Belinostat

Belinostat is an inhibitor of class I histone deacetylases (HDACs; IC₅₀s = 0.041, 0.125, 0.03, and 0.216 µM for HDAC1, -2, -3, and -8, respectively) and class II HDACs (IC₅₀s = 0.115, 0.082, 0.067, and 0.128 µM for HDAC4, -6, -7, and -9, respectively).¹ It inhibits HDAC activity in HeLa cell lysates (IC₅₀ = 0.027 µM) and the proliferation of A2780 ovarian, HCT116 colon, Calu-3 lung, and Hs 852.T melanoma cells (IC₅₀s = 0.2, 0.2, 0.66, and 3.37 µM, respectively).² It reduces tumor growth in an A2780 mouse xenograft model when administered at doses of 10, 20, and 40 mg/kg. Formulations containing belinostat have been used in the treatment of relapsed or refractory peripheral T cell lymphoma.

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1. Khan, N., Jeffers, M., Kumar, S., et al. Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. Biochem. J. 409(2), 581-589 (2008).

2. Plumb, J.A., Finn, P.W., Williams, R.J., et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol. Cancer Ther. 2(8), 721-728 (2003).