remetinostat

Remetinostat is a small molecule, topical histone deacetylase (HDAC) inhibitor developed primarily for the treatment of cutaneous T-cell lymphoma (CTCL), particularly mycosis fungoides (MF), and has also been investigated for basal cell carcinoma (BCC)[1][3][5][7]. Unlike systemic HDAC inhibitors, remetinostat is designed to be active only in the skin and is rapidly degraded upon entering the bloodstream, minimizing systemic side effects[1][5]. Mechanistically, it inhibits HDAC isoforms 1, 3, and 6[5][8], leading to increased acetylation of histones in skin cells. This results in chromatin remodeling and selective transcription of tumor suppressor genes that inhibit tumor cell division and induce apoptosis[3][6]. Remetinostat has demonstrated efficacy in phase II trials for both early-stage MF/CTCL—showing reduction of skin lesions and pruritus with high tolerability—and BCC—showing significant reduction in tumor burden with minimal adverse events[1][5][7]. The drug was developed by Medivir.

Brand names

SHAPE Gel

Other names

remetinostatmethylparaben suberohydroxamic acid phenyl ester946150-57-8