Drug intelligence / Profile preview

mocetinostat + gemcitabine

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**mocetinostat + gemcitabine** is an investigational combination therapy composed of mocetinostat, a Class I/IV histone deacetylase (HDAC) inhibitor, and gemcitabine, a nucleoside analog antimetabolite. Mocetinostat acts by inhibiting HDAC activity, targeting epigenetic regulation and leading to chromatin remodeling and apoptosis in cancer cells. Gemcitabine is incorporated into DNA as a false substrate, blocking DNA synthesis and promoting apoptosis. This combination has been studied primarily in advanced solid tumors including pancreatic cancer and metastatic leiomyosarcoma, aiming to overcome chemoresistance and enhance cytotoxicity. Mocetinostat was supplied by Mirati Therapeutics for clinical studies, while gemcitabine is a widely used generic chemotherapy agent.

Other names
mocetinostat and gemcitabinemocetinostat combined with gemcitabine
02

Targets

HDAC11 (Histone Deacetylase 11)DNA polymerase familyRNR (Ribonucleotide reductase)HDAC1 (Histone Deacetylase 1)DNA

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