Apeiron Therapeutics Announces First Patient Dosed in Phase 1a/b Trial of GTA182, a Brain-Penetrant PRMT5 Inhibitor for MTAP-Deficient Solid Tumors
Apeiron
Pharmaceutical R&D Developer
▎Edited by the WuXi AppTec content team
On November 19, Apeiron Therapeutics announced itsTargetingMTAPAdvanced Solid Tumors with LossThe GTA182 Phase 1a/b study successfully completed the enrollment of the first patient.This study aims to evaluate the safety, efficacy, and pharmacokinetic properties of GTA182 under multiple dose escalations, applicable toMTAPAdult patients with advanced solid tumors who are deficient, as a monotherapy or in combination with standard treatment.
GTA182 is a small molecule compound independently developed by Apeiron through its artificial intelligence (AI)-guided drug discovery platform. In preclinical studies, Apeiron demonstrated that GTA182 isA highly efficient and selective PRMT5 inhibitor, with over 100 times selectivity for MTAP-deficient tumor cell lines.. Importantly,GTA182 has the ability to penetrate the brain, in variousMTAPThe missing part includes the demonstration of inhibitory and shrinking effects on tumor growth in in vivo models of glioblastoma (GBM) and non-central nervous system tumors.。
The first-in-human Phase 1a/b clinical trial of GTA182 is an open-label, multi-center study covering dose escalation and dose expansion phases. The study will enroll patients with MTAP-deficient solid tumors, with the primary objective of evaluating the safety and tolerability of GTA182 and determining the optimal therapeutic dose.
Dr. Mingxi Li, CEO of Apeiron Therapeutics, stated: "The initiation of the GTA182 Phase 1a/b clinical trial is a significant milestone in the company’s development, marking the entry of our second drug candidate into clinical research."
Fred Aswad, Ph.D., Senior Vice President of Apeiron Therapeutics, stated:"GTA182 aims to overcome the limitations of existing second-generation PRMT5 inhibitors in terms of safety and efficacy, offering the potential for a transformative therapy for patients with limited treatment options."
[1] Apeiron | First Patient Successfully Enrolled in GTA182 Phase 1a/b Clinical Trial for the Treatment of MTAP-Deleted Solid Tumors. Retrieved Nov 19, 2024, from https://mp.weixin.qq.com/s/k1NFJdTdD99-jZ8krLIWyg
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