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HS-10352 is a highly potent and selective small molecule inhibitor of phosphoinositide 3-kinase alpha (PI3Kα, encoded by PIK3CA). It selectively targets, binds to, and inhibits both wild-type and mutated forms of PIK3CA in the PI3K/Akt/mTOR signaling pathway. This inhibition leads to apoptosis and growth inhibition in tumor cells expressing PIK3CA mutations. The drug is being developed primarily for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer, particularly in patients with PIK3CA mutations. Clinical studies have shown that HS-10352 is well-tolerated at a maximum tolerated dose of 6 mg once daily, with hyperglycemia as the most common adverse event. Preliminary antitumor activity has been observed in this patient population[1][2][7][9].
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