Given their pivotal role in cell survival, Bcl-2 family proteins are attractive targets for cancer therapy. BH3 mimetics are small molecules that mimic the activity of BH3-only proteins, promoting apoptosis by inhibiting anti-apoptotic Bcl-2 proteins. Venetoclax (ABT-199) is a BH3 mimetic that specifically targets Bcl-2 and has shown significant efficacy in treating chronic lymphocytic leukemia (CLL) and other hematologic malignancies.