JP2018528185A5 - - Google Patents

Info

Publication number

JP2018528185A5

JP2018528185A5 JP2018506600A JP2018506600A JP2018528185A5 JP 2018528185 A5 JP2018528185 A5 JP 2018528185A5 JP 2018506600 A JP2018506600 A JP 2018506600A JP 2018506600 A JP2018506600 A JP 2018506600A JP 2018528185 A5 JP2018528185 A5 JP 2018528185A5

Authority

JP

Japan

Prior art keywords

leucovorin

oxaliplatin

fluorouracil

liposomal irinotecan

irinotecan

Prior art date

2016-08-19

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

Withdrawn

Links

• Espacenet
• Global Dossier
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• UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims description 72
• 229960004768 irinotecan Drugs 0.000 claims description 71
• 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 50
• 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 50
• 235000008191 folinic acid Nutrition 0.000 claims description 50
• 239000011672 folinic acid Substances 0.000 claims description 50
• 229960001691 leucovorin Drugs 0.000 claims description 50
• 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 45
• 229960001756 oxaliplatin Drugs 0.000 claims description 45
• GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 42
• 229960002949 fluorouracil Drugs 0.000 claims description 42
• 230000001394 metastastic effect Effects 0.000 claims description 41
• 206010061289 metastatic neoplasm Diseases 0.000 claims description 41
• 206010052747 Adenocarcinoma pancreas Diseases 0.000 claims description 35
• 201000002094 pancreatic adenocarcinoma Diseases 0.000 claims description 35
• 238000002560 therapeutic procedure Methods 0.000 claims description 28
• 230000000259 anti-tumor effect Effects 0.000 claims description 21
• 238000002512 chemotherapy Methods 0.000 claims description 13
• HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](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 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims description 10
• 239000002502 liposome Substances 0.000 claims description 9
• 238000001802 infusion Methods 0.000 claims description 6
• NRJAVPSFFCBXDT-HUESYALOSA-N 1,2-distearoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCCCC NRJAVPSFFCBXDT-HUESYALOSA-N 0.000 claims description 5
• 235000012000 cholesterol Nutrition 0.000 claims description 5
• WEPNHBQBLCNOBB-FZJVNAOYSA-N sucrose octasulfate Chemical compound OS(=O)(=O)O[C@@H]1[C@H](OS(O)(=O)=O)[C@H](COS(=O)(=O)O)O[C@]1(COS(O)(=O)=O)O[C@@H]1[C@H](OS(O)(=O)=O)[C@@H](OS(O)(=O)=O)[C@@H](OS(O)(=O)=O)[C@@H](COS(O)(=O)=O)O1 WEPNHBQBLCNOBB-FZJVNAOYSA-N 0.000 claims description 5
• 206010061902 Pancreatic neoplasm Diseases 0.000 claims 6
• 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 6
• 201000002528 pancreatic cancer Diseases 0.000 claims 6
• 208000008443 pancreatic carcinoma Diseases 0.000 claims 6
• 239000000232 Lipid Bilayer Substances 0.000 claims 2
• 239000002202 Polyethylene glycol Substances 0.000 claims 2
• UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 2
• 229960003957 dexamethasone Drugs 0.000 claims 2
• 229960005277 gemcitabine Drugs 0.000 claims 2
• 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 2
• 229920001223 polyethylene glycol Polymers 0.000 claims 2
• 239000003369 serotonin 5-HT3 receptor antagonist Substances 0.000 claims 2
• 239000002356 single layer Substances 0.000 claims 2
• 230000003474 anti-emetic effect Effects 0.000 claims 1
• 239000002111 antiemetic agent Substances 0.000 claims 1
• 229940078646 other antiemetics in atc Drugs 0.000 claims 1
• KLEAIHJJLUAXIQ-JDRGBKBRSA-N irinotecan hydrochloride hydrate Chemical compound O.O.O.Cl.C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 KLEAIHJJLUAXIQ-JDRGBKBRSA-N 0.000 description 4
• 229950010538 irinotecan hydrochloride trihydrate Drugs 0.000 description 4
• 229940048191 onivyde Drugs 0.000 description 4
• 239000007858 starting material Substances 0.000 description 4
• 239000012467 final product Substances 0.000 description 2
• QHARDGMPGYZGKH-YCUNKVRLSA-N (19S)-10,19-diethyl-19-hydroxy-7-(1-piperidin-4-ylpiperidin-2-yl)-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaene-14,18-dione Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1C1CCCCN1C1CCNCC1 QHARDGMPGYZGKH-YCUNKVRLSA-N 0.000 description 1
• 229920002505 N-(Carbonyl-Methoxypolyethylene Glycol 2000)-1,2-Distearoyl-Sn-Glycero-3-Phosphoethanolamine Polymers 0.000 description 1
• 229960000779 irinotecan hydrochloride Drugs 0.000 description 1
• GURKHSYORGJETM-WAQYZQTGSA-N irinotecan hydrochloride (anhydrous) Chemical compound Cl.C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 GURKHSYORGJETM-WAQYZQTGSA-N 0.000 description 1
• 239000000047 product Substances 0.000 description 1
• SRLOHQKOADWDBV-NRONOFSHSA-M sodium;[(2r)-2,3-di(octadecanoyloxy)propyl] 2-(2-methoxyethoxycarbonylamino)ethyl phosphate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCCNC(=O)OCCOC)OC(=O)CCCCCCCCCCCCCCCCC SRLOHQKOADWDBV-NRONOFSHSA-M 0.000 description 1
• 239000000126 substance Substances 0.000 description 1