Therapeutic development and current uses of BCL-2 inhibition
Andrew W Roberts
Hematology | AMER SOC HEMATOLOGY | Published : 2020
B-cell lymphoma 2 (BCL2) is a key protein regulator of apoptosis. It is variably highly expressed in many hematological malignancies, providing protection from cell death induced by oncogenic and external stresses. Venetoclax is the first selective BCL2 inhibitor, and the first of a new class of anticancer drug (BH3-mimetics) to be approved for routine clinical practice, currently in chronic lymphocytic leukemia (CLL) and acute myeloid leukemia (AML). To help understand the potential and limitations of this therapy, this brief review will touch on the history of development of venetoclax, dissect its mechanism of action, and summarize critical evidence for its approved use in the management ..View full abstract
Academic research in the Roberts laboratory has been supported over the last 20 years by grants from the National Health and Medical Research Council (NHMRC) of Australia, the US Leukemia & Lymphoma Society, Cancer Council of Victoria, Victorian Cancer Agency, Leukaemia Foundation of Australia, and the Snowdome Foundation.