VX-765

VX-765 is a novel Caspase-1 inhibitor being investigated for the treatment of epilepsy, currently being developed by Vertex. VX-765 is an orally-absorbed pro-drug of VRT-043198, a potent and selective inhibitor of ICE/caspase-1 sub-family caspases. VRT-043198 exhibits 100-10, 000-fold selectivity against other caspase-3 and -6-9. In cultures of peripheral blood mononuclear cells and whole blood from healthy subjects stimulated with bacterial products, VRT-043198 inhibited the release of Interleukin (IL)-1beta and IL-18, but had little effect on the release of several other cytokines, including IL-1alpha, tumor necrosis factor-alpha, IL-6 and IL-8.

Store at 0° C (short term), -20° C (long term), desiccated

HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis

1. Boxer, Matthew B.; Quinn, Amy M.; Shen, Min; Jadhav, Ajit; Leister, William; Simeonov, Anton; Auld, Douglas S.; Thomas, Craig J. A Highly Potent and Selective Caspase 1 Inhibitor that Utilizes a Key 3-Cyanopropanoic Acid Moiety. ChemMedChem (2010), 5(5), 730-738.  

2. Eda, Hiroyuki. Therapeutic potential for caspase inhibitors: Present and future. Design of Caspase Inhibitors as Potential Clinical Agents (2009), 251-287