Talabostat.
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.
Cunningham
Charles Casey
CC
Mary Crowley Medical Research Center, Dallas, Texas 75201, USA. ccunningham@mcmrc.com
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D001897:Boronic Acids / Q000494:pharmacology / Q000627:therapeutic use*; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy / Q000201:enzymology / Q000276:immunology; D004151:Dipeptides; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / Q000037:antagonists & inhibitors*; D015507:Drugs, Investigational / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D008545:Melanoma / Q000188:drug therapy / Q000201:enzymology / Q000276:immunology; D011759:Pyrrolidines / Q000494:pharmacology / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D001897:Boronic Acids; D004151:Dipeptides; D015507:Drugs, Investigational; D004791:Enzyme Inhibitors; D011759:Pyrrolidines; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases; C514044:talabostat