REVIEW Mocetinostat (MGCD0103) is a potent benzamide histone deacetylase inhibitor with most potency for HDAC1 with IC50 of 0.15 μM, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinosta significantly inhibites growth of human tumor xenografts in nude mice and the antitumor activity correlated with induction of histone acetylation in tumors. MGCD0103 reduces pulmonary arterial pressure more dramatically than tadalafil, a standard-of-care therapy for human pulmonary hypertension that functions as a vasodilator. Moreover, MGCD0103 improves pulmonary artery acceleration time and reduced systolic notching of the pulmonary artery flow envelope, which suggests a positive impact of the HDAC inhibitor on pulmonary vascular remodeling and stiffening Mocetinostat is currently undergoing clinical trials for treatment of various cancers including follicular lymphoma, Hodgkin's lymphoma and acute myelogenous leukemia.
REFERENCES
[1]
K. Gelmon, A. Tolcher, M. Carducci, G. K. Reid, Z. Li, A. Kalita, V. Callejas, J. Longstreth, J. M. Besterman and L. L. Siu Phase I trials of the oral histone deacetylase (HDAC) inhibitor MGCD0103 given either daily or 3x weekly for 14 days every 3 weeks in patients (pts) with advanced solid tumors Journal of Clinical Oncology, 2005 ASCO Annual Meeting Proceedings. Vol 23, No 16S (June 1 Supplement), 2005: 3147.
[2]
Drug evaluation: MGCD-0103, a histone deacetylase inhibitor for the treatment of cancer. Kell J. Curr Opin Investig Drugs. 2007 Jun;8(6):485-92.
[3]
Paquin I, Raeppel S, Leit S, Gaudette F, Zhou N, Moradei O, Saavedra O, Bernstein N, Raeppel F, Bouchain G, Fréchette S, Woo SH, Vaisburg A, Fournel M, Kalita A, Robert MF, Lu A, Trachy-Bourget MC, Yan PT, Liu J, Rahil J, MacLeod AR, Besterman JM, Li Z, Delorme D, Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1067-71.
[4]
Le Tourneau C, Siu LL. Promising antitumor activity with MGCD0103, a novel isotype-selective histone deacetylase inhibitor. Expert Opin Investig Drugs. 2008 Aug;17(8):1247-54.
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