EZM8266 / Ipsen - LARVOL DELTA

Histone methyl-transferase G9a inhibition boosts the efficacy of immune checkpoint inhibitors in experimental hepatocellular carcinoma. (PubMed, Cell Rep Med) - "Using human and murine HCC cell lines and immunocompetent mouse models, we assess the antitumor effects of two G9a inhibitors, CM272 and EZM8266, combined with anti-PD1 therapy...In vivo, G9a inhibition synergizes with anti-PD1 therapy, suppresses tumor growth, and enhances CD8+ T cell infiltration. These findings support combining G9a inhibitors with immunotherapy in HCC."

Checkpoint inhibition • IO biomarker • Journal • Hepatocellular Cancer • Oncology • Solid Tumor • CD8 • CXCL10 • EHMT2 • IFNG

Antitumoral activity of the G9a inhibitor EZM8266 in hepatocellular carcinoma: potential for combination with immune checkpoint inhibitors (EASL-ILC 2023) - "G9a is confirmed as an effective druggable target in HCC. Pharmacological inhibition of G9a with EZM8266 antagonizes HCC cells growth and leverages the efficacy of ICIs. Our findings provide strong support for the combination immunotherapy with epigenetic drugs such as EZM8266 for HCC treatment."

Checkpoint inhibition • IO biomarker • Gastrointestinal Cancer • Hepatocellular Cancer • Hepatology • Immune Modulation • Oncology • Solid Tumor • CXCL10 • CXCL9

Antitumoral activity of the G9a inhibitor EZM8266 in hepatocellular carcinoma: potential for combination with immune checkpoint inhibitors (AEEH 2023) - No abstract available

Checkpoint inhibition • Gastrointestinal Cancer • Hepatocellular Cancer • Immune Modulation • Oncology • Solid Tumor

Antitumoral activity of the G9a inhibitor EZM8266 in hepatocellular carcinoma: potential for combination with immune checkpoint inhibitors (AEEH 2023) - No abstract available

Checkpoint inhibition • Gastrointestinal Cancer • Hepatocellular Cancer • Immune Modulation • Oncology • Solid Tumor

Epizyme announces positive pre-NDA meeting for tazemetostat for follicular lymphoma, pipeline updates and third quarter 2019 results (Businesswire) - "Epizyme has decided to refocus its preclinical program targeting G9a on other potential development candidates and discontinue development of EZM-8266. This decision was made after a review of development path implications of a preclinical toxicology finding of EZM-8266. The company is evaluating next steps for its G9a program to develop an oral, disease-modifying approach to treating a variety of hemoglobinopathies, including sickle cell disease."

Discontinued

Epizyme (EPZM) focuses on developing lead drug tazemetostat (Yahoo Finance) - "Epizyme also aims at completing IND-enabling studies on EZM8266, its G9a inhibitor designed to treat patients with sickle cell disease (SCD). It is on track to begin clinical development of the candidate in the second half of 2019 with a dose-finding and safety study."

New trial

Epizyme reports business progress and second quarter 2019 results (BioSpace) - "EZM8266 for Sickle Cell Disease: Epizyme anticipates beginning clinical development of EZM8266, a novel, first-in-class G9a inhibitor, with a Phase 1 clinical trial in the second half of 2019."

New P1 trial

Epizyme provides business update and reports first quarter 2019 financial results (Businesswire) - "Upon approval of an Investigational New Application (IND) for EZM8266 for the treatment of patients with sickle cell disease, Epizyme anticipates beginning clinical development in the second half of 2019 with a Phase 1 trial of EZM8266, a novel, first-in-class G9a inhibitor."

New P1 trial