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REC-7735 is a highly selective, structurally differentiated small molecule inhibitor designed to target the PI3Kα H1047R mutant. This mutation is commonly found in HER2-negative, hormone receptor-positive (HR+) breast cancer. The drug was developed using AI-driven design to enhance selectivity for the H1047R mutant form of PI3Kα, aiming to improve therapeutic index and reduce dose-limiting toxicities such as hyperglycemia that are associated with standard-of-care PI3K inhibitors. In preclinical models, REC-7735 demonstrated dose-dependent tumor regression in PI3Kα H1047R cell-derived xenograft (CDX) models and did not cause elevations in insulin levels or hyperglycemia markers in wild-type mice. Notably, low-dose REC-7735 outperformed high-dose capivasertib (an AKT inhibitor) both in efficacy and tolerability[1][2][6][7].
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