BCL-2, as an important protein regulating the cell survival, was discovered in a study of t(14;18) mutant follicular lymphoma 30 years ago. Venetoclax is the first BCL-2 inhibitor drug with small molecules of high BCL-2 selectivity and oral bioavailability. Venetoclax binds to BCL-2 protein directly, replaces precursor apoptotic proteins and triggers mitochondria by membrane cell permeabilization and activation of caspases that help restore the process of apoptosis. In 2017, following the successful approval of venetoclax for the treatment of chronic lymphocytic leukemia, the US FDA also approved the venetoclax use with azacitidine or decitabine, or with a low-dose cytarabine for the treatment of acute myeloid leukemia in patients not eligible for standard chemotherapy. Those new treatment combinations provide a safer and more effective option to treat patients with acute myeloid leukemia.