832 Meseres Species 0.000 description 1
206010027480 Metastatic malignant melanoma Diseases 0.000 description 1
241000699666 Mus <mouse, genus> Species 0.000 description 1
101000874159 Mus musculus Succinate dehydrogenase [ubiquinone] iron-sulfur subunit, mitochondrial Proteins 0.000 description 1
241000699670 Mus sp. Species 0.000 description 1
208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 1
WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
BHUZLJOUHMBZQY-YXQOSMAKSA-N N-[4-[(2R,4R,6S)-4-[[(4,5-diphenyl-2-oxazolyl)thio]methyl]-6-[4-(hydroxymethyl)phenyl]-1,3-dioxan-2-yl]phenyl]-N'-hydroxyoctanediamide Chemical compound C1=CC(CO)=CC=C1[C@H]1O[C@@H](C=2C=CC(NC(=O)CCCCCCC(=O)NO)=CC=2)O[C@@H](CSC=2OC(=C(N=2)C=2C=CC=CC=2)C=2C=CC=CC=2)C1 BHUZLJOUHMBZQY-YXQOSMAKSA-N 0.000 description 1
206010029155 Nephropathy toxic Diseases 0.000 description 1
102100038494 Nuclear receptor subfamily 1 group I member 2 Human genes 0.000 description 1
JWOGUUIOCYMBPV-UHFFFAOYSA-N OT-Key 11219 Natural products N1C(=O)C(CCCCCC(=O)CC)NC(=O)C2CCCCN2C(=O)C(C(C)CC)NC(=O)C1CC1=CN(OC)C2=CC=CC=C12 JWOGUUIOCYMBPV-UHFFFAOYSA-N 0.000 description 1
102000043276 Oncogene Human genes 0.000 description 1
206010033109 Ototoxicity Diseases 0.000 description 1
208000007571 Ovarian Epithelial Carcinoma Diseases 0.000 description 1
102000004316 Oxidoreductases Human genes 0.000 description 1
108090000854 Oxidoreductases Proteins 0.000 description 1
108091008606 PDGF receptors Proteins 0.000 description 1
229910019142 PO4 Inorganic materials 0.000 description 1
206010061902 Pancreatic neoplasm Diseases 0.000 description 1
108091005804 Peptidases Proteins 0.000 description 1
102000035195 Peptidases Human genes 0.000 description 1
102000017795 Perilipin-1 Human genes 0.000 description 1
108010067162 Perilipin-1 Proteins 0.000 description 1
102000011653 Platelet-Derived Growth Factor Receptors Human genes 0.000 description 1
244000236480 Podophyllum peltatum Species 0.000 description 1
229920001100 Polydextrose Polymers 0.000 description 1
239000002202 Polyethylene glycol Substances 0.000 description 1
208000004880 Polyuria Diseases 0.000 description 1
ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 1
108010001511 Pregnane X Receptor Proteins 0.000 description 1
208000004403 Prostatic Hyperplasia Diseases 0.000 description 1
239000004365 Protease Substances 0.000 description 1
102000001708 Protein Isoforms Human genes 0.000 description 1
108010029485 Protein Isoforms Proteins 0.000 description 1
102000052575 Proto-Oncogene Human genes 0.000 description 1
108700020978 Proto-Oncogene Proteins 0.000 description 1
206010061924 Pulmonary toxicity Diseases 0.000 description 1
108091030071 RNAI Proteins 0.000 description 1
208000015634 Rectal Neoplasms Diseases 0.000 description 1
108091006172 SLC21 Proteins 0.000 description 1
206010059516 Skin toxicity Diseases 0.000 description 1
206010041067 Small cell lung cancer Diseases 0.000 description 1
BCKXLBQYZLBQEK-KVVVOXFISA-M Sodium oleate Chemical compound [Na+].CCCCCCCC\C=C/CCCCCCCC([O-])=O BCKXLBQYZLBQEK-KVVVOXFISA-M 0.000 description 1
102100032846 Solute carrier organic anion transporter family member 1A2 Human genes 0.000 description 1
235000021355 Stearic acid Nutrition 0.000 description 1
208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 1
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
229940123237 Taxane Drugs 0.000 description 1
239000000317 Topoisomerase II Inhibitor Substances 0.000 description 1
102000004357 Transferases Human genes 0.000 description 1
108090000992 Transferases Proteins 0.000 description 1
DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 1
102000014384 Type C Phospholipases Human genes 0.000 description 1
108010079194 Type C Phospholipases Proteins 0.000 description 1
229910052770 Uranium Inorganic materials 0.000 description 1
