- Data demonstrate that ATV-1601, a selective allosteric inhibitor of AKT1 E17K, provides enhanced target inhibition, superior efficacy and improved tolerability compared to pan-AKT inhibitors in preclinical models
- Atavistik Bio anticipates initiating a first-in-human study with ATV-1601 in patients with AKT1 E17K mutant tumors in early 2025
Cambridge, Mass., October 23, 2024 – Atavistik Bio, a biotechnology company discovering the next generation of precision allosteric therapeutics inspired by the body’s natural regulators, today presented preclinical data at the 36th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics Meeting 2024 in Barcelona for ATV-1601, the company’s orally bioavailable selective allosteric small molecule inhibitor for AKT1 E17K-driven cancers. The preclinical data demonstrated that as a selective allosteric AKT1 E17K inhibitor, ATV-1601 provides enhanced target inhibition, superior efficacy and improved tolerability compared to pan-AKT inhibitors in preclinical models. Atavistik Bio anticipates initiating a first-in-human study with ATV-1601 in patients with AKT1 E17K mutant tumors in early 2025.
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. 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, such as AKT2-driven hyperglycemia, rash, and diarrhea, which lead to treatment discontinuation or dose reductions in a considerable subset of patients.
Data presented in today’s poster entitled, “ATV-1601 is a Potent and Selective Allosteric Inhibitor of AKT1 E17K and Shows Profound and Durable Regressions in AKT1 E17K-Driven Patient-Derived Xenograft Models,” demonstrates that the selectivity profile of ATV-1601 enables greater than 90% target engagement without inducing hyperglycemia in preclinical models. As a result of this potent target engagement and selectivity, ATV-1601 demonstrated profound and durable tumor regression in multiple AKT1 E17K driven patient-derived breast and endometrial tumor models and was well tolerated.
“We are pleased to share these exciting preclinical data for our ATV-1601 program with the oncology community,” said Marion Dorsch, Ph.D., President and Chief Scientific Officer, Atavistik Bio. “As a selective allosteric AKT1 E17K inhibitor, ATV-1601 has the potential to be a transformative precision therapy against the validated AKT1 E17K oncogenic driver. The patient populations impacted by the AKT1 E17K mutation have a significant unmet need, which we are working with urgency to address. We look forward to transitioning into the clinic in our planned first-in-human study.”
About Atavistik Bio
Atavistik Bio is a biotechnology company accelerating the discovery and development of transformative precision allosteric therapeutics to address serious unmet patient needs, with a focus on oncology. 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.
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