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Related Experiment Videos

Nonpeptide endothelin antagonists in clinical development.

Chengde Wu1, E. Radford Decker, George W. Holland

  • 1Texas Biotechnology Corporation, Houston, Texas, U.S.A. cwu@tbc.com

Drugs of Today (Barcelona, Spain : 1998)
|May 17, 2003
PubMed
Summary

Endothelin receptor antagonists, including ET(A)-selective and dual ET(A)/ET(B) blockers, are being evaluated for serious diseases like hypertension and cancer. This review highlights small-molecule antagonists in clinical trials, focusing on sitaxsentan.

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Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Cardiovascular Research

Background:

  • Endothelins (ET-1, ET-2, ET-3) are peptides regulating physiological and pathological processes via G-protein-coupled receptors.
  • Two receptors, ET(A) and ET(B), have been identified, with differing affinities for endothelin isoforms.
  • Endothelin's role in diseases like hypertension, heart failure, and cancer has spurred research into antagonists.

Purpose of the Study:

  • To review small-molecule endothelin antagonists under clinical evaluation.
  • To highlight ET(A)-selective and nonselective ET(A)/ET(B) antagonists.
  • To present the medicinal chemistry and clinical data for sitaxsentan.

Main Methods:

  • Review of clinical trial data for endothelin antagonists.

Related Experiment Videos

  • Medicinal chemistry analysis of small-molecule antagonists.
  • Focus on sitaxsentan's development and evaluation.

    • Main Results:

    • Numerous endothelin antagonists with sulfonamide or triaryl carboxylic acid scaffolds have been developed.
    • Several ET(A)-selective and nonselective ET(A)/ET(B) antagonists have advanced to clinical trials.
    • Sitaxsentan, a notable antagonist, has undergone animal and human clinical evaluation.

    Conclusions:

    • Small-molecule endothelin antagonists show promise for treating various diseases.
    • Ongoing clinical trials are assessing the efficacy and safety of these compounds.
    • Sitaxsentan represents a significant development in endothelin antagonist research.