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SDX-7539 is a small molecule inhibitor of methionine aminopeptidase type 2 (METAP2) and the active moiety of the polymer-conjugated drug evexomostat (SDX-7320). Developed by SynDevRx, it belongs to the fumagillin class of inhibitors. SDX-7539 works by inhibiting the METAP2 enzyme, which is involved in protein processing and has been linked to both metabolic regulation and tumor cell proliferation. Preclinical studies indicate that METAP2 inhibition by SDX-7539 and its prodrug form leads to weight loss, improved insulin sensitivity, and significant anti-tumor activity, particularly in obesity-accelerated cancers. It acts by suppressing cell cycle progression and modulating the immune microenvironment within tumors.
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