CA2693057A1 - Formulations orales pour du picoplatine - Google Patents

Info

Publication number

CA2693057A1

CA2693057A1 CA 2693057 CA2693057A CA2693057A1 CA 2693057 A1 CA2693057 A1 CA 2693057A1 CA 2693057 CA2693057 CA 2693057 CA 2693057 A CA2693057 A CA 2693057A CA 2693057 A1 CA2693057 A1 CA 2693057A1

Authority

CA

Canada

Prior art keywords

picoplatin

formulation

cancer

oil

combination

Prior art date

2007-07-16

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.)

Abandoned

Links

• Espacenet
• Global Dossier
• CIPO
• Discuss

• 229950005566 picoplatin Drugs 0.000 title claims abstract description 399
• IIMIOEBMYPRQGU-UHFFFAOYSA-L picoplatin Chemical compound N.[Cl-].[Cl-].[Pt+2].CC1=CC=CC=N1 IIMIOEBMYPRQGU-UHFFFAOYSA-L 0.000 title claims abstract description 377
• 239000000203 mixture Substances 0.000 title claims abstract description 200
• 238000009472 formulation Methods 0.000 title claims abstract description 152
• 238000000034 method Methods 0.000 claims abstract description 92
• 239000003921 oil Substances 0.000 claims abstract description 61
• 239000000725 suspension Substances 0.000 claims abstract description 44
• 239000002246 antineoplastic agent Substances 0.000 claims abstract description 37
• 238000002360 preparation method Methods 0.000 claims abstract description 20
• 239000007962 solid dispersion Substances 0.000 claims abstract description 18
• 239000002245 particle Substances 0.000 claims description 67
• 235000019198 oils Nutrition 0.000 claims description 60
• 239000002904 solvent Substances 0.000 claims description 56
• 229920001223 polyethylene glycol Polymers 0.000 claims description 51
• 239000002105 nanoparticle Substances 0.000 claims description 44
• 206010028980 Neoplasm Diseases 0.000 claims description 43
• 239000002202 Polyethylene glycol Substances 0.000 claims description 43
• 239000000787 lecithin Substances 0.000 claims description 43
• 235000010445 lecithin Nutrition 0.000 claims description 43
• 239000007787 solid Substances 0.000 claims description 43
• IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 42
• 229940067606 lecithin Drugs 0.000 claims description 42
• IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 39
• 239000002609 medium Substances 0.000 claims description 33
• 239000011159 matrix material Substances 0.000 claims description 30
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• 239000003112 inhibitor Substances 0.000 claims description 26
• 102000011632 Caseins Human genes 0.000 claims description 21
• 108010076119 Caseins Proteins 0.000 claims description 21
• 239000004094 surface-active agent Substances 0.000 claims description 21
• UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims description 21
• 239000003995 emulsifying agent Substances 0.000 claims description 20
• 238000002156 mixing Methods 0.000 claims description 19
• 150000002194 fatty esters Chemical class 0.000 claims description 18
• RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 16
• 239000007788 liquid Substances 0.000 claims description 16
• WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims description 13
• 206010041067 Small cell lung cancer Diseases 0.000 claims description 12
• 239000000155 melt Substances 0.000 claims description 12
• 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 12
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 12
• 229940068968 polysorbate 80 Drugs 0.000 claims description 12
• 229920000053 polysorbate 80 Polymers 0.000 claims description 12
• 208000000587 small cell lung carcinoma Diseases 0.000 claims description 12
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 11
• AOBORMOPSGHCAX-UHFFFAOYSA-N Tocophersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-UHFFFAOYSA-N 0.000 claims description 11
• 239000012736 aqueous medium Substances 0.000 claims description 11
• 239000005018 casein Substances 0.000 claims description 11
• BECPQYXYKAMYBN-UHFFFAOYSA-N casein, tech. Chemical compound NCCCCC(C(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(CC(C)C)N=C(O)C(CCC(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(C(C)O)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(COP(O)(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(N)CC1=CC=CC=C1 BECPQYXYKAMYBN-UHFFFAOYSA-N 0.000 claims description 11
• 235000021240 caseins Nutrition 0.000 claims description 11
• 239000012943 hotmelt Substances 0.000 claims description 11
• DMBUODUULYCPAK-UHFFFAOYSA-N 1,3-bis(docosanoyloxy)propan-2-yl docosanoate Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCCCCCC DMBUODUULYCPAK-UHFFFAOYSA-N 0.000 claims description 10
• 206010014733 Endometrial cancer Diseases 0.000 claims description 10
• 206010014759 Endometrial neoplasm Diseases 0.000 claims description 10
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• 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 10
• 206010038389 Renal cancer Diseases 0.000 claims description 10
• 239000000010 aprotic solvent Substances 0.000 claims description 10
• 229940071162 caseinate Drugs 0.000 claims description 10
• 230000002496 gastric effect Effects 0.000 claims description 10
• 201000010982 kidney cancer Diseases 0.000 claims description 10
• 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 10
• 230000005855 radiation Effects 0.000 claims description 10
• 229940080237 sodium caseinate Drugs 0.000 claims description 10
• UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims description 10
• 238000011282 treatment Methods 0.000 claims description 10
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• 239000000843 powder Substances 0.000 claims 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 claims description 8
• 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims description 8
• 230000000340 anti-metabolite Effects 0.000 claims description 8
• 229940100197 antimetabolite Drugs 0.000 claims description 8
