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SAR260301 is a potent and selective small molecule inhibitor of the class I phosphatidylinositol 3-kinase beta isoform (PI3Kβ). It was developed by Sanofi for its potential antineoplastic activity, particularly targeting tumors with PTEN deficiency or high PI3Kβ expression. By inhibiting PI3Kβ kinase activity in the PI3K/Akt/mTOR pathway, SAR260301 can induce apoptosis and inhibit growth in susceptible tumor cells. The drug demonstrated strong selectivity for the PI3Kβ isoform over other class I PI3Ks and showed synergistic antitumor effects when combined with BRAF or MEK inhibitors in preclinical models of PTEN-deficient/BRAF-mutant melanoma. Clinical development reached phase I trials in patients with advanced solid tumors; however, further development was terminated due to insufficient drug exposure resulting from rapid clearance[1][4][5][6].
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