APG-2575 created by Ascentage Pharma is one of the rare Bcl-2 selective inhibitors in active clinical studies apart from Venetoclax.

Ascentage Pharma has reportedly announced that it has dosed the first patient in a phase I medical study of APG-2575, a new Bcl-2 selective inhibitor, for treating hematologic malignancies in China. The company also has a continuing multi-center phase I APG-2575 dose-escalation trial as a single agent in Australia and the United States. APG-2575 is anticipated to potentially be the first Bcl-2 inhibitor made in China.

For the record, APG-2575 is an innovative, orally managed Bcl-2 selective inhibitor. It is created to heal hematologic malignancies through selective blocking Bcl-2 to recreate the regular apoptosis process in cancer cells.

Reportedly, the founding member of the Bcl-2 family proteins is Bcl-2. The Bcl-2 family proteins are most prominent for their significant roles in regulating apoptosis by the development of heterodimers through pro-apoptotic proteins (BAD, BIM and many others). It is complicated to create a drug which affects Bcl-2 family protein due to the hydrophobic and very large Bcl-2 protein interfaces. The promoted Bcl-2 inhibitor venetoclax/ABT-199 accepted by the U.S. FDA in April 2016 has legalized the medical basis for more targeted drug development. APG-2575 created by Ascentage Pharma is one of the rare Bcl-2 selective inhibitors in active clinical studies apart from Venetoclax.

Sources claimed that the Phase I trial is created to evaluate the tolerance and safety of APG-2575 in patients enduring hematologic malignancies. The trial is also designed to check the recommended Phase II dose (RP2D) or maximal tolerated dose (MTD) of APG-2575. Patients with acute Non-Hodgkin's Lymphoma (NHL) and Acute Myelogenous Leukemia (AML) have been Included in this trial. Presently, the first enrolled patient has been medicated during the initial stage of dose-escalation.

Ascentage Pharma has reportedly released numerous preclinical research outcomes of APG-2575 during the annual meeting of 2019 American Association for Cancer Research (AACR). The results have shown the potential in combination therapy.

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