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Mocetinostat

Description of Mocetinostat: Mocetinostat is a rationally designed, orally available, Class 1-selective, small molecule, 2-aminobenzamide HDAC inhibitor with potential antineoplastic activity. Mocetinostat binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur through the induction of apoptosis, differentiation, cell cycle arrest, inhibition of DNA repair, upregulation of tumor suppressors, down regulation of growth factors, oxidative stress, and autophagy, among others. Overexpression of Class I HDACs 1, 2 and 3 has been found in many tumors and has been correlated with a poor prognosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:   Methylgene and TAIHO PHARMACEUTICAL

MGCD0103 has been in multiple clinical trials and is licensed to TAIHO PHARMACEUTICAL for certain Asian countries. MGCD0103 is a rationally designed, oral, isotype-selective, small molecule HDAC inhibitor which has been designed to be a molecular-targeted cancer therapy.

MGCD0103 appears tolerable and exhibits favorable pharmacokinetic and pharmacodynamic profiles with evidence of target inhibition in surrogate tissues. Clinical and pharmacodynamic data support a three-times-weekly administration at a 90-mg fixed dose. MGCD0103 displays promising antitumor activity in hematological and lymphoproliferative diseases.

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