Drug intelligence / Profile preview

ALTA-2618

Development stage
Phase 1
Lead developer
Alterome Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

ALTA-2618 is an orally bioavailable, small molecule, mutant-selective, and covalent allosteric inhibitor of the AKT1 E17K mutation. Developed by Alterome Therapeutics, it is designed to selectively target and inhibit the oncogenic AKT1 E17K variant—a clinically validated driver mutation found in a subset of cancers including breast (notably hormone receptor-positive), endometrial, and prostate cancers. Unlike ATP-competitive inhibitors that affect both wild-type and mutant AKT isoforms (leading to toxicity), ALTA-2618 covalently binds to the E17K-mutant form of AKT1 with high selectivity, sparing wild-type protein and reducing on-target toxicities such as hyperglycemia. Preclinical studies have shown potent anti-tumor activity in patient-derived xenograft models with favorable pharmacokinetics and tolerability profiles. The drug is currently being evaluated in Phase I clinical trials for patients with advanced solid tumors harboring the AKT1 E17K mutation who have limited treatment options[1][4][6][7][9].

Other names
ALTA 2618ALTA2618ALTA-2618
02

Targets

AKT1 E17K (AKT serine/threonine kinase 1 E17K mutant)

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