Translating TRAIL-receptor targeting agents to the clinic

Cancer Lett. 2013 May 28;332(2):194-201. doi: 10.1016/j.canlet.2012.04.007. Epub 2012 Apr 21.


The extrinsic apoptotic pathway can be activated by the endogenous ligand TRAIL (Tumor Necrosis Factor (TNF)-Related Apoptosis-Inducing Ligand) by binding to the death receptors TRAIL-R1 and TRAIL-R2 on the cell surface. This pathway is currently evaluated as an anticancer treatment strategy. Both recombinant human TRAIL and several agonistic antibodies against TRAIL-R1 and R2 have been studied in single agent and combination studies and proved to be safe and well tolerated. In this article, the clinical studies published to date will be reviewed. Also, future perspectives and biomarker studies for selecting patients that will benefit from these agents will be discussed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antibodies, Monoclonal / therapeutic use
  • Antibodies, Monoclonal, Humanized
  • Apoptosis
  • Biomarkers, Tumor / metabolism
  • Cell Membrane / metabolism
  • Clinical Trials as Topic
  • Humans
  • Neoplasms / drug therapy*
  • Receptors, TNF-Related Apoptosis-Inducing Ligand / metabolism*
  • Recombinant Proteins / metabolism
  • Signal Transduction
  • TNF-Related Apoptosis-Inducing Ligand / therapeutic use


  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Biomarkers, Tumor
  • Receptors, TNF-Related Apoptosis-Inducing Ligand
  • Recombinant Proteins
  • TNF-Related Apoptosis-Inducing Ligand
  • TNFSF10 protein, human
  • mapatumumab