JP2011516587A5 - - Google Patents

Info

Publication number

JP2011516587A5

JP2011516587A5 JP2011504298A JP2011504298A JP2011516587A5 JP 2011516587 A5 JP2011516587 A5 JP 2011516587A5 JP 2011504298 A JP2011504298 A JP 2011504298A JP 2011504298 A JP2011504298 A JP 2011504298A JP 2011516587 A5 JP2011516587 A5 JP 2011516587A5

Authority

JP

Japan

Prior art keywords

composition

mixture

agent

solubilizer

seq

Prior art date

2009-04-20

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.)

Granted

Links

• Espacenet
• Global Dossier
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• IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 69
• 238000000034 method Methods 0.000 claims description 45
• 239000002904 solvent Substances 0.000 claims description 23
• 239000006172 buffering agent Substances 0.000 claims description 20
• KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 18
• 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 18
• 229920001184 polypeptide Polymers 0.000 claims description 16
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 16
• 239000004067 bulking agent Substances 0.000 claims description 15
• 239000003814 drug Substances 0.000 claims description 14
• 108090000765 processed proteins & peptides Proteins 0.000 claims description 14
• 102000004196 processed proteins & peptides Human genes 0.000 claims description 14
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical group [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 12
• 238000004108 freeze drying Methods 0.000 claims description 12
• JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 12
• 125000003275 alpha amino acid group Chemical group 0.000 claims description 11
• -1 polyoxyethylene Polymers 0.000 claims description 11
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 10
• 229930195725 Mannitol Natural products 0.000 claims description 10
• 229930012538 Paclitaxel Natural products 0.000 claims description 10
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• 206010028980 Neoplasm Diseases 0.000 claims description 8
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• 239000004615 ingredient Substances 0.000 claims description 8
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• 108010064942 Angiopep-2 Proteins 0.000 claims description 7
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• 239000004471 Glycine Substances 0.000 claims description 6
• DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Natural products NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 6
• 239000000872 buffer Substances 0.000 claims description 6
• GBVKRUOMSUTVPW-AHNVSIPUSA-N chembl1089636 Chemical group N([C@H]([C@@H](OC(=O)CCC(=O)N[C@@H](C(O)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCCNC(=O)CCC(=O)O[C@H]([C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)C(=O)O[C@@H]1C(=C2[C@@H](OC(C)=O)C(=O)[C@]3(C)[C@@H](O)C[C@H]4OC[C@]4([C@H]3[C@H](OC(=O)C=3C=CC=CC=3)[C@](C2(C)C)(O)C1)OC(C)=O)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCCNC(=O)CCC(=O)O[C@H]([C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)C(=O)O[C@@H]1C(=C2[C@@H](OC(C)=O)C(=O)[C@]3(C)[C@@H](O)C[C@H]4OC[C@]4([C@H]3[C@H](OC(=O)C=3C=CC=CC=3)[C@](C2(C)C)(O)C1)OC(C)=O)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(O)=O)C(=O)O[C@@H]1C(=C2[C@@H](OC(C)=O)C(=O)[C@]3(C)[C@@H](O)C[C@H]4OC[C@]4([C@H]3[C@H](OC(=O)C=3C=CC=CC=3)[C@](C2(C)C)(O)C1)OC(C)=O)C)C=1C=CC=CC=1)C(=O)C1=CC=CC=C1 GBVKRUOMSUTVPW-AHNVSIPUSA-N 0.000 claims description 6
• 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims description 6
• 239000007951 isotonicity adjuster Substances 0.000 claims description 6
• 239000004310 lactic acid Substances 0.000 claims description 6
• 235000014655 lactic acid Nutrition 0.000 claims description 6
• 108010046239 paclitaxel-Angiopep-2 conjugate Proteins 0.000 claims description 6
• 239000011780 sodium chloride Substances 0.000 claims description 6
• 229940124597 therapeutic agent Drugs 0.000 claims description 6
• 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 5
• 235000014113 dietary fatty acids Nutrition 0.000 claims description 5