208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
230000006682 Warburg effect Effects 0.000 description 1
208000008383 Wilms tumor Diseases 0.000 description 1
229920002494 Zein Polymers 0.000 description 1
150000007513 acids Chemical class 0.000 description 1
102000035181 adaptor proteins Human genes 0.000 description 1
108091005764 adaptor proteins Proteins 0.000 description 1
239000000654 additive Substances 0.000 description 1
230000000996 additive effect Effects 0.000 description 1
208000020990 adrenal cortex carcinoma Diseases 0.000 description 1
208000007128 adrenocortical carcinoma Diseases 0.000 description 1
239000008272 agar Substances 0.000 description 1
150000001298 alcohols Chemical class 0.000 description 1
239000000783 alginic acid Substances 0.000 description 1
229960001126 alginic acid Drugs 0.000 description 1
150000004781 alginic acids Chemical class 0.000 description 1
150000003797 alkaloid derivatives Chemical class 0.000 description 1
HZVVJJIYJKGMFL-UHFFFAOYSA-N almasilate Chemical compound O.[Mg+2].[Al+3].[Al+3].O[Si](O)=O.O[Si](O)=O HZVVJJIYJKGMFL-UHFFFAOYSA-N 0.000 description 1
235000012211 aluminium silicate Nutrition 0.000 description 1
229910000323 aluminium silicate Inorganic materials 0.000 description 1
229960003437 aminoglutethimide Drugs 0.000 description 1
ROBVIMPUHSLWNV-UHFFFAOYSA-N aminoglutethimide Chemical compound C=1C=C(N)C=CC=1C1(CC)CCC(=O)NC1=O ROBVIMPUHSLWNV-UHFFFAOYSA-N 0.000 description 1
229960002932 anastrozole Drugs 0.000 description 1
YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 description 1
239000003098 androgen Substances 0.000 description 1
229940030486 androgens Drugs 0.000 description 1
229960004977 anhydrous lactose Drugs 0.000 description 1
229940045799 anthracyclines and related substance Drugs 0.000 description 1
239000003242 anti bacterial agent Substances 0.000 description 1
230000002280 anti-androgenic effect Effects 0.000 description 1
230000002424 anti-apoptotic effect Effects 0.000 description 1
230000001093 anti-cancer Effects 0.000 description 1
229940046836 anti-estrogen Drugs 0.000 description 1
230000001833 anti-estrogenic effect Effects 0.000 description 1
230000003432 anti-folate effect Effects 0.000 description 1
230000000340 anti-metabolite Effects 0.000 description 1
230000001946 anti-microtubular Effects 0.000 description 1
230000001028 anti-proliverative effect Effects 0.000 description 1
230000000259 anti-tumor effect Effects 0.000 description 1
239000000051 antiandrogen Substances 0.000 description 1
229940030495 antiandrogen sex hormone and modulator of the genital system Drugs 0.000 description 1
229940088710 antibiotic agent Drugs 0.000 description 1
229940127074 antifolate Drugs 0.000 description 1
229940100197 antimetabolite Drugs 0.000 description 1
239000002256 antimetabolite Substances 0.000 description 1
239000003080 antimitotic agent Substances 0.000 description 1
108010082820 apicidin Proteins 0.000 description 1
229930186608 apicidin Natural products 0.000 description 1
230000006907 apoptotic process Effects 0.000 description 1
238000013459 approach Methods 0.000 description 1
239000008365 aqueous carrier Substances 0.000 description 1
239000003125 aqueous solvent Substances 0.000 description 1
239000007900 aqueous suspension Substances 0.000 description 1
239000003886 aromatase inhibitor Substances 0.000 description 1
229940046844 aromatase inhibitors Drugs 0.000 description 1
FZCSTZYAHCUGEM-UHFFFAOYSA-N aspergillomarasmine B Natural products OC(=O)CNC(C(O)=O)CNC(C(O)=O)CC(O)=O FZCSTZYAHCUGEM-UHFFFAOYSA-N 0.000 description 1
238000000376 autoradiography Methods 0.000 description 1
229960002756 azacitidine Drugs 0.000 description 1
229960002170 azathioprine Drugs 0.000 description 1
LMEKQMALGUDUQG-UHFFFAOYSA-N azathioprine Chemical compound CN1C=NC([N+]([O-])=O)=C1SC1=NC=NC2=C1NC=N2 LMEKQMALGUDUQG-UHFFFAOYSA-N 0.000 description 1
