romidepsin-fk228-depsipeptide

Description: Romidepsin (formerly FK-228, FR-901228, Depsipeptide, NSC-630176; trade name Istodax) is a novel, potent and naturally occuring bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum with potential anticancer activity. Romidepsin acts as a potent histone deacetylase (HDAC1/2) inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. After intracellular activation, romidepsin binds to and inhibits HDAC, resulting in alterations in gene expression and the induction of cell differentiation, cell cycle arrest, and apoptosis. The US FDA approved romidepsin for the treatment of cutaneous T-cell lymphoma (CTCL) in November 2009 and approved romidepsin for other peripheral T-cell lymphomas (PTCLs) in June 2011.

References: Cancer Res. 2002 Sep 1; 62(17):4916-21; Biochem Pharmacol. 2002 Oct 1; 64(7):1079-90; Int J Cancer. 2002 Jan 20; 97(3):290-6.