EP102 / Epics Therap - LARVOL DELTA

Mechanistic perspectives and clinical translation for EP102, a METTL3 inhibitor arresting plasticity and adaptive stress responses in solid tumors (EORTC-NCI-AACR 2026) - "Abstract will be available as of 4 November (with consent of the author)"

Clinical • Oncology • Solid Tumor • METTL3

EP102: Pharmacological inhibition of METTL3 is effective as a monotherapy and potentiates radiation therapy in pancreatic adenocarcinoma via DNA damage and stemness modulation (AACR 2026) - "Together, these findings support a model where EP102 impairs m6A-dependent repair and survival pathways, and radiation potentiates this disruption, driving synergistic antitumor activity. These findings validate METTL3 as a therapeutic target and provide a strong rationale for combining EP102 with radiotherapy in pancreatic cancer."

Monotherapy • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • BRCA1 • CHEK2 • MCL1 • METTL3

A study to test the safety and efficacy of EP102 in patients with advanced solid tumours (clinicaltrialsregister.eu) - P1 | N=92 | Recruiting | Sponsor: Epics Therapeutics

New P1 trial • Oncology • Solid Tumor

Optimization of METTL3 Inhibitors for the Treatment of Solid Tumors and AML. (PubMed, J Med Chem) - "This research culminates in the discovery of EP102, a compound with a clear selectivity profile and a favorable ADME/PK profile in addition to robust efficacy in AML and solid tumor models. EP102 has entered clinical development for the treatment of advanced solid tumors."

Journal • Acute Myelogenous Leukemia • Oncology • Solid Tumor • METTL3

EP102: Pharmacological Inhibition of METTL3 causes tumor growth inhibition and prolongs survival in preclinical models of NSCLC, ovarian and squamous cell carcinoma (AACR 2024) - "The current results extend the application of METTL3 inhibitors to include the treatment of various types of solid tumors. The efficacy of M3i as a single-agent on tumor growth inhibition and survival advances the validation of METTL3 as a cancer target and provides additional evidence for the applicability of mRNA epigenetic mechanisms to the treatment of solid tumors."

Preclinical • Hypopharyngeal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • Squamous Cell Carcinoma • METTL3

EP102: pharmacological inhibition of METTL3 in tumor growth inhibition and comparative efficacy in combination with anti-PD1 or PARP inhibitors (AACR 2025) - "METTL3 is the RNA methyltransferase predominantly responsible for the addition of N-6-methyladenosine (m6A), the most abundant epigenetic modification to mRNA. SKOV3 is an HR-proficient tumor known to be less sensitive to PARP inhibitors; in a final study, M3i-B effectively prolonged survival in the SKOV3 model in NSG mice (orthotopic implant) and further demonstrated heightened efficacy when tested in combination with Olaparib (50 mg/kg, PO, QD) in data complemented by the resolution of various downstream biomarkers. The current results extend the application of METTL3 inhibitors as a single-agent in the treatment of selected tumors and further suggest that METTL3 inhibitors may be ideally combined with cancer therapies targeting DNA damage response mechanisms, such as PARP inhibitors, as a refined strategy for treatment of solid tumors."

Clinical • Combination therapy • IO biomarker • B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor • Triple Negative Breast Cancer • CD34 • METTL3

EP102: Pharmacological Inhibition of METTL3 arrests tumor growth in NSCLC adenocarcinoma; comparative data versus an EGFR inhibitor. (AACR-NCI-EORTC 2025) - "The aim of the current study is to evaluate the efficacy of EP102, in comparison to an EGFR inhibitor (afatinib), in non-small cell lung adenocarcinoma (NSCLC) both in vitro and in a mouse tumor model. These results demonstrate the efficacy of EP102 in the treatment of NSCLC and provide insight into the potential therapeutic benefit of combining a METTL3 inhibitor with an EGFR inhibitor. Our findings advance the validation of METTL3 as a cancer target and provide additional evidence for the applicability of mRNA epigenetic mechanisms to the treatment of solid tumors."

Late-breaking abstract • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • METTL3 • STAT3

EP102 Safety and Efficacy in METTL3 Modulation in Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=48 | Recruiting | Sponsor: Epics Therapeutics

Monotherapy • New P1 trial • Solid Tumor

EP102: Pharmacological inhibition of METTL3 arrests tumor progression and prolongs survival in CDX and PDX models of AML (AACR 2023) - "In an orthotopic, patient-derived xenograft model of AML (LEXF 41283, intratibial implantation, female NSG mice), M3i (30 mg/kg, i.p., QDx91 days) significantly prolonged survival (p<0.01, relative to vehicle control) with a commensurate absence of hCD45+ cells following compound treatment. These results confirm that the pharmacological inhibition of METTL3 is a viable strategy for the treatment of AML and support the additional exploration of the role of METTL3 inhibitors in alternate blood cancers as well as solid tumors."

Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • Solid Tumor • METTL3 • PTPRC