tanerasertib

Tanerasertib (ALTA2618) is an orally bioavailable, first-in-class, mutation-selective, and covalent allosteric inhibitor of the AKT1 E17K mutant protein, developed by Alterome Therapeutics. The AKT1 E17K mutation is a key oncogenic driver found in various solid tumors, including breast and endometrial cancers. By selectively targeting the mutant AKT1 E17K variant while sparing wild-type AKT1 and avoiding AKT2-driven toxicities (such as hyperglycemia), tanerasertib is designed to offer a wider therapeutic index and improved tolerability compared to pan-AKT inhibitors. It is currently undergoing Phase 1/1b clinical evaluation for patients with advanced solid tumors harboring the AKT1 E17K mutation.