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GEN News Highlights : Nov 3, 2009

Astex Signs CRADA with NCI to Investigate Its Small Molecule Therapeutic

AT13387, an HSP90 inhibitor, reportedly concentrates in tumor cells to create a targeted treatment.

Astex Therapeutics signed a five-year CRADA with the NCI to study its small molecule HSP90 inhibitor, AT13387, for treatment of various cancers. The NCI’s Division of Cancer Treatment and Diagnosis (DCTD) and Astex will evaluate the compound in multiple Phase I and Phase II trials, both as a single agent and in combination, in patients with tumors that are expected to be sensitive to inhibition of HSP90. Nonclinical studies designed to enhance the development of AT13387 will also be pursued. 

AT13387 is retained by and becomes concentrated in tumor cells, creating the opportunity for a highly specific, targeted cancer treatment, according to Astex. It is currently being investigated in a Phase I trial in patients with solid tumors at three centers in Boston. Astex reports that AT13387 is differentiated from other molecules in the class by its potency, extended pharmacodynamics, long tumor half-life, and improved preclinical safety profile.

The new agreement builds on NCI’s earlier support of the geldanamycin class of natural product HSP90 inhibitors. Astex is a U.K.-based company that discovers and develops small molecule therapeutics. It has built a pipeline of five molecularly-targeted oncology drugs with its fragment-based drug discovery platform, Pyramid™. Three compounds are currently being tested in clinical trials and two are in preclinical development.