JP2018516964A5 - - Google Patents

Info

Publication number

JP2018516964A5

JP2018516964A5 JP2017564126A JP2017564126A JP2018516964A5 JP 2018516964 A5 JP2018516964 A5 JP 2018516964A5 JP 2017564126 A JP2017564126 A JP 2017564126A JP 2017564126 A JP2017564126 A JP 2017564126A JP 2018516964 A5 JP2018516964 A5 JP 2018516964A5

Authority

JP

Japan

Prior art keywords

nanodispersion

treatment

administered

nanodisperse

bleomycin

Prior art date

2016-06-08

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

Pending

Links

• Espacenet
• Global Dossier
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• 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
• -1 bevacizumab Chemical compound 0.000 claims description 10
• 229960000397 bevacizumab Drugs 0.000 claims description 9
• 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 8
• 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 8
• 229960004117 capecitabine Drugs 0.000 claims description 8
• 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 8
• 229960005277 gemcitabine Drugs 0.000 claims description 8
• 108010006654 Bleomycin Proteins 0.000 claims description 7
• 239000002246 antineoplastic agent Substances 0.000 claims description 7
• 229960001561 bleomycin Drugs 0.000 claims description 7
• OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims description 7
• 210000002603 extrahepatic bile duct Anatomy 0.000 claims description 7
• 210000003228 intrahepatic bile duct Anatomy 0.000 claims description 7
• 230000001394 metastastic effect Effects 0.000 claims description 7
• 206010061289 metastatic neoplasm Diseases 0.000 claims description 7
• 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
• GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 6
• 229930192392 Mitomycin Natural products 0.000 claims description 6
• NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims description 6
• 229960005395 cetuximab Drugs 0.000 claims description 6
• DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 6
• 229960004316 cisplatin Drugs 0.000 claims description 6
• 229960004679 doxorubicin Drugs 0.000 claims description 6
• 229960002949 fluorouracil Drugs 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
• 229960001691 leucovorin Drugs 0.000 claims description 6
• 229960004857 mitomycin Drugs 0.000 claims description 6
• 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 6
• 229960001756 oxaliplatin Drugs 0.000 claims description 6
• 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 6
• 229960005079 pemetrexed Drugs 0.000 claims description 6
• LKJPYSCBVHEWIU-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide Chemical compound C=1C=C(C#N)C(C(F)(F)F)=CC=1NC(=O)C(O)(C)CS(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-UHFFFAOYSA-N 0.000 claims description 5
• 229960004562 carboplatin Drugs 0.000 claims description 5
• 229940097647 casodex Drugs 0.000 claims description 5
• 229960005420 etoposide Drugs 0.000 claims description 5
• 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 5
• 239000002146 L01XE16 - Crizotinib Substances 0.000 claims description 4
• 229960005061 crizotinib Drugs 0.000 claims description 4
• KTEIFNKAUNYNJU-GFCCVEGCSA-N crizotinib Chemical compound O([C@H](C)C=1C(=C(F)C=CC=1Cl)Cl)C(C(=NC=1)N)=CC=1C(=C1)C=NN1C1CCNCC1 KTEIFNKAUNYNJU-GFCCVEGCSA-N 0.000 claims description 4
• 230000000750 progressive effect Effects 0.000 claims description 4
• 201000009030 Carcinoma Diseases 0.000 claims description 3
• 229930012538 Paclitaxel Natural products 0.000 claims description 3
• 210000000232 gallbladder Anatomy 0.000 claims description 3
• 229960001592 paclitaxel Drugs 0.000 claims description 3
• 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 3
• 239000003246 corticosteroid Substances 0.000 claims description 2
• 229960001334 corticosteroids Drugs 0.000 claims description 2
