This week in therapeutics




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Pyruvate dehydrogenase

kinase 1 (PDK1)

Cell culture and mouse studies suggest inhibiting PDK1 could help treat melanoma. In a mouse xenograft model for BRAF V600E mutant melanoma, small hairpin RNA-mediated knockdown of PDK1 slowed tumor growth. In cultured human BRAF V600E mutant melanoma cells, PDK1 knockdown plus Zelboraf vemurafenib increased cell death compared with Zelboraf alone. Next steps include developing PDK1 inhibitors and examining the therapeutic potential of inhibiting PDK1 in solid tumors.

Daiichi Sankyo Co. Ltd., Chugai Pharmaceutical Co. Ltd. and Roche market Zelboraf, an oral small molecule inhibitor of oncogenic BRAF V600E, to treat melanoma.

SciBX 6(23); doi:10.1038/scibx.2013.576
Published online June 13, 2013

Patent application filed; available for licensing

Kaplon, J. et al. Nature; published online May 19, 2013;
Contact: Daniel Peeper, The Netherlands Cancer Institute, Amsterdam,
the Netherlands

Contact: Eyal Gottlieb, Cancer Research UK, Beatson Institute for Cancer Research, Glasgow, U.K.