Apeiron Enrolls First Patient in Phase 1a/b Study of PRMT5 Inhibitor GTA182 for MTAP-Deleted Solid Tumors
- Potentially best-in-class MTA-cooperative PRMT5 inhibitor -
- First patient in for Phase 1a/b study to evaluate GTA182 clinically in patients having tumors with MTAP deletion -
SAN FRANCISCO, CA and SHANGHAI, China, Nov. 19th, 2024 — 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 enrollment of the first patient in its Phase 1a/b study to evaluate GTA182 for advanced solid tumors with MTAP deletions. The trial is designed to evaluate the safety, efficacy, and pharmacokinetics of GTA182 across multiple ascending doses, as a monotherapy and in combination with standard of care therapy, in adults with advanced MTAP null solid tumors.
“The initiation of the GTA182 Phase 1a/b clinical trial represents a significant milestone in our company’s growth and marks our second drug candidate to enter clinical studies,” said Mingxi Li, Ph.D., Chief Executive Officer of Apeiron.
“GTA182 was designed to overcome the safety and efficacy limitations of existing second-generation PRMT5 inhibitors, with the goal of delivering a transformative therapy for patients with few treatment options,” added Fred Aswad, J.D., Ph.D., Senior Vice President of Apeiron Therapeutics.
The first-in-human Phase 1a/b clinical trial of GTA182 is an open-label, multicenter study involving dose escalation and dose expansion. The study will enroll patients with MTAP-null solid tumors, with the primary objectives being to characterize the safety and tolerability of GTA182 and determine its optimal therapeutic dose. For more details about our trial, please visit: https://www.cde.org.cn.
About GTA182
GTA182 is a proprietary small molecule discovered through Apeiron’s AI-guided drug discovery platform. In preclinical studies, Apeiron’s preclinical studies demonstrated that GTA182 is a potent and selective PRMT5 inhibitor, exhibiting greater than 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 strategic locations in the San Francisco Bay Area and Shanghai, Apeiron combines world-class talent and cutting-edge technologies from across the globe. We are committed to pushing the frontiers of biomedical innovation to create breakthrough therapies that address the most pressing unmet medical needs.
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