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**AT-101 + rituximab** is an investigational combination therapy comprising the small molecule AT-101 and the monoclonal antibody rituximab. **AT-101** (a BH3 mimetic, also known as R-(–)-gossypol acetic acid) is a small molecule inhibitor that binds and inhibits anti-apoptotic Bcl-2 family proteins (Bcl-2, Bcl-xL, Mcl-1), thereby promoting apoptosis in cancer cells[1][2]. **Rituximab** is a chimeric monoclonal antibody directed against CD20, a protein present on the surface of B cells, leading to their depletion via various immune-mediated mechanisms. This combination has been investigated, particularly in relapsed or refractory chronic lymphocytic leukemia (CLL), showing enhanced pro-apoptotic and anti-tumor effects compared to either agent alone, with a focus on overcoming apoptosis resistance mediated by Bcl-2 proteins[1][2]. Both drugs are administered in cycles, with AT-101 delivered orally (various dosing regimens) and rituximab intravenously[1][2]. AT-101 is developed by Ascenta Therapeutics, and rituximab is marketed by Roche and Biogen.
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