Phase II trial of talabostat and docetaxel in advanced non-small cell lung cancer

Clin Oncol (R Coll Radiol). 2009 Aug;21(6):464-72. doi: 10.1016/j.clon.2009.04.007. Epub 2009 Jun 5.


Aims: Currently available therapies do improve survival in advanced stage non-small cell lung cancer (NSCLC), but only to a limited degree. Talabostat mesilate (PT-100) is an orally available amino boronic dipeptide that specifically inhibits dipeptidyl peptidases (including fibroblast activation protein) and enhances an immune response. The aim of this study was to determine the efficacy and safety of talabostat in NSCLC patients.

Materials and methods: A phase II trial was conducted to evaluate talabostat in combination with docetaxel in patients with advanced NSCLC after failure of previous platinum-based chemotherapy. In total, 42 patients were enrolled.

Results: Talabostat was well tolerated. Two patients achieved a partial response and one achieved a complete response.

Conclusion: There was no evidence that talabostat enhanced the clinical activity of docetaxel in patients with NSCLC.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Boronic Acids / administration & dosage
  • Boronic Acids / adverse effects
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Dipeptides / administration & dosage
  • Dipeptides / adverse effects
  • Docetaxel
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / pathology
  • Middle Aged
  • Taxoids / administration & dosage
  • Taxoids / adverse effects


  • Boronic Acids
  • Dipeptides
  • Taxoids
  • Docetaxel
  • talabostat