Inhibitors of histone deacetylases (HDACs) are emerging as a promising new class of anticancer agents. Inhibition of HDAC activities in cancer cells leads to inhibition of tumor cell proliferation, cell cycle arrest and induction of apoptosis. The recent approval of an HDAC inhibitor has provided clinical validation for the concept of HDAC inhibition in the treatment of cancer, and numerous HDAC inhibitors are currently being tested in clinical trials.

EntreMed has developed a series of novel, potent HDAC inhibitors that are currently in preclinical evaluation. The EntreMed portfolio of HDAC inhibitors encompasses several chemically distinct series of compounds. Comparisons in vitro and in vivo with benchmark compounds indicate that EntreMed’s HDAC inhibitors have superior potency and efficacy, and are potentially less toxic. Additionally, a chemical scaffold that can confer selectivity between Class I and II HDAC isoforms has been identified within a novel chemical series. Multiple patent applications have been filed, providing excellent protection as well as a good opportunity for second-generation molecules based on existing intellectual property.