239000000440 bentonite Substances 0.000 description 1
229910000278 bentonite Inorganic materials 0.000 description 1
SVPXDRXYRYOSEX-UHFFFAOYSA-N bentoquatam Chemical compound O.O=[Si]=O.O=[Al]O[Al]=O SVPXDRXYRYOSEX-UHFFFAOYSA-N 0.000 description 1
125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
102000012740 beta Adrenergic Receptors Human genes 0.000 description 1
108010079452 beta Adrenergic Receptors Proteins 0.000 description 1
208000036815 beta tubulin Diseases 0.000 description 1
229960000997 bicalutamide Drugs 0.000 description 1
210000003445 biliary tract Anatomy 0.000 description 1
238000001574 biopsy Methods 0.000 description 1
230000000903 blocking effect Effects 0.000 description 1
210000000601 blood cell Anatomy 0.000 description 1
210000000988 bone and bone Anatomy 0.000 description 1
ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 description 1
230000006931 brain damage Effects 0.000 description 1
231100000874 brain damage Toxicity 0.000 description 1
208000029028 brain injury Diseases 0.000 description 1
239000004067 bulking agent Substances 0.000 description 1
125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
239000011575 calcium Substances 0.000 description 1
229910000019 calcium carbonate Inorganic materials 0.000 description 1
229910000389 calcium phosphate Inorganic materials 0.000 description 1
235000011010 calcium phosphates Nutrition 0.000 description 1
235000013539 calcium stearate Nutrition 0.000 description 1
239000008116 calcium stearate Substances 0.000 description 1
230000005907 cancer growth Effects 0.000 description 1
229940022399 cancer vaccine Drugs 0.000 description 1
238000009566 cancer vaccine Methods 0.000 description 1
125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 description 1
230000015556 catabolic process Effects 0.000 description 1
239000003729 cation exchange resin Substances 0.000 description 1
229940023913 cation exchange resins Drugs 0.000 description 1
230000011712 cell development Effects 0.000 description 1
230000024245 cell differentiation Effects 0.000 description 1
230000010261 cell growth Effects 0.000 description 1
230000001413 cellular effect Effects 0.000 description 1
230000019522 cellular metabolic process Effects 0.000 description 1
238000001311 chemical methods and process Methods 0.000 description 1
239000003638 chemical reducing agent Substances 0.000 description 1
238000002512 chemotherapy Methods 0.000 description 1
208000032852 chronic lymphocytic leukemia Diseases 0.000 description 1
101150116749 chuk gene Proteins 0.000 description 1
150000001860 citric acid derivatives Chemical class 0.000 description 1
235000020971 citrus fruits Nutrition 0.000 description 1
229960002436 cladribine Drugs 0.000 description 1
210000001072 colon Anatomy 0.000 description 1
238000009500 colour coating Methods 0.000 description 1
238000010835 comparative analysis Methods 0.000 description 1
230000000052 comparative effect Effects 0.000 description 1
239000002131 composite material Substances 0.000 description 1
239000011246 composite particle Substances 0.000 description 1
238000013329 compounding Methods 0.000 description 1
239000008120 corn starch Substances 0.000 description 1
238000005336 cracking Methods 0.000 description 1
229960000913 crospovidone Drugs 0.000 description 1
229920006037 cross link polymer Polymers 0.000 description 1
125000004122 cyclic group Chemical group 0.000 description 1
CCQPAEQGAVNNIA-UHFFFAOYSA-L cyclobutane-1,1-dicarboxylate(2-) Chemical compound [O-]C(=O)C1(C([O-])=O)CCC1 CCQPAEQGAVNNIA-UHFFFAOYSA-L 0.000 description 1
229960000978 cyproterone acetate Drugs 0.000 description 1
UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 description 1
UHDGCWIWMRVCDJ-ZAKLUEHWSA-N cytidine Chemical class O=C1N=C(N)C=CN1[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-ZAKLUEHWSA-N 0.000 description 1
