POTENT CONJUGATES AND HYDROPHILIC LINKERS

摘要

PROBLEM TO BE SOLVED: To provide new linkers to link drugs (e.g. cytotoxic agents) to cell-binding agents (e.g., antibodies) such that the linker contributes to increase of the drug activity.SOLUTION: Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The linkers enhance the potency or the efficacy of the cell-binding agent-drug conjugates several-fold 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.