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**Talabostat + rituximab** is a combination therapy under investigation primarily for hematologic malignancies, notably chronic lymphocytic leukemia (CLL) that is refractory or relapsed after standard therapies including fludarabine and rituximab. Talabostat (also known as PT-100) is an oral, small-molecule inhibitor of dipeptidyl peptidases such as fibroblast activation protein (FAP) and CD26. It acts by inhibiting enzymatic degradation of cytokines and chemokines, thus boosting innate and adaptive T-cell immunity and stimulating hematopoietic progenitor cell growth. Rituximab is a monoclonal antibody targeting the CD20 antigen on B cells, mediating B-cell cytotoxicity via immune effector mechanisms. Preclinical models and phase I/II studies suggest that talabostat may enhance the antibody-dependent cellular cytotoxicity of rituximab and increase immune-mediated tumor cell clearance.
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