Cytokinetics, Inc. (CYTK) said Friday that an abstract summarizing non-clinical data relating to GSK-923295, an inhibitor of centromere-associated protein E, was presented as a poster at the 32nd Annual San Antonio Breast Cancer Symposium in San Antonio, Texas.
The authors studied inhibitors of the mitotic apparatus, including inhibitors of PLK1, CENP-E and AURKB, with the goal of identifying biomarkers of therapeutic response that could be used to identify responsive subpopulations of patients. In this analysis, the compounds GSK461364, GSK-923295 and GSK1070916, small molecules which inhibit PLK1, CENP-E and AURKB, respectively, were tested in a panel of 54 breast cancer cells. The authors identified a network of 54 genes encoding proteins of the mitotic apparatus that is transcriptionally active in subtypes of breast cancer cell lines and primary tumors. In breast cancer cell lines with high mitotic network activity, the small molecule inhibitors of PLK1, CENP-E, and AURKB were found to be preferentially effective.
GSK-923295 is being studied in a GlaxoSmithKline plc (GSK) sponsored Phase I, first-time-in-humans clinical trial designed to evaluate the safety, tolerability, pharmacodynamics and pharmacokinetic profile of this novel drug candidate in patients with advanced, refractory solid tumors. The primary objective of this trial is to determine the maximum-tolerated dose, dose-limiting toxicity, safety and pharmacokinetics of GSK-923295 in those patients.
In December 2009, Cytokinetics announced that it agreed with GlaxoSmithKline to terminate their collaboration and license agreement, effective February 28. As a result, all rights for GSK-923295 will revert to Cytokinetics effective February 28. GlaxoSmithKline remains responsible for all activities and costs associated with completing and reporting on the ongoing Phase I clinical trial of GSK-923295.
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