Apeiron Therapeutics' Second-Generation MTA-Cooperative PRMT5 Inhibitor GTA182 Receives NMPA IND Approval for MTAP-Deficient Solid Tumors
Apeiron
Pharmaceutical R&D Developer
▎WuXi AppTec Content Team Report
On October 14, Apeiron Therapeutics announced that the company has developedSecond-generation MTA in combination with PRMT5 inhibitorThe clinical trial application (IND) for GTA182 has been approved by the National Medical Products Administration (NMPA) of China, and it is intended to be developed for the treatment ofMTAP-Deleted Solid Tumors。
Protein Arginine Methyltransferase 5 (PRMT5)Inhibitors are a new class of anti-tumor drugs, also considered to be the successorsPARP InhibitorAfterwardsBelowA WaveHopefulThe"One of the 'synthetic lethality' therapies, itCan be used withMTAPGene mutations constitute "synthetic lethal" partners.MTAP (Methylthioadenosine Phosphorylase) and Tumor Suppressor GenesCDKN2ACommonly missing in 10%~15% of patients with various types of tumors.
GTA182 is a small molecule compound independently developed by Apeiron Therapeutics through its artificial intelligence-guided drug discovery platform. In preclinical studies, Apeiron Therapeutics demonstrated that GTA182 isA highly efficient and selective PRMT5 inhibitor, forMTAPThe missing tumor cell line has more than 100 times selectivity.. Importantly, GTA182With blood-brain barrier permeability, and has demonstrated inhibition and reduction of tumor growth in preclinical models in vivo, including glioblastoma (GBM) as well as various MTAP-deficient non-CNS cancer models.
According to the press release from Apeiron, the Phase 1 clinical trial of GTA182 is an open-label, multi-center study, divided into two phases: dose escalation and dose expansion. The study will recruit patients with MTAP-deficient solid tumors, with the primary objective of evaluating the safety and tolerability of GTA182 and determining its optimal therapeutic dose.
"NMPA's approval of GTA182's IND application is an important milestone for Apeiron Therapeutics," said Dr. Fred Aswad, Co-founder and Senior Vice President of Apeiron Therapeutics. "GTA182 represents a significant research advancement for MTAP-deleted tumors. Our preclinical data shows,It has demonstrated significant tumor suppression and shrinkage effects in multiple models, including the highly challenging glioblastoma (GBM)."We are very much looking forward to advancing this therapy into clinical trials and plan to submit an IND application to the U.S. FDA in 2025 to drive our global development program."
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