Rajeeva Singh,Yelena Kovtun,Sharon D. Wilhelm,Ravi V.J. Chari
申请号：
US14835236
公开号：
US20160114052A1
申请日:
2015.08.25
申请国别(地区):
US
年份:
2016
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.
