Description
MGCD-0103 (Mocetinostat) is a benzamide histone deacetylase (HDAC) inhibitor that exhibits anticancer chemotherapeutic, anti-fibrotic, antihypertensive, and cardiomodulatory activities. MGCD-0103 is currently in clinical trials as a potential treatment for several leukemias and lymphomas. In sham hearts, MGCD-0103 improves left ventricular and end diastolic pressure and decreases total collagen levels; in CD90+ cells, it decreases levels of collagen III, matrix metalloproteinase 2, and α-SMA. In other models, MGCD-0103 increases natriuretic peptide receptor (NPR1) promoter activity, increasing transcription of guanyl cyclase A/natriuretic peptide receptor A. MGCD-0103 also decreases pulmonary artery pressure, right ventricular hypertrophy, and vascular remodeling in animal models of myocardial infarction and heart failure. Additionally, this compound induces apoptosis, activates PI3K/Akt/mTOR signaling, and decreases autophagy in chronic lymphocytic leukemia (CLL) cells.