JP2016512832A5 - - Google Patents
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- JP2016512832A5 JP2016512832A5 JP2016501584A JP2016501584A JP2016512832A5 JP 2016512832 A5 JP2016512832 A5 JP 2016512832A5 JP 2016501584 A JP2016501584 A JP 2016501584A JP 2016501584 A JP2016501584 A JP 2016501584A JP 2016512832 A5 JP2016512832 A5 JP 2016512832A5
- Authority
- JP
- Japan
- Prior art keywords
- seq
- antibody
- drug conjugate
- chain variable
- variable region
- Prior art date
- 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.)
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- 239000000611 antibody drug conjugate Substances 0.000 claims description 70
- 229940049595 antibody-drug conjugate Drugs 0.000 claims description 70
- 239000003814 drug Substances 0.000 claims description 21
- 239000000427 antigen Substances 0.000 claims description 18
- 102000036639 antigens Human genes 0.000 claims description 18
- 108091007433 antigens Proteins 0.000 claims description 18
- 239000012634 fragment Substances 0.000 claims description 18
- 239000003112 inhibitor Substances 0.000 claims description 14
- 229940124597 therapeutic agent Drugs 0.000 claims description 12
- 150000001413 amino acids Chemical class 0.000 claims description 8
- 229940079593 drug Drugs 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- -1 2,5-dioxopyrrolidin-1-yl Chemical group 0.000 claims description 6
- VRDGQQTWSGDXCU-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 2-iodoacetate Chemical compound ICC(=O)ON1C(=O)CCC1=O VRDGQQTWSGDXCU-UHFFFAOYSA-N 0.000 claims description 4
- JWDFQMWEFLOOED-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 3-(pyridin-2-yldisulfanyl)propanoate Chemical group O=C1CCC(=O)N1OC(=O)CCSSC1=CC=CC=N1 JWDFQMWEFLOOED-UHFFFAOYSA-N 0.000 claims description 4
- JSHOVKSMJRQOGY-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 4-(pyridin-2-yldisulfanyl)butanoate Chemical compound O=C1CCC(=O)N1OC(=O)CCCSSC1=CC=CC=N1 JSHOVKSMJRQOGY-UHFFFAOYSA-N 0.000 claims description 4
- GTBCXYYVWHFQRS-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 4-(pyridin-2-yldisulfanyl)pentanoate Chemical compound C=1C=CC=NC=1SSC(C)CCC(=O)ON1C(=O)CCC1=O GTBCXYYVWHFQRS-UHFFFAOYSA-N 0.000 claims description 4
- BQWBEDSJTMWJAE-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 4-[(2-iodoacetyl)amino]benzoate Chemical compound C1=CC(NC(=O)CI)=CC=C1C(=O)ON1C(=O)CCC1=O BQWBEDSJTMWJAE-UHFFFAOYSA-N 0.000 claims description 4
- 108020004414 DNA Proteins 0.000 claims description 4
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims description 4
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims description 4
- 101710181812 Methionine aminopeptidase Proteins 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 239000003431 cross linking reagent Substances 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- FUHCFUVCWLZEDQ-UHFFFAOYSA-N 1-(2,5-dioxopyrrolidin-1-yl)oxy-1-oxo-4-(pyridin-2-yldisulfanyl)butane-2-sulfonic acid Chemical compound O=C1CCC(=O)N1OC(=O)C(S(=O)(=O)O)CCSSC1=CC=CC=N1 FUHCFUVCWLZEDQ-UHFFFAOYSA-N 0.000 claims description 2
- 229940121819 ATPase inhibitor Drugs 0.000 claims description 2
- 101100004408 Arabidopsis thaliana BIG gene Proteins 0.000 claims description 2
- 239000012664 BCL-2-inhibitor Substances 0.000 claims description 2
- 229940123711 Bcl2 inhibitor Drugs 0.000 claims description 2
- 108010047041 Complementarity Determining Regions Proteins 0.000 claims description 2
- 102000000578 Cyclin-Dependent Kinase Inhibitor p21 Human genes 0.000 claims description 2
- 108010016788 Cyclin-Dependent Kinase Inhibitor p21 Proteins 0.000 claims description 2
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 claims description 2
- 239000012624 DNA alkylating agent Substances 0.000 claims description 2
