This week in therapeutics




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Breast cancer

Histone deacetylase 1 (HDAC1); HDAC6; estrogen receptor-a

Cell culture studies suggest bifunctional compounds inhibiting HDAC1, HDAC6 and estrogen receptors (ERs) could help treat ER+ breast cancer. In human breast cancer cells, conjugates of the HDAC inhibitor Zolinza vorinostat with the generic ER antagonist tamoxifen showed more potent antiproliferative effects against ER+ cells than ER- cells. In breast cancer cell lines, the bifunctional compounds caused twofold more inhibition of growth than tamoxifen alone. Next steps include optimization of lead compounds and evaluating tumor-selective accumulation and efficacy in mouse models.
Merck & Co. Inc. and Taiho Pharmaceutical Co. Ltd. market Zolinza to treat cutaneous T cell lymphoma (CTCL).

SciBX 6(29); doi:10.1038/scibx.2013.749
Published online Aug. 1, 2013

Patent status undisclosed; available for licensing from the Georgia Tech Research Corp.

Gryder, B.E. et al. J. Med. Chem.; published online June 20, 2013;
Contact: Adegboyega K. Oyelere, Georgia Institute of Technology, Atlanta, Georgia