SINGH, RAJEEVA,KOVTUN, YELENA,WILHELM, SHARON D.,CHARI, RAVI V.J.
申请号：
EP09844200
公开号：
EP2486023A4
申请日:
2009.10.06
申请国别(地区):
EP
年份:
2014
代理人:
摘要：
Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.
