JP2015519382A5 - - Google Patents

Info

Publication number

JP2015519382A5

JP2015519382A5 JP2015516595A JP2015516595A JP2015519382A5 JP 2015519382 A5 JP2015519382 A5 JP 2015519382A5 JP 2015516595 A JP2015516595 A JP 2015516595A JP 2015516595 A JP2015516595 A JP 2015516595A JP 2015519382 A5 JP2015519382 A5 JP 2015519382A5

Authority

JP

Japan

Prior art keywords

antibody

pharmaceutical composition

concentration

composition according

fragment

Prior art date

2013-06-12

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
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• 239000008194 pharmaceutical composition Substances 0.000 claims 23
• 239000000203 mixture Substances 0.000 claims 17
• QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 9
• 239000012634 fragment Substances 0.000 claims 9
• HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims 6
• 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 6
• 229930195725 Mannitol Natural products 0.000 claims 6
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 6
• HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims 6
• HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims 6
• 238000002347 injection Methods 0.000 claims 6
• 239000007924 injection Substances 0.000 claims 6
• 239000000594 mannitol Substances 0.000 claims 6
• 235000010355 mannitol Nutrition 0.000 claims 6
• 239000004475 Arginine Substances 0.000 claims 4
• ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 4
• 238000012781 high pressure - size exclusion chromatography Methods 0.000 claims 4
• HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 4
• 238000007920 subcutaneous administration Methods 0.000 claims 4
• 230000001225 therapeutic effect Effects 0.000 claims 4
• GHCZTIFQWKKGSB-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;phosphoric acid Chemical compound OP(O)(O)=O.OC(=O)CC(O)(C(O)=O)CC(O)=O GHCZTIFQWKKGSB-UHFFFAOYSA-N 0.000 claims 3
• QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 3
• 239000008363 phosphate buffer Substances 0.000 claims 3
• 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 3
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 3
• 229920000053 polysorbate 80 Polymers 0.000 claims 3
• 229940068968 polysorbate 80 Drugs 0.000 claims 3
• 239000011780 sodium chloride Substances 0.000 claims 3
• 235000002639 sodium chloride Nutrition 0.000 claims 3
• KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 3
• 208000023275 Autoimmune disease Diseases 0.000 claims 2
• 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 2
• 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 2
• 206010028980 Neoplasm Diseases 0.000 claims 2
• 229960002964 adalimumab Drugs 0.000 claims 2
• 238000004220 aggregation Methods 0.000 claims 2
• 230000002776 aggregation Effects 0.000 claims 2
• 230000027455 binding Effects 0.000 claims 2
• 239000000872 buffer Substances 0.000 claims 2
• 201000011510 cancer Diseases 0.000 claims 2
• 229960003115 certolizumab pegol Drugs 0.000 claims 2
• 229960001743 golimumab Drugs 0.000 claims 2
• 229960000598 infliximab Drugs 0.000 claims 2
• 238000007918 intramuscular administration Methods 0.000 claims 2
• UYEUUXMDVNYCAM-UHFFFAOYSA-N lumazine Chemical compound N1=CC=NC2=NC(O)=NC(O)=C21 UYEUUXMDVNYCAM-UHFFFAOYSA-N 0.000 claims 2
• 230000036210 malignancy Effects 0.000 claims 2
• 238000000034 method Methods 0.000 claims 2
• NMWKYTGJWUAZPZ-WWHBDHEGSA-N (4S)-4-[[(4R,7S,10S,16S,19S,25S,28S,31R)-31-[[(2S)-2-[[(1R,6R,9S,12S,18S,21S,24S,27S,30S,33S,36S,39S,42R,47R,53S,56S,59S,62S,65S,68S,71S,76S,79S,85S)-47-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-oxobutanoyl]amino]-3-carboxypropanoyl]amino]-18-(4-aminobutyl)-27,68-bis(3-amino-3-oxopropyl)-36,71,76-tribenzyl-39-(3-carbamimidamidopropyl)-24-(2-carboxyethyl)-21,56-bis(carboxymethyl)-65,85-bis[(1R)-1-hydroxyethyl]-59-(hydroxymethyl)-62,79-bis(1H-imidazol-4-ylmethyl)-9-methyl-33-(2-methylpropyl)-8,11,17,20,23,26,29,32,35,38,41,48,54,57,60,63,66,69,72,74,77,80,83,86-tetracosaoxo-30-propan-2-yl-3,4,44,45-tetrathia-7,10,16,19,22,25,28,31,34,37,40,49,55,58,61,64,67,70,73,75,78,81,84,87-tetracosazatetracyclo[40.31.14.012,16.049,53]heptaoctacontane-6-carbonyl]amino]-3-methylbutanoyl]amino]-7-(3-carbamimidamidopropyl)-25-(hydroxymethyl)-19-[(4-hydroxyphenyl)methyl]-28-(1H-imidazol-4-ylmethyl)-10-methyl-6,9,12,15,18,21,24,27,30-nonaoxo-16-propan-2-yl-1,2-dithia-5,8,11,14,17,20,23,26,29-nonazacyclodotriacontane-4-carbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-3-carboxy-1-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid Chemical compound CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc4c[nH]cn4)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H]4CCCN4C(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc4c[nH]cn4)NC(=O)[C@H](Cc4ccccc4)NC3=O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)C(C)C)[C@@H](C)O)C(C)C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1)C(=O)N[C@@H](C)C(O)=O NMWKYTGJWUAZPZ-WWHBDHEGSA-N 0.000 claims 1
• KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
• 101000917858 Homo sapiens Low affinity immunoglobulin gamma Fc region receptor III-A Proteins 0.000 claims 1
• 101000917839 Homo sapiens Low affinity immunoglobulin gamma Fc region receptor III-B Proteins 0.000 claims 1
• ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 1
• HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 1
• 102100029185 Low affinity immunoglobulin gamma Fc region receptor III-B Human genes 0.000 claims 1
• 229910019142 PO4 Inorganic materials 0.000 claims 1
• 102000006747 Transforming Growth Factor alpha Human genes 0.000 claims 1
• 101800004564 Transforming growth factor alpha Proteins 0.000 claims 1
• 239000008351 acetate buffer Substances 0.000 claims 1
• 239000012062 aqueous buffer Substances 0.000 claims 1
• 229940090047 auto-injector Drugs 0.000 claims 1
• 230000015572 biosynthetic process Effects 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 238000013467 fragmentation Methods 0.000 claims 1
• 238000006062 fragmentation reaction Methods 0.000 claims 1
• 239000011859 microparticle Substances 0.000 claims 1
• 239000000178 monomer Substances 0.000 claims 1
• 238000004848 nephelometry Methods 0.000 claims 1
• NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
• 239000010452 phosphate Substances 0.000 claims 1
• 229920001184 polypeptide Polymers 0.000 claims 1
• 229940071643 prefilled syringe Drugs 0.000 claims 1
• 102000004196 processed proteins & peptides Human genes 0.000 claims 1
• 108090000765 processed proteins & peptides Proteins 0.000 claims 1
• 239000000243 solution Substances 0.000 claims 1
• 239000008362 succinate buffer Substances 0.000 claims 1
• 239000004094 surface-active agent Substances 0.000 claims 1
• 229940126622 therapeutic monoclonal antibody Drugs 0.000 claims 1
• 238000011179 visual inspection Methods 0.000 claims 1