发明名称 |
ANTIBODY-DRUG CONJUGATES WITH HIGH DRUG LOADING |
摘要 |
The present invention provides transglutaminase-mediated antibody-drug conjugates with high antibody-drug ratio (DAR) comprising 1) glutamine-containing tags, endogenous glutamines, and/or endogenous glutamines made reactive by antibody engineering or an engineered transglutaminase (e.g., with altered substrate specifity); and 2) amine donor agents comprising amine donor units, linkers, and agent moieties, wherein the DAR is at least about 5. The invention also provides methods of making and methods of using such higher drug loaded antibody-drug conjugates. |
申请公布号 |
CA2946488(A1) |
申请公布日期 |
2015.10.29 |
申请号 |
CA20152946488 |
申请日期 |
2015.04.21 |
申请人 |
RINAT NEUROSCIENCE CORP.;PFIZER INC. |
发明人 |
STROP, PAVEL;DELARIA, KATHERINE ANNE;DORYWALSKA, MAGDALENA;FOLETTI, DAVIDE LUCIANO;DUSHIN, RUSSELL GEORGE;SHELTON, DAVID LOUIS;RAJPAL, ARVIND |
分类号 |
C07K16/00;A61P35/00;C07K1/113;C07K1/13;C07K16/18;C07K16/28;C07K16/46 |
主分类号 |
C07K16/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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