APG-1252 is a novel, highly potent, small molecule drug designed to restore apoptosis through selective inhibition of the Bcl-2 and Bcl-xL proteins. Bcl-xL gene mutation and overexpression have been reported in many tumor types, including small cell lung cancer (SCLC). In preclinical studies with APG-1252, antitumor activity is observed in SCLC, lymphoma, colorectal cancer and metastatic breast cancer. With high potency and sub-nanomolar binding affinity to Bcl-2 proteins, APG-1252 minimizes platelet toxicity by design, has a favorable PK/PD profile and a potentially wider therapeutic window compared to the only other Bcl-2/Bcl-xL inhibitor in clinical development. We are conducting two Phase I trials in advanced cancers in the U.S. and Australia, and a Phase I/II trial in SCLC in China.
APG-1252
A Bcl-2/Bcl-xL dual inhibitor in Phase I for SCLC, lymphoma and solid tumors
