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REZO-001 is a covalent allosteric small-molecule inhibitor selectively targeting the oncogenic AKT1 E17K mutant, developed using Rezo Therapeutics’ integrated disease network mapping and discovery platform for precision oncology indications characterized by this driver mutation.[6][11] In preclinical studies, REZO-001 demonstrated potent inhibition of AKT1 E17K signaling with a more favorable off-target kinase profile and safety panel readout compared with earlier pan-AKT inhibitors, supporting its potential to deliver effective pathway suppression with reduced toxicity.[6] The compound is being advanced as a first-in-class, mutation-selective AKT inhibitor for solid tumors harboring AKT1 E17K alterations.
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