231100000135 cytotoxicity Toxicity 0.000 description 1
230000003013 cytotoxicity Effects 0.000 description 1
230000006378 damage Effects 0.000 description 1
230000009849 deactivation Effects 0.000 description 1
238000006731 degradation reaction Methods 0.000 description 1
230000003111 delayed effect Effects 0.000 description 1
239000008121 dextrose Substances 0.000 description 1
GUJOJGAPFQRJSV-UHFFFAOYSA-N dialuminum;dioxosilane;oxygen(2-);hydrate Chemical compound O.[O-2].[O-2].[O-2].[Al+3].[Al+3].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O GUJOJGAPFQRJSV-UHFFFAOYSA-N 0.000 description 1
JYIMWRSJCRRYNK-UHFFFAOYSA-N dialuminum;disodium;oxygen(2-);silicon(4+);hydrate Chemical compound O.[O-2].[O-2].[O-2].[O-2].[O-2].[O-2].[Na+].[Na+].[Al+3].[Al+3].[Si+4] JYIMWRSJCRRYNK-UHFFFAOYSA-N 0.000 description 1
HNPSIPDUKPIQMN-UHFFFAOYSA-N dioxosilane;oxo(oxoalumanyloxy)alumane Chemical compound O=[Si]=O.O=[Al]O[Al]=O HNPSIPDUKPIQMN-UHFFFAOYSA-N 0.000 description 1
229930004069 diterpene Natural products 0.000 description 1
230000035619 diuresis Effects 0.000 description 1
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 description 1
239000003534 dna topoisomerase inhibitor Substances 0.000 description 1
230000005782 double-strand break Effects 0.000 description 1
229950004203 droloxifene Drugs 0.000 description 1
238000007580 dry-mixing Methods 0.000 description 1
229960004199 dutasteride Drugs 0.000 description 1
JWJOTENAMICLJG-QWBYCMEYSA-N dutasteride Chemical compound O=C([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)N[C@@H]4CC3)C)CC[C@@]21C)NC1=CC(C(F)(F)F)=CC=C1C(F)(F)F JWJOTENAMICLJG-QWBYCMEYSA-N 0.000 description 1
239000012039 electrophile Substances 0.000 description 1
238000010828 elution Methods 0.000 description 1
201000003914 endometrial carcinoma Diseases 0.000 description 1
229940116977 epidermal growth factor Drugs 0.000 description 1
230000008472 epithelial growth Effects 0.000 description 1
229940011871 estrogen Drugs 0.000 description 1
239000000262 estrogen Substances 0.000 description 1
239000000328 estrogen antagonist Substances 0.000 description 1
102000015694 estrogen receptors Human genes 0.000 description 1
108010038795 estrogen receptors Proteins 0.000 description 1
RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 1
MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
210000003527 eukaryotic cell Anatomy 0.000 description 1
238000011156 evaluation Methods 0.000 description 1
229960000255 exemestane Drugs 0.000 description 1
239000007941 film coated tablet Substances 0.000 description 1
229960004039 finasteride Drugs 0.000 description 1
DBEPLOCGEIEOCV-WSBQPABSSA-N finasteride Chemical compound N([C@@H]1CC2)C(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)NC(C)(C)C)[C@@]2(C)CC1 DBEPLOCGEIEOCV-WSBQPABSSA-N 0.000 description 1
GIUYCYHIANZCFB-FJFJXFQQSA-N fludarabine phosphate Chemical compound C1=NC=2C(N)=NC(F)=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]1O GIUYCYHIANZCFB-FJFJXFQQSA-N 0.000 description 1
229960005304 fludarabine phosphate Drugs 0.000 description 1
239000012530 fluid Substances 0.000 description 1
150000005699 fluoropyrimidines Chemical class 0.000 description 1
229960002074 flutamide Drugs 0.000 description 1
MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 description 1
239000004052 folic acid antagonist Substances 0.000 description 1
229940028334 follicle stimulating hormone Drugs 0.000 description 1
201000003444 follicular lymphoma Diseases 0.000 description 1
LNTHITQWFMADLM-UHFFFAOYSA-M gallate Chemical compound OC1=CC(C([O-])=O)=CC(O)=C1O LNTHITQWFMADLM-UHFFFAOYSA-M 0.000 description 1
238000003304 gavage Methods 0.000 description 1
230000009368 gene silencing by RNA Effects 0.000 description 1
