The China National Medical Products Administration’s (NMPA) Centre for Drug Evaluation (CDE) has granted clearance for Ascentage Pharma’s investigational new drug (IND) application to begin a Phase I clinical trial of APG-5918 for patients with advanced solid tumours or haematologic malignancies. 

The open-label, multicentre, dose-escalation and dose-expansion trial will evaluate the safety, pharmacokinetics, and efficacy of oral doses of APG-5918 in these patients. 

A new, small-molecule embryonic ectoderm development (EED) protein inhibitor, APG-5918 was discovered and developed by Ascentage.

This therapy is said to be the first EED inhibitor developed locally to enter clinical development in the country.

APG-5918 can regulate the tumours’ epigenetics, as well as their microenvironment, and has a wider-ranging treatment potential to treat solid tumours, haematologic malignancies, and nononcologic conditions. 

According to the initial data, APG-5918 has in vitro antiproliferative activity in several tumour cell lines.

It also showed antitumor activity in EZH1-mutant B-cell non-Hodgkin lymphoma, IN1-negative malignant rhabdoid tumours, and BAP1-mutant mesothelioma and prostate cancer’s xenograft (PDX)/cell line-derived xenograft (CDX) models obtained from patients.

Ascentage Pharma chief medical officer Dr Yifan Zhai said: “This approval of the clinical study of APG-5918 in China came shortly after the clearance for the study in the US, hence signals major progress in Ascentage Pharma’s efforts to simultaneously advance clinical programs in China and the US and is also a strong testament to our global innovation capabilities.” 

In June this year, the company received IND clearance from the US Food and Drug Administration to commence the Phase I trial of APG-5918 for solid tumours or haematologic malignancies.