GTA182 / GT Apeiron Therap - LARVOL DELTA

First-in-human phase I study of GTA182, a novel MTA-cooperative PRMT5 inhibitor, in patients with MTAP-deleted advanced non-small cell lung cancer (ESMO Asia 2025) - P | "GTA182 demonstrated a favorable safety profile and encouraging antitumor activity in MTAP-deleted NSCLC, with emerging evidence of intracranial activity."

Clinical • First-in-human • Late-breaking abstract • Metastases • P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Thoracic Cancer • MTAP

Apeiron Therapeutics Presents First-in-Human Data from Phase 1 Clinical Trial of GTA182 in MTAP-Deleted Advanced Non-Small Cell Lung Cancer at the ESMO Asia Congress 2025 (The Manila Times) - "As of October 9, 2025, the data cutoff, 41 subjects with MTAP-deleted advanced solid tumors were treated at doses ranging from 20 to 450 mg once daily. This was a heavily pre-treated patient population representative of the genomic setting, and the maximum tolerated dose had not been reached. GTA182 was generally well tolerated, with the most frequent treatment-related adverse events being anemia (51.2%), decreased appetite (43.9%), and asthenia (39.0%)."

P1 data • Non Small Cell Lung Cancer

GTA182: A potentially best-in-class, MTA-cooperative PRMT5 inhibitor for MTAP-deleted advanced solid tumors (AACR 2025) - "GTA182 represents a highly selective, MTA-cooperative PRMT5 inhibitor with significant preclinical efficacy and a broad therapeutic window. GTA182 is now advancing through phase 1 trials with the aim to establish safety, pharmacokinetics, and efficacy in MTAP-deleted advanced tumors. With the potential to safely address both CNS and non-CNS malignancies, GTA182 is positioned to emerge as a differentiated therapeutic in precision oncology."

Metastases • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Osteosarcoma • Sarcoma • Solid Tumor • CDKN2A • MTAP

GT Apeiron Announces Development Candidate Nomination of Brain Penetrant PRMT5 Inhibitor, GTA182, for the Potential Treatment of MTAP-Deleted Solid Cancers (GlobeNewswire) - "GT Apeiron Therapeutics...today announced the development candidate nomination of GTA182, a brain penetrant protein arginine methyltransferase 5 (PRMT5) inhibitor that exhibits methylthioadenosine (MTA)....This selectivity is expected to provide a more effective and safer treatment option for patients with MTAP-deleted cancers....In preclinical studies, Apeiron has demonstrated that GTA182 is a potent and selective PRMT5 inhibitor exhibiting greater than 100-fold selectivity for MTAP deleted tumor cell lines. GTA182 is brain penetrant and has demonstrated tumor growth inhibition and tumor regression in in vivo pre-clinical models of glioblastoma (GBM) as well as non-CNS murine cancer models with MTAP deletions....Apeiron plans to file an Investigational New Drug (IND) application in mid-2024."

IND • Pipeline update • Preclinical • Oncology