JP2010523469A5 - - Google Patents
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- JP2010523469A5 JP2010523469A5 JP2009534901A JP2009534901A JP2010523469A5 JP 2010523469 A5 JP2010523469 A5 JP 2010523469A5 JP 2009534901 A JP2009534901 A JP 2009534901A JP 2009534901 A JP2009534901 A JP 2009534901A JP 2010523469 A5 JP2010523469 A5 JP 2010523469A5
- Authority
- JP
- Japan
- Prior art keywords
- antibody
- amino acid
- immunoconjugate
- seq
- acid sequence
- 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.)
- Granted
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- 229940127121 immunoconjugate Drugs 0.000 claims 25
- 125000003275 alpha amino acid group Chemical group 0.000 claims 22
- 235000018417 cysteine Nutrition 0.000 claims 14
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 14
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 13
- 239000000611 antibody drug conjugate Substances 0.000 claims 12
- 229940049595 antibody-drug conjugate Drugs 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 229940079593 drug Drugs 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 9
- 229940127089 cytotoxic agent Drugs 0.000 claims 8
- 238000000034 method Methods 0.000 claims 7
- -1 6-maleimidocaproyl Chemical group 0.000 claims 6
- 125000005647 linker group Chemical group 0.000 claims 6
- JJAHTWIKCUJRDK-UHFFFAOYSA-N succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate Chemical compound C1CC(CN2C(C=CC2=O)=O)CCC1C(=O)ON1C(=O)CCC1=O JJAHTWIKCUJRDK-UHFFFAOYSA-N 0.000 claims 5
- 239000002246 antineoplastic agent Substances 0.000 claims 4
- 239000002254 cytotoxic agent Substances 0.000 claims 4
- 231100000599 cytotoxic agent Toxicity 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 230000002062 proliferating effect Effects 0.000 claims 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 3
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 3
- 239000012472 biological sample Substances 0.000 claims 3
- 125000004452 carbocyclyl group Chemical group 0.000 claims 3
- 229960002173 citrulline Drugs 0.000 claims 3
- AGGWFDNPHKLBBV-YUMQZZPRSA-N (2s)-2-[[(2s)-2-amino-3-methylbutanoyl]amino]-5-(carbamoylamino)pentanoic acid Chemical compound CC(C)[C@H](N)C(=O)N[C@H](C(O)=O)CCCNC(N)=O AGGWFDNPHKLBBV-YUMQZZPRSA-N 0.000 claims 2
- 108090000790 Enzymes Proteins 0.000 claims 2
- 102000004190 Enzymes Human genes 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Chemical compound CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 2
- 235000001014 amino acid Nutrition 0.000 claims 2
- 239000003242 anti bacterial agent Substances 0.000 claims 2
- 229940088710 antibiotic agent Drugs 0.000 claims 2
- 108010044540 auristatin Proteins 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 210000001072 colon Anatomy 0.000 claims 2
- 239000000562 conjugate Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 230000001293 nucleolytic effect Effects 0.000 claims 2
- 229960001592 paclitaxel Drugs 0.000 claims 2
- 210000002307 prostate Anatomy 0.000 claims 2
- 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 2
- 239000003053 toxin Substances 0.000 claims 2
- 231100000765 toxin Toxicity 0.000 claims 2
- 108700012359 toxins Proteins 0.000 claims 2
- 210000003932 urinary bladder Anatomy 0.000 claims 2
- 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 1
- DJQYYYCQOZMCRC-UHFFFAOYSA-N 2-aminopropane-1,3-dithiol Chemical compound SCC(N)CS DJQYYYCQOZMCRC-UHFFFAOYSA-N 0.000 claims 1
- VVIAGPKUTFNRDU-UHFFFAOYSA-N 6S-folinic acid Natural products C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-UHFFFAOYSA-N 0.000 claims 1
