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XS-02 is an orally administered, small molecule inhibitor developed for the treatment of advanced solid tumors. Its primary mechanism of action is inhibition of checkpoint kinase 1 (CHK1) and checkpoint kinase 2 (CHK2), enzymes involved in cell cycle regulation and DNA damage response. Preclinical research and early clinical development have also described XS-02 as a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), showing anti-cancer activity, particularly in breast cancer models and potentially triple-negative breast cancer. It is being developed by XSXH Therapeutics, with reported collaboration or trial activity involving NovaOnco Therapeutics. XS-02 is currently undergoing a phase I/II clinical trial assessing safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced solid tumors. It is a new molecular entity and not designated as an orphan drug.[1][3][4]
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