125000002686 geranylgeranyl group Chemical group [H]C([*])([H])/C([H])=C(C([H])([H])[H])/C([H])([H])C([H])([H])/C([H])=C(C([H])([H])[H])/C([H])([H])C([H])([H])/C([H])=C(C([H])([H])[H])/C([H])([H])C([H])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
239000008103 glucose Substances 0.000 description 1
150000002303 glucose derivatives Chemical class 0.000 description 1
230000004153 glucose metabolism Effects 0.000 description 1
239000004220 glutamic acid Substances 0.000 description 1
125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 description 1
229960003690 goserelin acetate Drugs 0.000 description 1
238000000227 grinding Methods 0.000 description 1
239000003102 growth factor Substances 0.000 description 1
235000010417 guar gum Nutrition 0.000 description 1
239000000665 guar gum Substances 0.000 description 1
229960002154 guar gum Drugs 0.000 description 1
210000003128 head Anatomy 0.000 description 1
208000018821 hormone-resistant prostate carcinoma Diseases 0.000 description 1
239000008172 hydrogenated vegetable oil Substances 0.000 description 1
230000007062 hydrolysis Effects 0.000 description 1
238000006460 hydrolysis reaction Methods 0.000 description 1
125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
238000005286 illumination Methods 0.000 description 1
125000002883 imidazolyl group Chemical group 0.000 description 1
230000028993 immune response Effects 0.000 description 1
239000002955 immunomodulating agent Substances 0.000 description 1
230000001024 immunotherapeutic effect Effects 0.000 description 1
238000009169 immunotherapy Methods 0.000 description 1
238000010348 incorporation Methods 0.000 description 1
239000004615 ingredient Substances 0.000 description 1
229940102223 injectable solution Drugs 0.000 description 1
229940125396 insulin Drugs 0.000 description 1
102000006495 integrins Human genes 0.000 description 1
108010044426 integrins Proteins 0.000 description 1
239000003456 ion exchange resin Substances 0.000 description 1
229920003303 ion-exchange polymer Polymers 0.000 description 1
NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
150000002576 ketones Chemical class 0.000 description 1
229940043355 kinase inhibitor Drugs 0.000 description 1
208000032839 leukemia Diseases 0.000 description 1
108020001756 ligand binding domains Proteins 0.000 description 1
229940057995 liquid paraffin Drugs 0.000 description 1
210000004185 liver Anatomy 0.000 description 1
201000005202 lung cancer Diseases 0.000 description 1
208000020816 lung neoplasm Diseases 0.000 description 1
230000000527 lymphocytic effect Effects 0.000 description 1
208000025036 lymphosarcoma Diseases 0.000 description 1
229960003511 macrogol Drugs 0.000 description 1
ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
239000001095 magnesium carbonate Substances 0.000 description 1
229910000021 magnesium carbonate Inorganic materials 0.000 description 1
229940037627 magnesium lauryl sulfate Drugs 0.000 description 1
HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 description 1
201000004792 malaria Diseases 0.000 description 1
230000003211 malignant effect Effects 0.000 description 1
208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
210000001161 mammalian embryo Anatomy 0.000 description 1
229960004296 megestrol acetate Drugs 0.000 description 1
RQZAXGRLVPAYTJ-GQFGMJRRSA-N megestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 RQZAXGRLVPAYTJ-GQFGMJRRSA-N 0.000 description 1
230000002503 metabolic effect Effects 0.000 description 1
239000002207 metabolite Substances 0.000 description 1
230000031864 metaphase Effects 0.000 description 1
208000021039 metastatic melanoma Diseases 0.000 description 1
DASQOOZCTWOQPA-GXKRWWSZSA-L methotrexate disodium Chemical compound [Na+].[Na+].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 DASQOOZCTWOQPA-GXKRWWSZSA-L 0.000 description 1
229960003058 methotrexate sodium Drugs 0.000 description 1