- OMNVYXHOSHNURL-WPRPVWTQSA-N Ala-Phe Chemical compound C[C@H](N)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 OMNVYXHOSHNURL-WPRPVWTQSA-N 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 1
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 1
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical group NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- IEDXPSOJFSVCKU-HOKPPMCLSA-N [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrolidin-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate Chemical compound CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)CCC2=O)C(C)C)cc1)C(C)C IEDXPSOJFSVCKU-HOKPPMCLSA-N 0.000 claims 1
- 108010011559 alanylphenylalanine Proteins 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 229960004050 aminobenzoic acid Drugs 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 201000011281 bladder sarcoma Diseases 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 190000008236 carboplatin Chemical compound 0.000 claims 1
- 230000022534 cell killing Effects 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 235000013477 citrulline Nutrition 0.000 claims 1
- 201000002660 colon sarcoma Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 238000001514 detection method Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229960002949 fluorouracil Drugs 0.000 claims 1
- VVIAGPKUTFNRDU-ABLWVSNPSA-N folinic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-ABLWVSNPSA-N 0.000 claims 1
- 235000008191 folinic acid Nutrition 0.000 claims 1
- 239000011672 folinic acid Substances 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 229960004891 lapatinib Drugs 0.000 claims 1
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims 1
- 229960003881 letrozole Drugs 0.000 claims 1
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical group C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims 1
- 229960001691 leucovorin Drugs 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000003866 lung sarcoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000002611 ovarian Effects 0.000 claims 1
- 208000011932 ovarian sarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 201000008079 ovary sarcoma Diseases 0.000 claims 1
- 229960001756 oxaliplatin Drugs 0.000 claims 1
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 201000002025 prostate sarcoma Diseases 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 125000006850 spacer group Chemical group 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
- 0 CC[C@](C)[C@](CN(C)C([C@@](*C([C@](C(C)C)N(C)C)=O)C(C)C)=O)[C@@](CC(N(CCC1)[C@@]1[C@@](C(C(NC([C@](c1ccccc1)O)=C)=O)=C)OC)=O)OC Chemical compound CC[C@](C)[C@](CN(C)C([C@@](*C([C@](C(C)C)N(C)C)=O)C(C)C)=O)[C@@](CC(N(CCC1)[C@@]1[C@@](C(C(NC([C@](c1ccccc1)O)=C)=O)=C)OC)=O)OC 0.000 description 3
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92130007P | 2007-03-30 | 2007-03-30 | |
| US60/921,300 | 2007-03-30 | ||
| US93785707P | 2007-06-29 | 2007-06-29 | |
| US60/937,857 | 2007-06-29 | ||
| PCT/US2007/082726 WO2008052187A2 (en) | 2006-10-27 | 2007-10-26 | Antibodies and immunoconjugates and uses therefor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013217609A Division JP5837019B2 (ja) | 2007-03-30 | 2013-10-18 | 抗体及びイムノコンジュゲートとこれらの使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010523469A JP2010523469A (ja) | 2010-07-15 |
| JP2010523469A5 true JP2010523469A5 (enExample) | 2010-12-16 |
| JP5394246B2 JP5394246B2 (ja) | 2014-01-22 |
Family
ID=42575819
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009534901A Active JP5394246B2 (ja) | 2007-03-30 | 2007-10-26 | 抗体及びイムノコンジュゲートとこれらの使用方法 |
