HBI-8000: A novel histone deacetylase (HDAC) inhibitor for cancer
- HBI-8000 is a low nanomolar inhibitor of cancer-associated HDACs with broad spectrum in vitro and in vivo anti-tumor activity
- Phase 2 clinical trial completed in China: Safety, PK, Biomarker, and Efficacy data highly encouraging - preclinical and clinical data demonstrate best in class potential
- Two Phase 2 trials are in progress in China
- Successful Pre-IND consultation with US FDA: Plan acceptable, including use of preclinical and clinical Chinese data as supportive for US IND and Phase 1 trial
- IND-enabling studies completed in US, including GLP toxicology and GMP drug substance and drug product manufacturing
- US Phase 1 planned for Q1 2010
About HDACs and HDAC inhibitors
HDAC inhibitors work by controlling how tightly DNA is wound around histone proteins. By deacetylating (removing an acetyl group from) histones, HDACs appear to promote tighter winding of DNA around these proteins, leading to reduced access by gene transcription factors. This results in decreased expression of proteins involved in cell differentiation, cell cycle arrest, tumor immunity, and apoptotic elimination of damaged cells, all of which contribute to the development of cancer. HDAC inhibitors are able to restore expression of tumor suppressor and other anti-tumor genes in a selective manner. Treatment with HDAC inhibitors also leads, indirectly, to inhibition of the expression of angiogenesis factors, helping to choke off the blood supply to tumors. Although significant preclinical and clinical activity has been observed with HDAC inhibitors, most have characteristics which may limit their potential for clinical success or broad applicability. In contrast, HBI-8000 has selectivity, potency, PK and side effect profiles that make it more suitable for use as a stand-alone therapeutic, as well as in combination with a wide variety of marketed anti-tumor agents. Worldwide licensing rights ex-China are available.