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news.Serenex is beginning advanced preclinical cancer studies on a novel series of Heat Shock Protein 90 inhibitors following their demonstrated efficacy in multiple mouse xenograft tumor studies.
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The small molecule Heat Shock Protein 90 or HSP90 inhibitors have low molecular weights, require few synthetic steps and are derived from a novel chemical scaffold. They exhibit good oral bioavailability, are water soluble and have broad anti-proliferative activity.
Importantly, they do not contain a quinone functionality which has been suggested to be linked to the dose-limiting toxicities observed with geldanamycin related HSP90 inhibitors. These molecules address many of the limitations of the natural product-based HSP90 inhibitors currently in development.
“Based on current information, we believe our compounds are best-in- class,” said Dr Richard Kent, Serenex CEO and president. “This is significant news for the pharmaceutical industry, because HSP90 is among the top 10 new drug development targets in cancer research.”
Serenex expects to select a development candidate from its current lead series before the end of the year and initiate clinical studies in 2006.
The company is hoping that the encouraging results will help Serenex form a partnership with an established company with complementary expertise, and thereby accelerate development. Dr Kent said: “Our goal is to keep the Serenex team focused on the HSP90 inhibitor platform, working with our partner through at least phase II proof of concept.”