This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Ovarian cancer

Nicotinamide phosphoribosyl transferase (NAMPT; NamPRT)

In vitro and mouse studies identified thiourea inhibitors of NAMPT that could be useful for treating ovarian cancer. In cultured ovarian tumor cells, SAR studies identified a lead thiourea-based compound that inhibited NAMPT with an IC50 value of 32 nM. In mouse xenograft models for human ovarian cancer, the most potent compounds decreased tumor growth compared with vehicle and showed oral bioavailability. Next steps include further chemical optimization.

SciBX 6(21); doi:10.1038/scibx.2013.517
Published online May 30, 2013

Patent and licensing status undisclosed

Zheng, X. et al. J. Med. Chem.; published online April 25, 2013;
doi:10.1021/jm400186h
Contact: Xiaozhang Zheng, Forma Therapeutics Inc., Watertown, Mass.
e-mail:

xzheng@formatherapeutics.com