JP2010523469A5 - - Google Patents
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- Publication number
- 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
Links
- 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 |
| HUE038908T2 (hu) | 2010-09-29 | 2018-12-28 | Agensys Inc | 191P4D12 proteinekhez kötõdõ antitest-gyógyszerkonjugátumok (ADC) |
| WO2012041805A1 (de) * | 2010-09-29 | 2012-04-05 | Bayer Pharma Aktiengesellschaft | N-carboxyalkyl-auristatine und ihre verwendung |
| CN103228674B (zh) * | 2010-11-10 | 2019-07-05 | 霍夫曼-拉罗奇有限公司 | 用于神经疾病免疫疗法的方法和组合物 |
| MY170719A (en) * | 2011-04-01 | 2019-08-27 | Wyeth Llc | Antibody-drug conjugates |
| SI2780039T1 (en) | 2011-11-17 | 2018-06-29 | Pfizer Inc. | Cytotoxic peptides and their conjugates between the antibody and the drug |
| EP2786151B1 (en) * | 2011-11-29 | 2019-07-03 | F.Hoffmann-La Roche Ag | Methods for prostate cancer analysis |
| HK1206386A1 (en) * | 2012-04-04 | 2016-01-08 | Perseus Proteomics Inc. | Conjugate of anti-cdh3 (p-cadherin) antibody and drug |
| CN112587658A (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 |
| MA38496B2 (fr) * | 2013-03-15 | 2021-01-29 | Regeneron Pharma | Molécules biologiquement actives, leurs conjugués, et utilisations thérapeutiques |
| AU2015205753A1 (en) * | 2014-01-10 | 2016-07-21 | Birdie Biopharmaceuticals Inc. | Compounds and compositions for treating HER2 positive tumors |
| MX2016009515A (es) * | 2014-01-24 | 2016-10-26 | Genentech Inc | Metodos para utilizar anticuerpos anti-steap1 e inmunoconjugados. |
| CA2942101A1 (en) * | 2014-03-21 | 2015-09-24 | Abbvie Inc. | Anti-egfr antibodies and antibody drug conjugates |
| AU2015294389B2 (en) | 2014-07-24 | 2021-04-29 | Genentech, Inc. | Methods of conjugating an agent to a thiol moiety in a protein that contains at least one trisulfide bond |
| US20170096495A1 (en) * | 2015-10-02 | 2017-04-06 | Hoffmann-La Roche Inc. | Bispecific t cell activating antigen binding molecules |
| PE20211091A1 (es) * | 2018-07-02 | 2021-06-14 | Amgen Inc | Proteina de union al antigeno anti-steap1 |
| IL283522B2 (en) | 2018-12-03 | 2025-03-01 | Agensys Inc | Pharmaceutical compositions containing anti-191P4D12 antibody drug conjugates and methods of using them |
| EP4093439A1 (en) * | 2020-01-22 | 2022-11-30 | 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 |
| CN117750980A (zh) * | 2021-05-24 | 2024-03-22 | 荣昌生物制药(烟台)股份有限公司 | Her2靶向抗体-药物偶联物用于治疗her2低表达乳腺癌的用途 |
| CA3129419C (en) * | 2021-07-19 | 2023-02-28 | Mabplex International Co., Ltd. | Antibody drug conjugate loaded with binary toxins and its application |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001040276A2 (en) * | 1999-12-06 | 2001-06-07 | Agensys, Inc | Serpentine transmembrane antigens expressed in human prostate cancers and uses thereof |
| PL1742966T3 (pl) * | 2004-04-22 | 2014-04-30 | Agensys Inc | Przeciwciała i pochodzące z nich cząsteczki, które wiążą się z białkami STEAP-1 |
| BRPI0516284A (pt) * | 2004-09-23 | 2008-09-02 | Genentech Inc | anticorpo construìdo com cisteìna, método de selecionar anticorpos, compostos conjugados de droga-anticorpo, composição farmacêutica, método para matar ou inibir a proliferação de células de tumor, métodos de inibir a proliferação celular e o crescimento de células de tumor, artigo manufaturado e método para produzir um composto |
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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