| JP2013217609A Active JP5837019B2 (ja) | 2007-03-30 | 2013-10-18 | 抗体及びイムノコンジュゲートとこれらの使用方法 |
| JP2015217734A Active JP6185540B2 (ja) | 2007-03-30 | 2015-11-05 | 抗体及びイムノコンジュゲートとこれらの使用方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013217609A Active JP5837019B2 (ja) | 2007-03-30 | 2013-10-18 | 抗体及びイムノコンジュゲートとこれらの使用方法 |
| JP2015217734A Active JP6185540B2 (ja) | 2007-03-30 | 2015-11-05 | 抗体及びイムノコンジュゲートとこれらの使用方法 |
Country Status (1)
| Country | Link |
|---|---|
| JP (3) | JP5394246B2 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5990947A (ja) * | 1982-11-16 | 1984-05-25 | Matsushita Electronics Corp | 半導体装置 |
| ES2874306T3 (es) | 2010-09-29 | 2021-11-04 | Agensys Inc | Conjugados de anticuerpos y fármacos (CAF) que se unen a las proteínas 191P4D12 |
| EP2621508B1 (de) * | 2010-09-29 | 2015-08-26 | Seattle Genetics, Inc. | N-carboxyalkyl-auristatine und ihre verwendung |
| US8772457B2 (en) * | 2010-11-10 | 2014-07-08 | Genentech, Inc. | BACE1 antibodies |
| AU2012235817B2 (en) * | 2011-04-01 | 2016-03-10 | Wyeth Llc | Antibody-drug conjugates |
| HUE053589T2 (hu) | 2011-11-17 | 2021-07-28 | Pfizer | Citotoxikus peptidek és azok antitest-hatóanyag konjugátumai |
| AR089028A1 (es) * | 2011-11-29 | 2014-07-23 | Genentech Inc | Composiciones y metodos para el analisis de cancer de prostata |
| HK1206386A1 (en) * | 2012-04-04 | 2016-01-08 | Perseus Proteomics Inc. | Conjugate of anti-cdh3 (p-cadherin) antibody and drug |
| CN112587671A (zh) * | 2012-07-18 | 2021-04-02 | 博笛生物科技有限公司 | 癌症的靶向免疫治疗 |
| MY183572A (en) * | 2013-03-15 | 2021-02-26 | Regeneron Pharma | Biologically active molecules, conjugates thereof, and therapeutic uses |
| CA2936375A1 (en) * | 2014-01-10 | 2015-07-16 | Shanghai Birdie Biotech, Inc. | Compounds and compositions for treating her2 positive tumors |
| JP2017505305A (ja) * | 2014-01-24 | 2017-02-16 | ジェネンテック, インコーポレイテッド | 抗steap1抗体及びイムノコンジュゲートを使用する方法 |
| TWI684600B (zh) * | 2014-03-21 | 2020-02-11 | 美商艾伯維有限公司 | 抗-egfr抗體及抗體藥物結合物 |
| MX2017001022A (es) | 2014-07-24 | 2017-12-20 | Genentech Inc | Metodos para conjugar un agente a un resto tiol en una proteina que contiene al menos un enlace trisulfuro. |
| CN107949574A (zh) * | 2015-10-02 | 2018-04-20 | 豪夫迈·罗氏有限公司 | 双特异性t细胞活化性抗原结合分子 |
| SG11202013138RA (en) * | 2018-07-02 | 2021-01-28 | Amgen Inc | Anti-steap1 antigen-binding protein |
| KR20210100671A (ko) | 2018-12-03 | 2021-08-17 | 어젠시스 인코포레이티드 | 항-191p4d12 항체 약물 컨쥬게이트를 포함하는 약제학적 조성물 및 이의 사용 방법 |
| CA3166732A1 (en) * | 2020-01-22 | 2021-07-29 | Medimmune Limited | Compounds and conjugates thereof |
| CN111494645B (zh) * | 2020-05-20 | 2022-09-30 | 中国药科大学 | 抗人dll4人源化抗体与美登素生物碱dm1的偶联物及其制备方法与应用 |
| TW202313121A (zh) * | 2021-05-24 | 2023-04-01 | 中國大陸商榮昌生物製藥(煙臺)股份有限公司 | Her2靶向抗體-藥物結合物用於治療her2-低表現乳癌之用途 |
| WO2023000131A1 (zh) * | 2021-07-19 | 2023-01-26 | 烟台迈百瑞国际生物医药股份有限公司 | 一种负载双毒素的抗体药物偶联物及其应用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU775366B2 (en) * | 1999-12-06 | 2004-07-29 | Agensys, Inc. | Serpentine transmembrane antigens expressed in human cancers and uses thereof |
| CN101258166B (zh) * | 2004-04-22 | 2013-01-30 | 阿根西斯公司 | 与steap-1蛋白结合的抗体及其衍生的分子 |
| SI1791565T1 (sl) * | 2004-09-23 | 2016-08-31 | Genentech, Inc. | Cisteinsko konstruirana protitelesa in konjugati |
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2007
- 2007-10-26 JP JP2009534901A patent/JP5394246B2/ja active Active
-
2013
- 2013-10-18 JP JP2013217609A patent/JP5837019B2/ja active Active
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2015
- 2015-11-05 JP JP2015217734A patent/JP6185540B2/ja active Active