JP2016519670A5 - - Google Patents

Info

Publication number

JP2016519670A5

JP2016519670A5 JP2016502963A JP2016502963A JP2016519670A5 JP 2016519670 A5 JP2016519670 A5 JP 2016519670A5 JP 2016502963 A JP2016502963 A JP 2016502963A JP 2016502963 A JP2016502963 A JP 2016502963A JP 2016519670 A5 JP2016519670 A5 JP 2016519670A5

Authority

JP

Japan

Prior art keywords

polysorbate

pharmaceutical composition

polypeptide

factor

item

Prior art date

2014-03-14

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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• HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims description 154
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 152
• 239000008194 pharmaceutical composition Substances 0.000 claims description 145
• 229920001184 polypeptide Polymers 0.000 claims description 113
• 108090000765 processed proteins & peptides Proteins 0.000 claims description 113
• 102000004196 processed proteins & peptides Human genes 0.000 claims description 113
• 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 claims description 83
• 229930006000 Sucrose Natural products 0.000 claims description 83
• 239000005720 sucrose Substances 0.000 claims description 83
• 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 82
• 229930195725 Mannitol Natural products 0.000 claims description 82
• 239000000594 mannitol Substances 0.000 claims description 82
• 235000010355 mannitol Nutrition 0.000 claims description 82
• 229920001213 Polysorbate 20 Polymers 0.000 claims description 78
• 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims description 78
• 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims description 78
• 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 78
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 78
• 229940068977 polysorbate 20 Drugs 0.000 claims description 78
• 229920000053 polysorbate 80 Polymers 0.000 claims description 78
• 229940068968 polysorbate 80 Drugs 0.000 claims description 78
• 229960002885 histidine Drugs 0.000 claims description 77
• 239000011780 sodium chloride Substances 0.000 claims description 76
• 102100022641 Coagulation factor IX Human genes 0.000 claims description 59
• 108010076282 Factor IX Proteins 0.000 claims description 45
• 229960004222 factor ix Drugs 0.000 claims description 45
• 239000008176 lyophilized powder Substances 0.000 claims description 40
• 208000032843 Hemorrhage Diseases 0.000 claims description 24
• 208000034158 bleeding Diseases 0.000 claims description 24
• 230000000740 bleeding effect Effects 0.000 claims description 24
• 239000000843 powder Substances 0.000 claims description 19
• 208000009429 hemophilia B Diseases 0.000 claims description 14
• 150000001413 amino acids Chemical group 0.000 claims description 12
• 230000000694 effects Effects 0.000 claims description 10
• 229940024606 amino acid Drugs 0.000 claims description 8
• 102100026120 IgG receptor FcRn large subunit p51 Human genes 0.000 claims description 7
• 101710177940 IgG receptor FcRn large subunit p51 Proteins 0.000 claims description 7
• 108700007283 factor IX Fc fusion Proteins 0.000 claims description 6
• 230000002265 prevention Effects 0.000 claims description 5
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 4
• 229960000027 human factor ix Drugs 0.000 claims description 4
• 239000011521 glass Substances 0.000 claims description 3
• 239000000203 mixture Substances 0.000 claims description 3
• 150000001720 carbohydrates Chemical class 0.000 claims description 2
• 239000000725 suspension Substances 0.000 claims description 2
• 239000007787 solid Substances 0.000 claims 2
• 208000024891 symptom Diseases 0.000 claims 2
• 239000003085 diluting agent Substances 0.000 claims 1
• FBPFZTCFMRRESA-UHFFFAOYSA-N hexane-1,2,3,4,5,6-hexol Chemical compound OCC(O)C(O)C(O)C(O)CO FBPFZTCFMRRESA-UHFFFAOYSA-N 0.000 claims 1
• 238000000034 method Methods 0.000 description 45
• 238000001802 infusion Methods 0.000 description 7
• WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical group OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 6
• 229940031422 benefix Drugs 0.000 description 6
• 238000001990 intravenous administration Methods 0.000 description 6
• 239000003755 preservative agent Substances 0.000 description 5
• 230000002335 preservative effect Effects 0.000 description 5
• 238000001356 surgical procedure Methods 0.000 description 5
• 206010051077 Post procedural haemorrhage Diseases 0.000 description 4
• ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 2
• 230000000845 anti-microbial effect Effects 0.000 description 2
• 235000019445 benzyl alcohol Nutrition 0.000 description 2
• OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 2
• RLSSMJSEOOYNOY-UHFFFAOYSA-N m-cresol Chemical compound CC1=CC=CC(O)=C1 RLSSMJSEOOYNOY-UHFFFAOYSA-N 0.000 description 2
• LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
• QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
• QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 description 1
• 239000002253 acid Substances 0.000 description 1
• 239000003795 chemical substances by application Substances 0.000 description 1
• 229960004926 chlorobutanol Drugs 0.000 description 1
• 230000009977 dual effect Effects 0.000 description 1
• 239000007788 liquid Substances 0.000 description 1
• 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
• 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
• 229960002216 methylparaben Drugs 0.000 description 1
• 239000008177 pharmaceutical agent Substances 0.000 description 1
• 229960005323 phenoxyethanol Drugs 0.000 description 1
• WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
• 230000000069 prophylactic effect Effects 0.000 description 1
• 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
• 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
• 229960003415 propylparaben Drugs 0.000 description 1