talabostat

Talabostat is an orally available small molecule inhibitor of dipeptidyl peptidases—including dipeptidyl peptidase 4 (DPP4), dipeptidyl peptidase 8 (DPP8), dipeptidyl peptidase 9 (DPP9), and fibroblast activation protein (FAP). It acts as an antineoplastic and immunomodulatory agent. By inhibiting these proteases, talabostat stimulates cytokine and chemokine production and enhances both innate and adaptive immune responses against tumors. This dual mechanism includes direct inhibition of tumor-associated FAP as well as upregulation of immune mediators to promote T-cell immunity. Talabostat has been investigated in various cancers including non-Hodgkin's lymphoma, lymphoid leukemia, lung cancer (including non-small cell lung cancer), melanoma, pancreatic cancer, prostate cancer (notably small cell neuroendocrine subtype), adenocarcinoma, acute myeloid leukemia, myelodysplastic syndromes, soft tissue sarcoma, solid tumors generally—including in combination with checkpoint inhibitors such as pembrolizumab[1][2][3][4][5][6].

Brand names

PT-100PT100PT 100

Other names

talabostat mesylatetalabostat mesilate[(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid