- ATV-1601 is a first-in-class allosteric selective inhibitor of AKT1 E17K
- Pan-AKT inhibitors offer limited efficacy for patients with AKT1 E17K-driven mutant tumors due to insufficient inhibition of the AKT1 E17K mutation and AKT2-driven tolerability issues
- In preclinical studies, ATV-1601 has demonstrated enhanced target inhibition, superior efficacy, and improved tolerability compared to pan-AKT inhibitors
CAMBRIDGE, Mass., Aug. 04, 2025 (GLOBE NEWSWIRE) -- Atavistik Bio, a biotechnology company discovering the next generation of precision allosteric therapeutics inspired by the body’s natural regulators, today announced the dosing of the first patient in its Phase 1 study of ATV-1601 in adults with AKT1 E17K-mutant solid tumors.
ATV-1601 is a first-in-class selective inhibitor of AKT1 E17K, which leverages a reversible allosteric mechanism of action. Preclinically, ATV-1601 has demonstrated greater target engagement, superior efficacy, and improved tolerability compared to pan-AKT inhibitors. AKT1 E17K is a clinically validated oncogene that impacts greater than 40,000 cancer patients per year in the United States, with the highest prevalence in breast, endometrial, and prostate cancers. In addition, early evidence indicates that the AKT1 E17K mutation appears to be an emerging mechanism of resistance to PI3Kα-targeted cancer therapies. A selective allosteric AKT1 E17K inhibitor has the potential to be a transformative therapy against the validated AKT1 E17K oncogenic driver.
“Dosing the initial patient in our first-in-human study of ATV-1601 represents a significant milestone as we transition to a clinical stage biotechnology company and an important step forward in our efforts to develop innovative treatments for patients,” said Bryan Stuart, Chief Executive Officer at Atavistik Bio. “As a selective allosteric AKT1 E17K inhibitor, ATV-1601 has generated a highly differentiated preclinical profile, which we believe has the potential to address significant unmet need for patients. We look forward to evaluating ATV-1601 in the clinic and moving rapidly toward early proof-of-concept data for this program.”
The only approved AKT-targeted therapy is a pan-AKT inhibitor that blocks all three isoforms of AKT (AKT1, AKT2, and AKT3). Pan-AKT inhibitors offer limited efficacy for patients with AKT1 E17K-driven mutant tumors due to insufficient inhibition of the AKT1 E17K mutation. Additionally, pan-AKT inhibitors can cause significant adverse events, which leads to treatment discontinuation or dose-reductions in a considerable subset of patients. As a selective allosteric AKT1 E17K inhibitor, ATV-1601 has the potential to provide greater efficacy and tolerability compared to pan-AKT inhibitors for AKT1 E17K-driven cancers.
The first-in-human, open-label Phase 1a/1b study (NCT07038369) will evaluate the safety, tolerability, pharmacokinetics, and preliminary antitumor activity of ATV-1601 as monotherapy in participants with advanced or metastatic AKT1 E17K-mutant solid tumors, and in combination with fulvestrant in participants with AKT1 E17K-mutant HR-positive/HER2-negative breast cancer. The Phase 1 study has a dose escalation and expansion phase with AKT-1601 monotherapy, and an escalation and expansion phase with AKT-1601 in combination with fulvestrant.
ATV-1601 was developed leveraging Atavistik Bio’s AMPS™ technology, which is seamlessly integrated with its AI-enabled drug discovery engine to rapidly advance programs from discovery into development. Atavistik Bio is advancing a pipeline of precision allosteric oncology candidates, all discovered in-house, against a broad range of target classes.
About Atavistik Bio
Atavistik Bio is a clinical stage biotechnology company accelerating the discovery and development of transformative precision allosteric therapeutics to address serious unmet patient needs. Since its inception, Atavistik Bio has rapidly established an emerging pipeline of allosteric therapeutics with the potential to achieve superior efficacy and tolerability profiles by leveraging the power of allostery. Atavistik Bio is currently conducting a Phase 1 clinical trial of ATV-1601, a selective allosteric inhibitor for solid tumors.
Atavistik Bio is led by an experienced team of drug hunters with a proven track record of developing marketed small molecule therapies and supported by top-tier investors, including The Column Group, Nextech Invest, and Lux Capital. To learn more, visit us at atavistikbio.com and follow us on LinkedIn.
Media Contact:
Liz Melone
Melone Communications, LLC
liz@melonecomm.com
