Our broad strategic alliance with GlaxoSmithKline has yielded a third novel drug candidate, GSK-923295, a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E, (CENP-E).

CENP-E plays an essential role in chromosome movement during early cell division or mitosis and integrates mitotic spindle mechanics with regulators of the mitotic checkpoint regulating cell-cycle transition from metaphase to anaphase. Inhibition of CENP-E induces cell cycle arrest during cell duplication leading to subsequent apoptosis or cell death. In preclinical studies, GSK-923295 demonstrated a broad spectrum of activity against a range of human tumor xenografts grown in nude mice, including models of colon, breast, ovarian, lung and other tumors.

GSK-923295 is the first drug candidate to enter human clinical trials that specifically targets CENP-E and is currently in Phase I human clinical trials being conducted by GSK. Information regarding this ongoing Phase I clinical trial is below:

Development Status for GSK-923295

Ongoing Phase I Clinical Trial Details