Talabostat

Expert Opin Investig Drugs. 2007 Sep;16(9):1459-65. doi: 10.1517/13543784.16.9.1459.

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.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Boronic Acids / pharmacology
  • Boronic Acids / therapeutic use*
  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Carcinoma, Non-Small-Cell Lung / enzymology
  • Carcinoma, Non-Small-Cell Lung / immunology
  • Dipeptides
  • Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / antagonists & inhibitors*
  • Drugs, Investigational / chemistry*
  • Drugs, Investigational / pharmacology
  • Drugs, Investigational / therapeutic use*
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use*
  • Humans
  • Melanoma / drug therapy
  • Melanoma / enzymology
  • Melanoma / immunology
  • Pyrrolidines / pharmacology
  • Pyrrolidines / therapeutic use*

Substances

  • Antineoplastic Agents
  • Boronic Acids
  • Dipeptides
  • Drugs, Investigational
  • Enzyme Inhibitors
  • Pyrrolidines
  • Dipeptidyl-Peptidases and Tripeptidyl-Peptidases
  • talabostat