Apeiron Therapeutics Presents Preclinical Data from its Oncology Program on PRMT5 Inhibitor GTA182 at AACR 2025 Annual Meeting
SAN FRANCISCO, CA, Apr. 25, 2025 – Apeiron Therapeutics (Apeiron), a precision oncology company leveraging state-of-the-art structural biology and AI-guided molecular modeling for drug discovery, today announced the presentation of preclinical data on its investigational PRMT5 inhibitor, GTA182, at the American Association for Cancer Research (AACR) 2025 Annual Meeting in Chicago, IL. The data, presented in a poster session, highlight GTA182’s selectivity and anti-tumor efficacy in disease-relevant models. GTA182 is currently being evaluated in ongoing Phase 1 clinical trials for patients with advanced MTAP-null solid tumors.
“Our preclinical data underscore GTA182’s potential to transform the treatment landscape for MTAP-deleted cancers by offering superior selectivity, optimized pharmacokinetics, and blood-brain barrier penetration,” said Fred Aswad, Ph.D., Co-founder and Chief Scientific Officer of Apeiron Therapeutics. “By leveraging our expertise in structure-based drug design and AI-guided molecular modeling, we have developed a PRMT5 inhibitor that not only demonstrates strong monotherapy activity but also has the potential to be an effective combination therapy across multiple tumor types.”
GTA182 is a second-generation MTA-cooperative PRMT5 inhibitor targeting MTAP-deleted tumors with remarkable selectivity. Preclinical data shows GTA182 achieves over 100-fold selectivity for MTAP-/- cells, demonstrating superior anti-tumor efficacy at 3 mg/kg compared to competitor compounds. Its optimized pharmacokinetic profile provides a 30-fold exposure multiple and up to 23-fold therapeutic index, supporting once-daily dosing with a favorable safety margin. GTA182 also demonstrates effective blood-brain barrier penetration with promising activity in glioblastoma models, suggesting potential for CNS malignancies. Preliminary data indicates synergistic potential with multiple therapeutic classes, positioning GTA182 as a potentially best-in-class therapy for MTAP-deleted solid tumors.
About GTA182
GTA182 is a proprietary small molecule discovered through Apeiron’s AI-guided drug discovery platform. Currently in Phase 1 clinical development, GTA182 demonstrated potent and selective inhibition of PRMT5, exhibiting over 100-fold selectivity for MTAP-deleted tumor cell lines. Importantly, GTA182 is brain-penetrant and has shown tumor growth inhibition and regression in in vivo preclinical models, including glioblastoma (GBM) and various non-CNS cancer models with MTAP deletions.
About Apeiron Therapeutics
Apeiron is redefining medical discovery through the integration of artificial intelligence, streamlining the drug development process from target selection to clinical trials. With a strategic presence in the San Francisco Bay Area, Apeiron combines world-class talent and cutting-edge technologies to drive biomedical innovation. We are committed to advancing breakthrough therapies that address the most pressing unmet medical needs.
For more information, please visit https://www.apeiron-bio.com.
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