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In vitro and mouse studies suggest prodrugs of the duocarmycin family of DNA-alkylating agents could help treat cancer. In a murine leukemia cell line, two of the lead N-acyl O-amino prodrugs of duocarmycin analogs showed cytotoxicity with subnanomolar IC50 values. In a mouse model for leukemia, one of the lead prodrugs increased survival compared with the nonprodrug compound. Ongoing work includes testing the lead compound in rodent xenograft models for undisclosed cancers.
Synthon B.V.'s anti-HER2-ADC, an antibody-drug conjugate consisting of trastuzumab conjugated to duocarmycin analogs using the company's SpaceLink technology, is in preclinical testing to treat cancer.
Roche's Genentech Inc. unit and Chugai Pharmaceutical Co. Ltd. market Herceptin trastuzumab, an anti-HER2 (EGFR2; ErbB2; neu) antibody, to treat breast and gastric cancers.

SciBX 6(19); doi:10.1038/scibx.2013.462
Published online May 16, 2013

Patented; unlicensed

Wolfe, A.L. et al. J. Med. Chem.; published online April 29, 2013;
Contact: Dale L. Boger,
The Scripps Research Institute,
La Jolla, Calif.