Related Experiment Videos
Renin inhibitors: discovery and development. An overview and perspective
1Cardiovascular Research Division, Abbott Laboratories, Abbott Park, IL 60064.
American Journal of Hypertension
|October 1, 1989
Summary
Renin inhibitors offer a targeted approach to managing hypertension and heart failure by blocking the initial step in angiotensin II production. This may lead to fewer side effects compared to current treatments like ACE inhibitors.
Area of Science:
- Cardiovascular Pharmacology
- Renin-Angiotensin System (RAS) Modulation
Background:
- Pharmacological suppression of the renin angiotensin system (RAS) via angiotensin-converting enzyme (ACE) inhibition is effective for hypertension and heart failure.
- Renin initiates the RAS cascade by acting on angiotensinogen, preceding ACE activity.
Purpose of the Study:
- To explore the therapeutic potential of renin inhibitors as a targeted treatment for cardiovascular disorders.
- To highlight the advantages of interrupting the RAS at the renin-dependent step.
Main Methods:
- Review of advancements in the discovery and synthesis of renin inhibitors.
- Evaluation of laboratory and early clinical data on renin inhibitor efficacy and bioavailability.
Main Results:
- Potent dipeptide renin inhibitors demonstrate efficacy as hypotensive agents in laboratory settings, particularly when administered intravenously.
- Ongoing efforts focus on enhancing oral bioavailability for therapeutic development.
Conclusions:
- Renin inhibitors offer a highly specific mechanism for RAS intervention, potentially reducing clinical side effects.
- Development of orally active renin inhibitors promises novel treatments for cardiovascular diseases and valuable research tools for RAS studies.