On July 14, 2019 Ascentage Pharma, a globally-focused, clinical-stage biotechnology company engaged in developing novel therapies for cancers, hepatitis B virus and age-related diseases, reported that the company recently dosed the first patient successfully in a Phase I clinical trial of APG-2575, a novel Bcl-2 selective inhibitor, for the treatment of hematologic malignancies in China (Press release, , JUL 14, 2019, View Source [SID1234537515]). The Company also has an ongoing multi-center Phase I dose-escalation study of APG-2575 as a single agent in the United States and Australia. APG-2575 could potentially be the first China-made Bcl-2 inhibitor.

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APG-2575 is a novel, orally administered Bcl-2 selective inhibitor. It is designed to treat hematologic malignancies by selective blocking Bcl-2 to restore the normal apoptosis process in cancer cells.

Bcl-2 is the founding member of the Bcl-2 family proteins which are most notable for their critical roles in the regulation of apoptosis through the formation of heterodimers with pro-apoptotic proteins (BIM, BAD and most others). Due to the very large and hydrophobic interfaces of Bcl-2 proteins, it is difficult to develop a drug that targets Bcl-2 family protein. The marketed Bcl-2 inhibitor venetoclax/ABT-199 approved by the U.S. FDA in April 2016 has validated the clinical basis for further targeted drug development. Ascentage Pharma’s APG-2575 is one of the few Bcl-2 selective inhibitors in active clinical trials other than Venetoclax.

This Phase I trial is designed to assess the safety and tolerance of APG-2575 in patients with hematologic malignancies and confirm the maximal tolerated dose (MTD) or recommended Phase II dose (RP2D) of APG-2575. Included in this trial are patients with acute myelogenous leukemia (AML), non-Hodgkin’s lymphoma (NHL). Currently, the first patient enrolled in China has been dosed at Institute of Hematology, Blood Disease Hospital of Chinese Academy of Medical Sciences during the first stage of dose-escalation.

The Phase I dose-escalation clinical trial of APG-2575 in the United States and Australia is being conducted at several academic institutions including MD Anderson Cancer Center and Mayo Clinic. Included in this trial are patients with various types of blood cancer, such as CLL, NHL, MM, AML. At present, 4 dose cohorts have been completed in the United States and Australia. Preliminary data suggested that APG-2575 was well tolerated and safe, it had promising anti-tumor activity in the treatment of relapsed/refractory CLL.

During the 2019 American Association for Cancer Research (AACR) (Free AACR Whitepaper) annual meeting, Ascentage Pharma released several preclinical research results of APG-2575, which demonstrated the potential in combination therapy.

"APG-2575 is a key product in our development pipeline of apoptosis. Initiating the clinical trial in China represents a new step in our global clinical development. We believe that APG-2575 may provide more therapy options to patients with blood diseases," said Dr. Dajun Yang, Chairman and CEO of Ascentage Pharma.

About APG-2575
APG-2575 is a novel, orally administered Bcl-2 selective inhibitor developed by Ascentage Pharma. It is designed to treat hematologic malignancies by selective blocking Bcl-2 to restore the normal apoptosis process in cancer cells.

The Company recently initiated a phase I clinical trial of APG-2575 in China, which is the first domestic Bcl-2 selective inhibitor entered the clinical stage. Ascentage previously has initiated a multi-center Phase I dose-escalation study of APG-2575 as a single agent in multiple hematologic malignancies in the United States and Australia in August 2018.