Description
Resminostat is an orally bioavailable inhibitor of histone deacetylase 1 (HDAC1), HDAC3, and HDAC6 (IC
50s = 43-72 nM), resulting in hyperacetylation of histone H4 in multiple myeloma cells. It abrogates cell growth and strongly induces apoptosis in multiple myeloma cells (IC
50s = 2.5-3 μM). Resminostat displays synergistic effects when combined with melphalan and the proteasome inhibitors bortezomib and S-2209. It dose-dependently inhibits HDAC activity
in vivo.
References
[1] mandl-weber s, meinel fg, jankowsky r, oduncu f, schmidmaier r, baumann p. the novel inhibitor of histone deacetylase resminostat (ras2410) inhibits proliferation and induces apoptosis in multiple myeloma (mm) cells. br j haematol. 2010 may;149(4):518-28.
[2] brunetto at, ang je, lal r, olmos d, molife lr, kristeleit r, parker a, casamayor i, olaleye m, mais a, hauns b, strobel v, hentsch b, de bono js. first-in-human, pharmacokinetic and pharmacodynamic phase i study of resminostat, an oral histone deacetylase inhibitor, in patients with advanced solid tumors. clin cancer res. 2013 oct 1;19(19):5494-504.
