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Endothelin-receptor antagonists: current and future perspectives.

Ray1, Hegde, Chugh

  • 1Cardiovascular Pharmacology Laboratory, New Drug Discovery Research, Ranbaxy Laboratories Ltd, R&D II, Sector 18, Udyog Vihar, Haryana, Gurgaon, India

Drug Discovery Today
|October 6, 2000
PubMed
Summary
This summary is machine-generated.

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Endothelin-receptor antagonists show promise but face potency challenges compared to ACE inhibitors like enalapril. Further research is needed to optimize their use in various therapeutic areas.

Area of Science:

  • Pharmacology
  • Cardiovascular Medicine

Background:

  • Endothelin-receptor antagonists (ERAs) development has faced challenges in becoming new drug entities.
  • Bosentan is the only ERA currently in Phase III clinical trials.

Purpose of the Study:

  • Review preclinical data on ERAs.
  • Analyze clinical data for bosentan, focusing on its potency.
  • Explore potential therapeutic areas for ERAs.

Main Methods:

  • Review of preclinical data on select endothelin-receptor antagonists.
  • Analysis of clinical trial data for bosentan.
  • Comparative efficacy assessment with angiotensin converting enzyme (ACE) inhibitors.

Main Results:

  • Bosentan, while efficacious, demonstrates lower potency than enalapril in hypertensive patients.

Related Experiment Videos

  • The article discusses reasons for bosentan's observed low potency.

    • Conclusions:

    • Endothelin-receptor antagonists require further development to overcome potency limitations.
    • Identifying optimal therapeutic applications is crucial for ERA success.