Apeiron Receives IND Clearance from NMPA for next generation PRMT5 Inhibitor GTA182 to Treat MTAP Null Tumors

- Potentially best-in-class MTA-cooperative PRMT5 inhibitor

- Demonstrates substantially expanded therapeutic window in pre-clinical models of glioblastoma and non-CNS tumor models with MTAP deletion

- Apeiron plans to file an Investigational New Drug (IND) application with the US FDA for GTA182 in 2025

SAN FRANCISCO, CA and SHANGHAI, China, Oct. 14th, 2024 — Apeiron Therapeutics (Apeiron), a precision oncology company leveraging cutting-edge technology and artificial intelligence (AI) for cancer drug discovery, today announced that the China National Medical Products Administration (NMPA) has cleared Apeiron’s Investigational New Drug (IND) application for GTA182, its potentially best-in-class MTA-cooperative PRMT5 inhibitor, for the treatment of MTAP-null solid tumors.

MTAP (Methylthioadenosine Phosphorylase) is co-deleted with the tumor suppressor gene CDKN2A in 10-15% of cancer patients across a broad spectrum of tumor types. GTA182 is a next-generation MTA-cooperative, brain-penetrant inhibitor of protein arginine methyltransferase 5 (PRMT5) with a substantially expanded therapeutic window, as demonstrated in preclinical studies.

“NMPA’s clearance of the GTA182 IND is an important milestone for Apeiron,” said Fred Aswad, Ph.D., Co-Founder and Senior Vice President of Apeiron. “GTA182 represents a significant advance in targeting MTAP-null tumors. Our preclinical data shows compelling tumor growth inhibition and regression in multiple models, including glioblastoma, one of the most challenging cancers to treat. We are excited to advance this therapy into clinical trials and look forward to filing a US IND with the FDA in 2025 to expand our global development efforts.”

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.

About GTA182

GTA182 is a proprietary small molecule discovered through Apeiron’s AI-guided drug discovery platform. In preclinical studies, Apeiron 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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