Ascentage Pharma, a global biopharmaceutical company engaged in developing novel therapies for cancers, chronic hepatitis B (CHB), and age-related diseases, today announced that its novel inhibitor of the embryonic ectoderm development (EED) protein, APG-5918, has been cleared by the US Food and Drug Administration (FDA) to enter a first-in-human (FIH) study that will assess the safety, pharmacokinetics, and preliminary efficacy of APG-5918 in patients with solid tumors or hematologic malignancies.

This multicenter, open-label Phase I study is designed to assess the safety and tolerability, and determine the dose-limiting toxicity, maximum tolerated dose, and recommended Phase II dose (RP2D) of orally administered APG-5918. Prof. Joseph Paul Eder, Clinical Director of the Early Drug Development Program at Yale Cancer Center will be the Principal Investigator of this multicentric clinical trial.

EZH2, which is highly expressed in multiple tumors in humans, was found to promote the development and progression of tumors, and the targeted inhibition of EZH2's methyltransferase activity has already been proven as an effective mechanistic approach for cancer treatment. However, the secondary mutation of EZH2 may lead to acquired drug resistances, while the homologous EZH1 also has methyltransferase activity that could limit the effects of EZH2 inhibitors.

Discovered and developed by Ascentage Pharma, APG-5918 is an orally active, potent, selective, small-molecule EED inhibitor with high binding affinity. As an allosteric inhibitor, APG-5918 selectively binds to the EED protein. By regulating tumor epigenetics and microenvironment, APG-5918 can potentially overcome tumor resistance and deliver complete and durable tumor regression.

Dr. Yifan Zhai, Chief Medical Officer of Ascentage Pharma, commented, "I am excited that we are poised to initiate the FIH study of APG-5918 under the leadership of Prof Paul Eder. In preclinical studies, APG-5918 showed potent binding activity with the EED protein, in vitro antiproliferative activity, and in vivo antitumor activity."

"We look forward to advancing the clinical development of APG-5918 to hopefully bring clinically meaningful benefits to patients as early as possible", added Prof Paul Eder.