• 150000002148 esters Chemical class 0.000 claims description 5
• 229930195729 fatty acid Natural products 0.000 claims description 5
• 239000000194 fatty acid Substances 0.000 claims description 5
• 150000004665 fatty acids Chemical class 0.000 claims description 5
• 230000002209 hydrophobic effect Effects 0.000 claims description 5
• 239000012929 tonicity agent Substances 0.000 claims description 5
• 208000003174 Brain Neoplasms Diseases 0.000 claims description 4
• 238000001035 drying Methods 0.000 claims description 4
• 206010003571 Astrocytoma Diseases 0.000 claims description 2
• 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
• 206010014967 Ependymoma Diseases 0.000 claims description 2
• 208000032612 Glial tumor Diseases 0.000 claims description 2
• 206010018338 Glioma Diseases 0.000 claims description 2
• 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
• 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
• 208000000172 Medulloblastoma Diseases 0.000 claims description 2
• 206010033128 Ovarian cancer Diseases 0.000 claims description 2
• 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
• 206010038389 Renal cancer Diseases 0.000 claims description 2
• 208000000277 Splenic Neoplasms Diseases 0.000 claims description 2
• 210000004556 brain Anatomy 0.000 claims description 2
• 238000004090 dissolution Methods 0.000 claims description 2
• 238000007710 freezing Methods 0.000 claims description 2
• 230000008014 freezing Effects 0.000 claims description 2
• 208000005017 glioblastoma Diseases 0.000 claims description 2
• 201000010982 kidney cancer Diseases 0.000 claims description 2
• 210000004185 liver Anatomy 0.000 claims description 2
• 201000007270 liver cancer Diseases 0.000 claims description 2
• 208000014018 liver neoplasm Diseases 0.000 claims description 2
• 210000004072 lung Anatomy 0.000 claims description 2
• 201000005202 lung cancer Diseases 0.000 claims description 2
• 208000020816 lung neoplasm Diseases 0.000 claims description 2
• 238000004519 manufacturing process Methods 0.000 claims description 2
• 230000002611 ovarian Effects 0.000 claims description 2
• 150000003839 salts Chemical class 0.000 claims description 2
• 239000000600 sorbitol Substances 0.000 claims description 2
• 210000000952 spleen Anatomy 0.000 claims description 2
• 201000002471 spleen cancer Diseases 0.000 claims description 2
• 239000002202 Polyethylene glycol Substances 0.000 claims 6
• 229920001577 copolymer Polymers 0.000 claims 6
• 229920001223 polyethylene glycol Polymers 0.000 claims 6
• 239000004359 castor oil Substances 0.000 claims 3
• 235000019438 castor oil Nutrition 0.000 claims 3
• 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 3
• 238000001914 filtration Methods 0.000 claims 1
• 210000002418 meninge Anatomy 0.000 claims 1
• JVKUCNQGESRUCL-UHFFFAOYSA-N 2-Hydroxyethyl 12-hydroxyoctadecanoate Chemical group CCCCCCC(O)CCCCCCCCCCC(=O)OCCO JVKUCNQGESRUCL-UHFFFAOYSA-N 0.000 description 6
• 229920001304 Solutol HS 15 Polymers 0.000 description 6
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
• 239000003795 chemical substances by application Substances 0.000 description 2
• 238000009472 formulation Methods 0.000 description 2
• 239000008389 polyethoxylated castor oil Substances 0.000 description 2
• 239000000243 solution Substances 0.000 description 2
• PZNPLUBHRSSFHT-RRHRGVEJSA-N 1-hexadecanoyl-2-octadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[C@@H](COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCCCCCCCCCC PZNPLUBHRSSFHT-RRHRGVEJSA-N 0.000 description 1
• RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical group CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 1
• 238000010790 dilution Methods 0.000 description 1
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• 206010027191 meningioma Diseases 0.000 description 1
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• 230000000717 retained effect Effects 0.000 description 1
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• 238000005063 solubilization Methods 0.000 description 1
• 239000008347 soybean phospholipid Substances 0.000 description 1