JP2016511637A5 - - Google Patents
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- JP2016511637A5 JP2016511637A5 JP2015557139A JP2015557139A JP2016511637A5 JP 2016511637 A5 JP2016511637 A5 JP 2016511637A5 JP 2015557139 A JP2015557139 A JP 2015557139A JP 2015557139 A JP2015557139 A JP 2015557139A JP 2016511637 A5 JP2016511637 A5 JP 2016511637A5
- Authority
- JP
- Japan
- Prior art keywords
- antibody
- positions
- light chain
- heavy chain
- immunoconjugate
- 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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- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims description 91
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims description 91
- 229940127121 immunoconjugate Drugs 0.000 claims description 66
- 238000006467 substitution reaction Methods 0.000 claims description 45
- 235000018417 cysteine Nutrition 0.000 claims description 39
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims description 35
- 235000001014 amino acid Nutrition 0.000 claims description 27
- 150000001413 amino acids Chemical class 0.000 claims description 26
- 229940079593 drug Drugs 0.000 claims description 19
- 239000003814 drug Substances 0.000 claims description 19
- NFGXHKASABOEEW-UHFFFAOYSA-N 1-methylethyl 11-methoxy-3,7,11-trimethyl-2,4-dodecadienoate Chemical compound COC(C)(C)CCCC(C)CC=CC(C)=CC(=O)OC(C)C NFGXHKASABOEEW-UHFFFAOYSA-N 0.000 claims description 9
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 7
- 210000004027 cell Anatomy 0.000 claims description 7
- 229910052717 sulfur Inorganic materials 0.000 claims description 7
- 239000011593 sulfur Substances 0.000 claims description 7
- 108020004707 nucleic acids Proteins 0.000 claims description 4
- 102000039446 nucleic acids Human genes 0.000 claims description 4
- 150000007523 nucleic acids Chemical class 0.000 claims description 4
- 239000002458 cell surface marker Substances 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 239000012624 DNA alkylating agent Substances 0.000 claims description 2
- 229940123237 Taxane Drugs 0.000 claims description 2
- 102000004243 Tubulin Human genes 0.000 claims description 2
- 108090000704 Tubulin Proteins 0.000 claims description 2
- 229940045799 anthracyclines and related substance Drugs 0.000 claims description 2
- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
- 239000002254 cytotoxic agent Substances 0.000 claims description 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims description 2
- VQNATVDKACXKTF-XELLLNAOSA-N duocarmycin Chemical class COC1=C(OC)C(OC)=C2NC(C(=O)N3C4=CC(=O)C5=C([C@@]64C[C@@H]6C3)C=C(N5)C(=O)OC)=CC2=C1 VQNATVDKACXKTF-XELLLNAOSA-N 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 241000182341 Cubitermes group Species 0.000 claims 1
- 101150029707 ERBB2 gene Proteins 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 22
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 description 9
- 229960000575 trastuzumab Drugs 0.000 description 7
- 241000699670 Mus sp. Species 0.000 description 5
- 238000001727 in vivo Methods 0.000 description 5
- 150000001945 cysteines Chemical class 0.000 description 4
- 230000021615 conjugation Effects 0.000 description 3
- 238000002844 melting Methods 0.000 description 3
- 230000008018 melting Effects 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 2
- 125000003275 alpha amino acid group Chemical group 0.000 description 2
- 239000000427 antigen Substances 0.000 description 2
- 239000012634 fragment Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- LGNCNVVZCUVPOT-FUVGGWJZSA-N (2s)-2-[[(2r,3r)-3-[(2s)-1-[(3r,4s,5s)-4-[[(2s)-2-[[(2s)-2-(dimethylamino)-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl]-3-methoxy-2-methylpropanoyl]amino]-3-phenylpropanoic acid Chemical compound CC(C)[C@H](N(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 LGNCNVVZCUVPOT-FUVGGWJZSA-N 0.000 description 1
- 229940126161 DNA alkylating agent Drugs 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241001024304 Mino Species 0.000 description 1
- 241000699660 Mus musculus Species 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 102000036639 antigens Human genes 0.000 description 1