• 239000002256 antimetabolite Substances 0.000 claims description 8
• 239000003381 stabilizer Substances 0.000 claims description 8
• 239000006228 supernatant Substances 0.000 claims description 8
• LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 claims description 7
• HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims description 7
• 229940100198 alkylating agent Drugs 0.000 claims description 7
• 239000002168 alkylating agent Substances 0.000 claims description 7
• 239000004359 castor oil Substances 0.000 claims description 7
• 235000019438 castor oil Nutrition 0.000 claims description 7
• 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 description 7
• 230000008569 process Effects 0.000 claims description 7
• 229960000303 topotecan Drugs 0.000 claims description 7
• JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims description 6
• 102000009465 Growth Factor Receptors Human genes 0.000 claims description 6
• 108010009202 Growth Factor Receptors Proteins 0.000 claims description 6
• 239000002147 L01XE04 - Sunitinib Substances 0.000 claims description 6
• 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 6
• 206010033128 Ovarian cancer Diseases 0.000 claims description 6
• 206010061535 Ovarian neoplasm Diseases 0.000 claims description 6
• 206010060862 Prostate cancer Diseases 0.000 claims description 6
• 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
• 229940123237 Taxane Drugs 0.000 claims description 6
• 239000002775 capsule Substances 0.000 claims description 6
• 150000001720 carbohydrates Chemical class 0.000 claims description 6
• 239000003102 growth factor Substances 0.000 claims description 6
• 229940043355 kinase inhibitor Drugs 0.000 claims description 6
• 239000000314 lubricant Substances 0.000 claims description 6
• 201000005202 lung cancer Diseases 0.000 claims description 6
• 208000020816 lung neoplasm Diseases 0.000 claims description 6
• YJGVMLPVUAXIQN-XVVDYKMHSA-N podophyllotoxin Chemical class COC1=C(OC)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@H](O)[C@@H]3[C@@H]2C(OC3)=O)=C1 YJGVMLPVUAXIQN-XVVDYKMHSA-N 0.000 claims description 6
• 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 claims description 6
• 239000003549 soybean oil Substances 0.000 claims description 6
• 235000012424 soybean oil Nutrition 0.000 claims description 6
• DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims description 6
• 206010005003 Bladder cancer Diseases 0.000 claims description 5
• 206010006187 Breast cancer Diseases 0.000 claims description 5
• 208000026310 Breast neoplasm Diseases 0.000 claims description 5
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• 208000007766 Kaposi sarcoma Diseases 0.000 claims description 5
• 206010025323 Lymphomas Diseases 0.000 claims description 5
• 206010027406 Mesothelioma Diseases 0.000 claims description 5
• 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 5
• 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 5
• 229920002690 Polyoxyl 40 HydrogenatedCastorOil Polymers 0.000 claims description 5
• 206010039491 Sarcoma Diseases 0.000 claims description 5
• 208000024313 Testicular Neoplasms Diseases 0.000 claims description 5
• 206010057644 Testis cancer Diseases 0.000 claims description 5
• 208000000728 Thymus Neoplasms Diseases 0.000 claims description 5
• 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 5
• 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 5
• 208000002495 Uterine Neoplasms Diseases 0.000 claims description 5
• 229940122803 Vinca alkaloid Drugs 0.000 claims description 5
• 210000000988 bone and bone Anatomy 0.000 claims description 5
• 208000002458 carcinoid tumor Diseases 0.000 claims description 5
• 201000010881 cervical cancer Diseases 0.000 claims description 5
• GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims description 5
• AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 5
• 201000004101 esophageal cancer Diseases 0.000 claims description 5
• 238000004108 freeze drying Methods 0.000 claims description 5
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• 201000007270 liver cancer Diseases 0.000 claims description 5
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• 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 5
• 201000001441 melanoma Diseases 0.000 claims description 5
• 208000014761 nasopharyngeal type undifferentiated carcinoma Diseases 0.000 claims description 5
• WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims description 5
• 201000002528 pancreatic cancer Diseases 0.000 claims description 5
• 208000008443 pancreatic carcinoma Diseases 0.000 claims description 5
• 239000008389 polyethoxylated castor oil Substances 0.000 claims description 5
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• 201000003120 testicular cancer Diseases 0.000 claims description 5
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• 235000019483 Peanut oil Nutrition 0.000 claims description 4
• 229960002550 amrubicin Drugs 0.000 claims description 4
• VJZITPJGSQKZMX-XDPRQOKASA-N amrubicin Chemical compound O([C@H]1C[C@](CC2=C(O)C=3C(=O)C4=CC=CC=C4C(=O)C=3C(O)=C21)(N)C(=O)C)[C@H]1C[C@H](O)[C@H](O)CO1 VJZITPJGSQKZMX-XDPRQOKASA-N 0.000 claims description 4
• 229960000397 bevacizumab Drugs 0.000 claims description 4
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• YMNCVRSYJBNGLD-KURKYZTESA-N cephalotaxine Chemical class C([C@@]12C=C([C@H]([C@H]2C2=C3)O)OC)CCN1CCC2=CC1=C3OCO1 YMNCVRSYJBNGLD-KURKYZTESA-N 0.000 claims description 4
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• RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 4
• 229960002066 vinorelbine Drugs 0.000 claims description 4
• 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 3
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• 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 3
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