125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
239000002480 mineral oil Substances 0.000 description 1
235000010446 mineral oil Nutrition 0.000 description 1
239000003595 mist Substances 0.000 description 1
210000003470 mitochondria Anatomy 0.000 description 1
239000002829 mitogen activated protein kinase inhibitor Substances 0.000 description 1
230000004048 modification Effects 0.000 description 1
238000012986 modification Methods 0.000 description 1
238000012544 monitoring process Methods 0.000 description 1
150000004682 monohydrates Chemical class 0.000 description 1
229910052901 montmorillonite Inorganic materials 0.000 description 1
230000036457 multidrug resistance Effects 0.000 description 1
210000000663 muscle cell Anatomy 0.000 description 1
230000035772 mutation Effects 0.000 description 1
BLCLNMBMMGCOAS-UHFFFAOYSA-N n-[1-[[1-[[1-[[1-[[1-[[1-[[1-[2-[(carbamoylamino)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amin Chemical compound C1CCC(C(=O)NNC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(COC(C)(C)C)NC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 BLCLNMBMMGCOAS-UHFFFAOYSA-N 0.000 description 1
210000003739 neck Anatomy 0.000 description 1
230000001613 neoplastic effect Effects 0.000 description 1
231100000417 nephrotoxicity Toxicity 0.000 description 1
230000007694 nephrotoxicity Effects 0.000 description 1
230000000926 neurological effect Effects 0.000 description 1
229910052759 nickel Inorganic materials 0.000 description 1
229960002653 nilutamide Drugs 0.000 description 1
XWXYUMMDTVBTOU-UHFFFAOYSA-N nilutamide Chemical compound O=C1C(C)(C)NC(=O)N1C1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 XWXYUMMDTVBTOU-UHFFFAOYSA-N 0.000 description 1
LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 description 1
229940127082 non-receptor tyrosine kinase inhibitor Drugs 0.000 description 1
239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
230000000269 nucleophilic effect Effects 0.000 description 1
239000002773 nucleotide Substances 0.000 description 1
125000003729 nucleotide group Chemical group 0.000 description 1
ZWLPBLYKEWSWPD-UHFFFAOYSA-N o-toluic acid Chemical compound CC1=CC=CC=C1C(O)=O ZWLPBLYKEWSWPD-UHFFFAOYSA-N 0.000 description 1
QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
230000003287 optical effect Effects 0.000 description 1
238000003305 oral gavage Methods 0.000 description 1
150000002891 organic anions Chemical class 0.000 description 1
239000003960 organic solvent Substances 0.000 description 1
231100000262 ototoxicity Toxicity 0.000 description 1
210000001672 ovary Anatomy 0.000 description 1
230000002018 overexpression Effects 0.000 description 1
230000003647 oxidation Effects 0.000 description 1
238000007254 oxidation reaction Methods 0.000 description 1
230000004783 oxidative metabolism Effects 0.000 description 1
210000000496 pancreas Anatomy 0.000 description 1
201000002528 pancreatic cancer Diseases 0.000 description 1
208000008443 pancreatic carcinoma Diseases 0.000 description 1
JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 description 1
229960002340 pentostatin Drugs 0.000 description 1
FPVKHBSQESCIEP-JQCXWYLXSA-N pentostatin Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(N=CNC[C@H]2O)=C2N=C1 FPVKHBSQESCIEP-JQCXWYLXSA-N 0.000 description 1
229940124531 pharmaceutical excipient Drugs 0.000 description 1
239000000825 pharmaceutical preparation Substances 0.000 description 1
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
239000010452 phosphate Substances 0.000 description 1
NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
230000026731 phosphorylation Effects 0.000 description 1
238000006366 phosphorylation reaction Methods 0.000 description 1
239000003757 phosphotransferase inhibitor Substances 0.000 description 1
238000001782 photodegradation Methods 0.000 description 1