- 108091007433 antigens Proteins 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229940041181 antineoplastic drug Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 235000015220 hamburgers Nutrition 0.000 description 1
- 238000003018 immunoassay Methods 0.000 description 1
- 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 238000011580 nude mouse model Methods 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 238000010405 reoxidation reaction Methods 0.000 description 1
- 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 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361762563P | 2013-02-08 | 2013-02-08 | |
| US61/762,563 | 2013-02-08 | ||
| PCT/US2014/015393 WO2014124316A2 (en) | 2013-02-08 | 2014-02-07 | Specific sites for modifying antibodies to make immunoconjugates |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016511637A JP2016511637A (ja) | 2016-04-21 |
| JP2016511637A5 true JP2016511637A5 (https=) | 2017-03-16 |
| JP6609477B2 JP6609477B2 (ja) | 2019-11-20 |
Family
ID=50179939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015557139A Active JP6609477B2 (ja) | 2013-02-08 | 2014-02-07 | イムノコンジュゲートを調製する修飾抗体のための特定部位 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US20160067351A1 (https=) |
| EP (2) | EP2953976B1 (https=) |
| JP (1) | JP6609477B2 (https=) |
| KR (3) | KR20150115000A (https=) |
| CN (2) | CN115925957A (https=) |
| AU (2) | AU2014214751B2 (https=) |
| BR (1) | BR112015018899B1 (https=) |
| CA (1) | CA2900755C (https=) |
| DK (1) | DK2953976T3 (https=) |
| EA (1) | EA201591465A1 (https=) |
| ES (1) | ES2874493T3 (https=) |
| HU (1) | HUE054443T2 (https=) |
| IL (1) | IL240406B (https=) |
| MX (2) | MX2015010146A (https=) |
| PL (1) | PL2953976T3 (https=) |
| PT (1) | PT2953976T (https=) |
| SG (2) | SG10201706468RA (https=) |
| SI (1) | SI2953976T1 (https=) |
| WO (1) | WO2014124316A2 (https=) |
Families Citing this family (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015502397A (ja) | 2011-12-23 | 2015-01-22 | ファイザー・インク | 部位特異的コンジュゲーションのための操作された抗体定常領域、ならびにそのための方法および使用 |
| US9089614B2 (en) | 2012-12-21 | 2015-07-28 | Bioalliance C.V. | Hydrophilic self-immolative linkers and conjugates thereof |
| EP2953976B1 (en) | 2013-02-08 | 2021-03-24 | Novartis Ag | Specific sites for modifying antibodies to make immunoconjugates |
| SG11201601424PA (en) | 2013-08-28 | 2016-03-30 | Stemcentrx Inc | Site-specific antibody conjugation methods and compositions |
| RU2016122041A (ru) | 2013-11-06 | 2017-12-11 | ЭББВИ СТЕМСЕНТРКС ЭлЭлСи | Новые анти-клаудин антитела и способы их применения |
| SG11201604664PA (en) | 2013-12-12 | 2016-07-28 | Stemcentrx Inc | Novel anti-dpep3 antibodies and methods of use |
| JP6636925B2 (ja) | 2013-12-17 | 2020-01-29 | ノバルティス アーゲー | 細胞障害性ペプチドおよびその抱合体 |
| CA2939941A1 (en) | 2014-02-21 | 2015-08-27 | Abbvie Stemcentrx Llc | Anti-dll3 antibodies and drug conjugates for use in melanoma |
| JP2017509337A (ja) * | 2014-03-12 | 2017-04-06 | ノバルティス アーゲー | イムノコンジュゲートを作製する抗体を修飾するための特定部位 |
| JP6685924B2 (ja) | 2014-04-11 | 2020-04-22 | メディミューン，エルエルシー | システイン操作抗体を含むコンジュゲート化合物 |
| SG11201609372UA (en) | 2014-05-22 | 2016-12-29 | Synthon Biopharmaceuticals Bv | Site-specific conjugation of linker drugs to antibodies and resulting adcs |
| US9950077B2 (en) * | 2014-06-20 | 2018-04-24 | Bioalliance C.V. | Anti-folate receptor alpha (FRA) antibody-drug conjugates and methods of using thereof |
| SG11201610624WA (en) * | 2014-06-20 | 2017-01-27 | Bioalliance Cv | Anti-cd22 antibody-drug conjugates and methods of using thereof |
| AU2015277100A1 (en) * | 2014-06-20 | 2017-02-02 | Abgenomics International Inc. | HER2 antibody-drug conjugates |
| TW201617368A (zh) | 2014-09-05 | 2016-05-16 | 史坦森特瑞斯公司 | 新穎抗ｍｆｉ２抗體及使用方法 |
| SG11201701128YA (en) * | 2014-09-12 | 2017-03-30 | Genentech Inc | Cysteine engineered antibodies and conjugates |
| AU2015366284B2 (en) | 2014-12-19 | 2021-07-22 | Ablynx N.V. | Cysteine linked nanobody dimers |
| EP4592311A3 (en) * | 2015-02-16 | 2026-02-25 | Lonza Ltd | Antibodies |
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