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XL495 is a novel, potent small molecule inhibitor of protein kinase membrane associated tyrosine/threonine 1 (PKMYT1), developed by Exelixis for the treatment of advanced solid tumors. PKMYT1 inhibition is synthetically lethal in cancer cells with genetic anomalies that lead to replication stress—a vulnerability not typically present in normal cells. The drug is currently being evaluated in phase 1 clinical trials as both monotherapy and in combination with select cytotoxic agents for patients with locally advanced or metastatic solid tumors who have limited or no remaining standard treatment options.
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