238000006303 photolysis reaction Methods 0.000 description 1
XNGIFLGASWRNHJ-UHFFFAOYSA-N phthalic acid Chemical class OC(=O)C1=CC=CC=C1C(O)=O XNGIFLGASWRNHJ-UHFFFAOYSA-N 0.000 description 1
230000000704 physical effect Effects 0.000 description 1
230000035790 physiological processes and functions Effects 0.000 description 1
230000036470 plasma concentration Effects 0.000 description 1
239000004033 plastic Substances 0.000 description 1
229920003023 plastic Polymers 0.000 description 1
150000003057 platinum Chemical class 0.000 description 1
231100000374 pneumotoxicity Toxicity 0.000 description 1
YVCVYCSAAZQOJI-UHFFFAOYSA-N podophyllotoxin Natural products COC1=C(O)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YVCVYCSAAZQOJI-UHFFFAOYSA-N 0.000 description 1
229920000058 polyacrylate Polymers 0.000 description 1
208000030761 polycystic kidney disease Diseases 0.000 description 1
239000001259 polydextrose Substances 0.000 description 1
235000013856 polydextrose Nutrition 0.000 description 1
229940035035 polydextrose Drugs 0.000 description 1
235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
229920001184 polypeptide Polymers 0.000 description 1
239000003910 polypeptide antibiotic agent Substances 0.000 description 1
229940068968 polysorbate 80 Drugs 0.000 description 1
229920000053 polysorbate 80 Polymers 0.000 description 1
229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
230000029279 positive regulation of transcription, DNA-dependent Effects 0.000 description 1
239000011591 potassium Substances 0.000 description 1
229910052700 potassium Inorganic materials 0.000 description 1
229920001592 potato starch Polymers 0.000 description 1
230000003389 potentiating effect Effects 0.000 description 1
239000002243 precursor Substances 0.000 description 1
102000004196 processed proteins & peptides Human genes 0.000 description 1
108090000765 processed proteins & peptides Proteins 0.000 description 1
239000000583 progesterone congener Substances 0.000 description 1
230000035755 proliferation Effects 0.000 description 1
BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
230000001681 protective effect Effects 0.000 description 1
230000017854 proteolysis Effects 0.000 description 1
230000002685 pulmonary effect Effects 0.000 description 1
239000008213 purified water Substances 0.000 description 1
230000006825 purine synthesis Effects 0.000 description 1
150000003212 purines Chemical class 0.000 description 1
230000006824 pyrimidine synthesis Effects 0.000 description 1
150000008512 pyrimidinediones Chemical class 0.000 description 1
150000003230 pyrimidines Chemical class 0.000 description 1
150000003254 radicals Chemical class 0.000 description 1
238000001959 radiotherapy Methods 0.000 description 1
229960004622 raloxifene Drugs 0.000 description 1
GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 description 1
238000011552 rat model Methods 0.000 description 1
108091006082 receptor inhibitors Proteins 0.000 description 1
238000011084 recovery Methods 0.000 description 1
206010038038 rectal cancer Diseases 0.000 description 1
210000000664 rectum Anatomy 0.000 description 1
201000001275 rectum cancer Diseases 0.000 description 1
230000022983 regulation of cell cycle Effects 0.000 description 1
230000008439 repair process Effects 0.000 description 1
201000009410 rhabdomyosarcoma Diseases 0.000 description 1
108091092562 ribozyme Proteins 0.000 description 1
238000005096 rolling process Methods 0.000 description 1
239000000523 sample Substances 0.000 description 1
238000009094 second-line therapy Methods 0.000 description 1
239000013049 sediment Substances 0.000 description 1
230000005783 single-strand break Effects 0.000 description 1
231100000438 skin toxicity Toxicity 0.000 description 1
208000000587 small cell lung carcinoma Diseases 0.000 description 1
