Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM.
1. Clinical pharmacology proﬁle of vorinostat, a histone deacetylase inhibitor
Marian Iwamoto • Evan J. Friedman •Punam Sandhu • Nancy G. B. Agrawal. Cancer Chemother Pharmacol (2013) 72:493–508
Vorinostat is an HDAC inhibitor currently marketed in the United States and other countries for the treatment of cutaneous manifestations in patients with cutaneous T cell lymphoma (CTCL) who have progressive disease, persistent, or recurrent disease following two systemic therapies. Vorinostat inhibits the enzymatic activity of Class I (HDAC1, HDAC2, HDAC3) and Class II (HDAC6) HDACs at nanomolar concentrations (IC50<86 nM). A clinical study of vorinostat in patients with stage Ib and higher CTCL, who had failed to two systemic therapies (one containing bexarotene), demonstrated a 30 % overall objective response. An additional study in refractory CTCL patients demonstrated a similar response rate of 31 %.