Talabostat

Abstract

Talabostat mesilate is an orally active, specific inhibitor of dipeptidyl peptidases, including tumor-associated fibroblast activation protein. However, by an independent mechanism, talabostat also stimulates the upregulation of cytokines and chemokines to engender a tumor-specific host immune response, thus giving it a unique dual mechanism of action. In clinical trials, talabostat has demonstrated significant activity, including achieving complete responses in patients with non-small-cell lung cancer and malignant melanoma.