Drug intelligence / Profile preview

talabostat + rituximab

Development stage
Unknown
Lead developer
BioXcel Therapeutics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

**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.

Other names
talabostat + rituxanPT-100 + rituximabPT-100 + rituxan
02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)CD20 (B-lymphocyte antigen CD20)DPP9 (Dipeptidyl Peptidase 9)DPP8 (Dipeptidyl peptidase 8)FAP (Fibroblast activation protein alpha)

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