239000011734 sodium Substances 0.000 description 1
229940083542 sodium Drugs 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
235000017557 sodium bicarbonate Nutrition 0.000 description 1
229920003109 sodium starch glycolate Polymers 0.000 description 1
239000008109 sodium starch glycolate Substances 0.000 description 1
229940079832 sodium starch glycolate Drugs 0.000 description 1
229940045902 sodium stearyl fumarate Drugs 0.000 description 1
229960002920 sorbitol Drugs 0.000 description 1
241000894007 species Species 0.000 description 1
238000005507 spraying Methods 0.000 description 1
206010041823 squamous cell carcinoma Diseases 0.000 description 1
229940032147 starch Drugs 0.000 description 1
239000008117 stearic acid Substances 0.000 description 1
210000002784 stomach Anatomy 0.000 description 1
239000000758 substrate Substances 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
229940124530 sulfonamide Drugs 0.000 description 1
150000003456 sulfonamides Chemical class 0.000 description 1
239000006188 syrup Substances 0.000 description 1
235000020357 syrup Nutrition 0.000 description 1
238000009492 tablet coating Methods 0.000 description 1
239000002700 tablet coating Substances 0.000 description 1
239000000454 talc Substances 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
229960001603 tamoxifen Drugs 0.000 description 1
239000011975 tartaric acid Substances 0.000 description 1
235000002906 tartaric acid Nutrition 0.000 description 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 description 1
150000004579 taxol derivatives Chemical class 0.000 description 1
150000003505 terpenes Chemical class 0.000 description 1
235000007586 terpenes Nutrition 0.000 description 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
229940044693 topoisomerase inhibitor Drugs 0.000 description 1
XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 description 1
229960005026 toremifene Drugs 0.000 description 1
231100000607 toxicokinetics Toxicity 0.000 description 1
102000035160 transmembrane proteins Human genes 0.000 description 1
108091005703 transmembrane proteins Proteins 0.000 description 1
230000032258 transport Effects 0.000 description 1
QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
230000004102 tricarboxylic acid cycle Effects 0.000 description 1
WEAPVABOECTMGR-UHFFFAOYSA-N triethyl 2-acetyloxypropane-1,2,3-tricarboxylate Chemical compound CCOC(=O)CC(C(=O)OCC)(OC(C)=O)CC(=O)OCC WEAPVABOECTMGR-UHFFFAOYSA-N 0.000 description 1
239000001069 triethyl citrate Substances 0.000 description 1
VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
235000013769 triethyl citrate Nutrition 0.000 description 1
230000004614 tumor growth Effects 0.000 description 1
229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
239000005483 tyrosine kinase inhibitor Substances 0.000 description 1
125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
230000003827 upregulation Effects 0.000 description 1
210000003932 urinary bladder Anatomy 0.000 description 1
201000005112 urinary bladder cancer Diseases 0.000 description 1
229960005486 vaccine Drugs 0.000 description 1
230000002792 vascular Effects 0.000 description 1
229960002166 vinorelbine tartrate Drugs 0.000 description 1
GBABOYUKABKIAF-IWWDSPBFSA-N vinorelbinetartrate Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC(C23[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-IWWDSPBFSA-N 0.000 description 1
239000003021 water soluble solvent Substances 0.000 description 1
239000001993 wax Substances 0.000 description 1
238000005550 wet granulation Methods 0.000 description 1
238000009736 wetting Methods 0.000 description 1
238000002424 x-ray crystallography Methods 0.000 description 1
229940093612 zein Drugs 0.000 description 1
239000005019 zein Substances 0.000 description 1
XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1