- 229940126161 DNA alkylating agent Drugs 0.000 claims description 2
- 239000012623 DNA damaging agent Substances 0.000 claims description 2
- 102100024746 Dihydrofolate reductase Human genes 0.000 claims description 2
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims description 2
- 101100485279 Drosophila melanogaster emb gene Proteins 0.000 claims description 2
- 102100029095 Exportin-1 Human genes 0.000 claims description 2
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 claims description 2
- 101001056180 Homo sapiens Induced myeloid leukemia cell differentiation protein Mcl-1 Proteins 0.000 claims description 2
- 101000684208 Homo sapiens Prolyl endopeptidase FAP Proteins 0.000 claims description 2
- 102100026539 Induced myeloid leukemia cell differentiation protein Mcl-1 Human genes 0.000 claims description 2
- 102100027670 Islet amyloid polypeptide Human genes 0.000 claims description 2
- 229940124179 Kinesin inhibitor Drugs 0.000 claims description 2
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 2
- 102000029749 Microtubule Human genes 0.000 claims description 2
- 108091022875 Microtubule Proteins 0.000 claims description 2
- 229940119336 Microtubule stabilizer Drugs 0.000 claims description 2
- 108091000080 Phosphotransferase Proteins 0.000 claims description 2
- 229940079156 Proteasome inhibitor Drugs 0.000 claims description 2
- 229940123573 Protein synthesis inhibitor Drugs 0.000 claims description 2
- 101100485284 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) CRM1 gene Proteins 0.000 claims description 2
- 101150094313 XPO1 gene Proteins 0.000 claims description 2
- 239000000362 adenosine triphosphatase inhibitor Substances 0.000 claims description 2
- 108010044540 auristatin Proteins 0.000 claims description 2
- 239000011230 binding agent Substances 0.000 claims description 2
- 108020001096 dihydrofolate reductase Proteins 0.000 claims description 2
- AMRJKAQTDDKMCE-UHFFFAOYSA-N dolastatin Chemical compound CC(C)C(N(C)C)C(=O)NC(C(C)C)C(=O)N(C)C(C(C)C)C(OC)CC(=O)N1CCCC1C(OC)C(C)C(=O)NC(C=1SC=CN=1)CC1=CC=CC=C1 AMRJKAQTDDKMCE-UHFFFAOYSA-N 0.000 claims description 2
- 229930188854 dolastatin Natural products 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 108700002148 exportin 1 Proteins 0.000 claims description 2
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims description 2
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims description 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 239000000138 intercalating agent Substances 0.000 claims description 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims description 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims description 2
- 210000004688 microtubule Anatomy 0.000 claims description 2
- 210000003470 mitochondria Anatomy 0.000 claims description 2
- 230000025308 nuclear transport Effects 0.000 claims description 2
- LFGREXWGYUGZLY-UHFFFAOYSA-N phosphoryl Chemical group [P]=O LFGREXWGYUGZLY-UHFFFAOYSA-N 0.000 claims description 2
- 102000020233 phosphotransferase Human genes 0.000 claims description 2
- 150000003141 primary amines Chemical class 0.000 claims description 2
- 230000000861 pro-apoptotic effect Effects 0.000 claims description 2
- 239000003207 proteasome inhibitor Substances 0.000 claims description 2
- 239000000007 protein synthesis inhibitor Substances 0.000 claims description 2
- 238000006276 transfer reaction Methods 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 description 4
- 201000011510 cancer Diseases 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 206010041067 Small cell lung cancer Diseases 0.000 description 3
- 208000000587 small cell lung carcinoma Diseases 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 2
- 239000000032 diagnostic agent Substances 0.000 description 2