• 238000001990 intravenous administration Methods 0.000 claims description 2
• 238000009101 premedication Methods 0.000 claims description 2
• 239000002904 solvent Substances 0.000 claims description 2
• 239000004094 surface-active agent Substances 0.000 claims description 2
• 229920003169 water-soluble polymer Polymers 0.000 claims description 2
• 150000003839 salts Chemical class 0.000 claims 4
• 239000006185 dispersion Substances 0.000 claims 3
• 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 claims 2
• 239000007788 liquid Substances 0.000 claims 2
• 239000000203 mixture Substances 0.000 claims 2
• 239000002245 particle Substances 0.000 claims 2
• 102000004169 proteins and genes Human genes 0.000 claims 2
• 108090000623 proteins and genes Proteins 0.000 claims 2
• KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 1
• 102000009027 Albumins Human genes 0.000 claims 1
• 108010088751 Albumins Proteins 0.000 claims 1
• HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 1
• 239000002138 L01XE21 - Regorafenib Substances 0.000 claims 1
• 108010020346 Polyglutamic Acid Proteins 0.000 claims 1
• 239000002253 acid Substances 0.000 claims 1
• 229940042992 afinitor Drugs 0.000 claims 1
• 150000001298 alcohols Chemical class 0.000 claims 1
• 239000004359 castor oil Substances 0.000 claims 1
• 235000019438 castor oil Nutrition 0.000 claims 1
• BHYOQNUELFTYRT-DPAQBDIFSA-N cholesterol sulfate Chemical compound C1C=C2C[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 BHYOQNUELFTYRT-DPAQBDIFSA-N 0.000 claims 1
• 229940080277 cholesteryl sulfate Drugs 0.000 claims 1
• ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 1
• 229920002674 hyaluronan Polymers 0.000 claims 1
• 229960003160 hyaluronic acid Drugs 0.000 claims 1
• 229920001223 polyethylene glycol Polymers 0.000 claims 1
• 229920002643 polyglutamic acid Polymers 0.000 claims 1
• 229920001451 polypropylene glycol Polymers 0.000 claims 1
• 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
• 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
• 229960004836 regorafenib Drugs 0.000 claims 1
• ZOPOQLDXFHBOIH-UHFFFAOYSA-N regorafenib hydrate Chemical compound O.C1=NC(C(=O)NC)=CC(OC=2C=C(F)C(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 ZOPOQLDXFHBOIH-UHFFFAOYSA-N 0.000 claims 1
• 150000003467 sulfuric acid derivatives Chemical class 0.000 claims 1
• 235000021419 vinegar Nutrition 0.000 claims 1
• 239000000052 vinegar Substances 0.000 claims 1
• 239000002147 L01XE04 - Sunitinib Substances 0.000 description 3
• 190000008236 carboplatin Chemical compound 0.000 description 3
• 238000002512 chemotherapy Methods 0.000 description 3
• 238000000034 method Methods 0.000 description 3
• 229960001796 sunitinib Drugs 0.000 description 3
• WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 description 3
• 206010028980 Neoplasm Diseases 0.000 description 2
• 210000000941 bile Anatomy 0.000 description 2
• 201000008819 extrahepatic bile duct carcinoma Diseases 0.000 description 2
• 201000010175 gallbladder cancer Diseases 0.000 description 2
• 201000007487 gallbladder carcinoma Diseases 0.000 description 2
• 206010004593 Bile duct cancer Diseases 0.000 description 1
• 206010006187 Breast cancer Diseases 0.000 description 1
• 208000026310 Breast neoplasm Diseases 0.000 description 1
• 108010000817 Leuprolide Proteins 0.000 description 1
• 239000012736 aqueous medium Substances 0.000 description 1
• 208000026900 bile duct neoplasm Diseases 0.000 description 1
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• 238000007865 diluting Methods 0.000 description 1
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• RGLRXNKKBLIBQS-XNHQSDQCSA-N leuprolide acetate Chemical compound CC(O)=O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](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)CC1=CC=C(O)C=C1 RGLRXNKKBLIBQS-XNHQSDQCSA-N 0.000 description 1
• 229940087857 lupron Drugs 0.000 description 1