Endothelin receptor antagonists

World J Urol. 2005 Feb;23(1):19-27. doi: 10.1007/s00345-004-0478-9. Epub 2005 Jan 15.

Abstract

Hormone refractory prostate cancer remains true to its middle name: it is largely refractory to attempts to delay its progression. New targets and new therapies are demanded. Through a review of the available literature on endothelin and several preclinical observations, the endothelin axis has emerged as one such target. In phase II and III clinical trials of atrasentan, a potent and selective endothelin receptor A subtype (ET(A)) antagonist, disease progression was delayed in some men. This well tolerated, oral agent may help convert advanced prostate cancer to a more chronic disease. This review will discuss the endothelin axis, preclinical rationale and some of the available clinical trial data on this promising new approach.

Publication types

  • Review

MeSH terms

  • Apoptosis / drug effects
  • Atrasentan
  • Biomarkers, Tumor / metabolism
  • Clinical Trials as Topic
  • Disease Progression
  • Endothelin Receptor Antagonists*
  • Endothelin-1 / antagonists & inhibitors
  • Endothelin-1 / metabolism
  • Humans
  • Male
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / pathology
  • Pyrrolidines / therapeutic use*
  • Receptors, Endothelin / metabolism
  • Treatment Outcome

Substances

  • Biomarkers, Tumor
  • Endothelin Receptor Antagonists
  • Endothelin-1
  • Pyrrolidines
  • Receptors, Endothelin
  • Atrasentan