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Is there a future for renin inhibitors?
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
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.
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.
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.