- 229940039227 diagnostic agent Drugs 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 208000000516 mast-cell leukemia Diseases 0.000 description 2
- 108020004707 nucleic acids Proteins 0.000 description 2
- 102000039446 nucleic acids Human genes 0.000 description 2
- 150000007523 nucleic acids Chemical class 0.000 description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 208000009905 Neurofibromatoses Diseases 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- 229920001213 Polysorbate 20 Polymers 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000001268 conjugating effect Effects 0.000 description 1
- 238000012258 culturing Methods 0.000 description 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 description 1
- 239000012216 imaging agent Substances 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 208000008585 mastocytosis Diseases 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 229910021645 metal ion Inorganic materials 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 201000004931 neurofibromatosis Diseases 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 1
- 229940068977 polysorbate 20 Drugs 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 229940074404 sodium succinate Drugs 0.000 description 1
- ZDQYSKICYIVCPN-UHFFFAOYSA-L sodium succinate (anhydrous) Chemical compound [Na+].[Na+].[O-]C(=O)CCC([O-])=O ZDQYSKICYIVCPN-UHFFFAOYSA-L 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361793641P | 2013-03-15 | 2013-03-15 | |
| US61/793,641 | 2013-03-15 | ||
| PCT/US2014/024597 WO2014150937A1 (en) | 2013-03-15 | 2014-03-12 | Antibody drug conjugates |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018049209A Division JP6578400B2 (ja) | 2013-03-15 | 2018-03-16 | 抗体薬物コンジュゲート |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016512832A JP2016512832A (ja) | 2016-05-09 |
| JP2016512832A5 true JP2016512832A5 (enExample) | 2017-04-13 |
| JP6333943B2 JP6333943B2 (ja) | 2018-05-30 |
Family
ID=50721874
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501584A Expired - Fee Related JP6333943B2 (ja) | 2013-03-15 | 2014-03-12 | 抗体薬物コンジュゲート |
| JP2018049209A Expired - Fee Related JP6578400B2 (ja) | 2013-03-15 | 2018-03-16 | 抗体薬物コンジュゲート |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018049209A Expired - Fee Related JP6578400B2 (ja) | 2013-03-15 | 2018-03-16 | 抗体薬物コンジュゲート |
Country Status (26)
| Country | Link |
|---|---|
| US (6) | US9498543B2 (enExample) |
| EP (2) | EP2968590B1 (enExample) |
| JP (2) | JP6333943B2 (enExample) |
| KR (1) | KR20150131173A (enExample) |
| CN (1) | CN105007950B (enExample) |
| AP (1) | AP2015008656A0 (enExample) |
| AR (1) | AR095666A1 (enExample) |
| AU (1) | AU2014235474B2 (enExample) |
| BR (1) | BR112015021134A2 (enExample) |
| CA (1) | CA2903772A1 (enExample) |
| CL (1) | CL2015002246A1 (enExample) |
| CR (1) | CR20150488A (enExample) |
| CU (1) | CU20150128A7 (enExample) |
| EA (1) | EA035253B1 (enExample) |
| ES (1) | ES2701051T3 (enExample) |
| IL (1) | IL241277A0 (enExample) |
| MA (1) | MA38396B1 (enExample) |
| MX (1) | MX366978B (enExample) |
| NZ (1) | NZ710929A (enExample) |
| PH (1) | PH12015501902A1 (enExample) |
| SG (1) | SG11201506395RA (enExample) |
| TN (1) | TN2015000396A1 (enExample) |
| TW (1) | TW201446806A (enExample) |
| UY (1) | UY35490A (enExample) |
| WO (1) | WO2014150937A1 (enExample) |
| ZA (1) | ZA201505656B (enExample) |
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- 2014-03-12 WO PCT/US2014/024597 patent/WO2014150937A1/en not_active Ceased
- 2014-03-12 KR KR1020157028519A patent/KR20150131173A/ko not_active Ceased
- 2014-03-12 CN CN201480013720.XA patent/CN105007950B/zh not_active Expired - Fee Related
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