Apeiron Therapeutics Unveils Promising Phase I Data of GTA182, a Brain-Penetrant MTA-Cooperative PRMT5 Inhibitor, at ESMO Asia 2025
Apeiron
Pharmaceutical R&D Developer
Apeiron TherapeuticsFirst-in-human Phase I Clinical Data
GTA182 Clinical Data Stuns Debut
In2025 ESMO AsiaAt the conference,ApeironAnnouncement of PRMT5 InhibitorGTA182Treatment of MTAP-Deleted Advanced Non-Small Cell Lung CancerFor the first timePhase I Clinical Trial Data in Humans
GTA182 demonstrated good safety and dose-proportional pharmacokinetic properties in Phase I clinical trials, along with potent inhibition of the PRMT5 pathway and early anti-tumor activity.
Preliminary results show that GTA182 has an objective response rate (ORR) of 57.1% in MTAP-deficient non-small cell lung cancer (NSCLC) patients and demonstrates intracranial activity.
01
GTA182 Phase I Clinical Data Global Premiere
2025Year12Month5Day
Apeiron( Apeiron Therapeutics)PublishedGTA182(Oral, with blood-brain barrier permeability)MTASynergyPRMT5Inhibitor) inMTAPAdvanced Solid Tumors with LossClinical1Latest in Phase TrialsData, including preliminary antitumor activity observed in non-small cell lung cancer.. The data is provided byThe Leading Researcher of the Trial、Apeiron TherapeuticsSea ChestDepartmentMedHospitalProfessor Lu ShunHeld in Singapore2025YearESMO Asia Congress(ESMO Asia)Above, presented in the form of an oral report.
02
The Differentiated Competitiveness of GTA182
CEO of Apeiron TherapeuticsDr. Li MingxiSaid: "We are pleased to share the clinical data of GTA182 for the first time. In patients with advanced solid tumors lacking MTAP, the drug has demonstratedSignificant Target Binding Ability、Early Tumor Response, andEncouraging Intracranial Activity。
These results highlightGTA182As a differentiated MTA-cooperative PRMT5 inhibitor with brain penetrability specifically designed for MTAP-deleted tumors, the accumulating data on safety, pharmacokinetics/pharmacodynamics, and anti-tumor activity strongly support our continued advancement in dose exploration and cohort expansion studies.
03
Threefold Advantages Highlighted
✅ GTA182 was generally well tolerated.
The most common treatment-related adverse event was anemia[51.2%], decreased appetite [43.9%], and fatigue [39.0%].
The incidence of Grade ≥3 adverse events was 26.8%, consistent with expectations for selective PRMT5 inhibitors.
? Pharmacokinetics：Good dose correlation
Pharmacokinetic analysis showed that drug exposure increased proportionally with escalating doses up to 450 mg, with low interpatient variability.
AndGTA182The mechanism of action is consistent with the research observations.GTA182Potent inhibition of the PRMT5 pathway – at active doses [100-450 mg], plasma SDMA levels decreased on average71.8%[95% CI: 69.7%–73.8%]. The aforementioned pharmacodynamic effects are correlated with systemic exposure, providing support for the ongoing dose optimization efforts.
? Impressive Anti-Tumor Activity
Among the 30 evaluable subjects,GTA182Showing encouraging and lastingAntitumor Activity：
Objective Response Rate【ORR] Da30.0%[95% CI:14.7%–49.4%]
Disease Control Rate [DCR] Da83.3%[95% CI:65.3%–94.4%]
InMTAP-Deficient Non-Small Cell Lung Cancer Subgroup[n=14] in China,The efficacy is more prominent.：
[ORR] Increased to 57.1% [95% CI: 28.9%–82.3%]
【DCR】Increased to85.7%[95% CI:57.2%–98.2%]
And tumor responses were observed at different dose levels.
Notably, among the 3 patients with baseline brain metastases, significant intracranial tumor shrinkage was observed in 2 cases, consistent with the unique brain-penetrating properties of GTA182.
04
About GTA182
? GTA182It is Apeiron Therapeutics through itsAI-Guided Drug Discovery PlatformA small-molecule compound independently developed by Apeiron Therapeutics is currently in Phase I clinical trials.
High Selectivity
In preclinical studies, Apeiron demonstratedGTA182It is a highly efficient and selective PRMT5 inhibitor, exhibiting over 100 times selectivity for MTAP-deficient tumor cell lines.
Blood-Brain Barrier Advantage
GTA182With blood-brain barrier penetrability, it has demonstrated inhibition and reduction of tumor growth in preclinical in vivo models, including glioblastoma [GBM].】and various MTAP-deficient non-CNS tumor models.
05
About Apeiron
? ApeironLeveraging AI to Optimize the Entire Drug Discovery Process — From Target Selection to Clinical Trials, Redefining Medical Innovation. With Two Strategic R&D Centers Located in the San Francisco Bay Area and Shanghai, Apeiron Therapeutics Integrates Top Talent and Cutting-Edge Technologies Across Multiple Regions to Drive Biomedical Innovation. We Are Committed to Delivering Breakthrough Therapies for Highly Unmet Medical Needs.
Investment and Media Cooperation
Silinda Neou
Email
Silinda@apeiron-bio.us
Official Website
https://www.apeiron-bio.com
