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Drug intelligence / Profile preview
tanerasertib
- Development stage
- Phase 1
- Lead developer
- Alterome Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
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.
- Other names
- ALTA 2618ALTA2618ALTA-2618
02
Targets
AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)AKT1 E17K (AKT serine/threonine kinase 1 E17K mutant)AKT2 (Rac-beta serine/threonine-protein kinase)
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