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Related Experiment Videos

Is there a future for renin inhibitors?

N D Fisher1, N K Hollenberg

  • 1Departments of Radiology and Medicine, Brigham and Womens Hospital and Harvard Medical School, Boston, MA, USA. nfisher@partners.org

Expert Opinion on Investigational Drugs
|February 28, 2001
PubMed
Summary

Renin inhibition, a promising approach to blocking the renin-angiotensin system, has stalled due to synthesis costs and bioavailability issues. Despite setbacks, renin inhibitors still hold significant therapeutic potential.

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Area of Science:

  • Pharmacology
  • Cardiovascular system
  • Drug development

Background:

  • The renin-angiotensin system (RAS) is a key regulator of blood pressure.
  • Pharmacological interruption of RAS can occur at ACE, AT1 receptor, or renin.
  • Renin inhibition, though logical, has lagged behind other RAS-targeting strategies.

Purpose of the Study:

  • To review the reasons for the slow evolution of renin inhibition.
  • To discuss the potential of renin inhibitors in modern pharmacotherapy.

Main Methods:

  • Review of historical development and current status of renin inhibitors.
  • Analysis of challenges including synthesis, bioavailability, and competition.
  • Exploration of novel approaches like x-ray crystallography for drug design.

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Main Results:

  • Renin inhibitor development has faced significant challenges, leading to program closures.
  • High synthesis costs and bioavailability issues have hampered progress.
  • The success of Angiotensin II (AngII) antagonists has overshadowed renin inhibition.

Conclusions:

  • The therapeutic potential of renin inhibitors is underestimated.
  • Novel approaches, such as structure-based design using x-ray crystallography, could revitalize renin inhibitor development.
  • Renin inhibition remains a promising, albeit under-explored, therapeutic strategy for RAS modulation.