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Published on: November 10, 2017
Current Knowledge about the New Drug Firibastat in Arterial Hypertension
Emma Hansen1, Daniela Grimm1,2, Markus Wehland2
1Department of Biomedicine, Aarhus University, Ole Worms Allé 4, 8000 Aarhus, Denmark.
Insights
Firibastat, a novel antihypertensive drug, targets the brain renin-angiotensin system by inhibiting aminopeptidase A. Clinical trials indicate it is safe and well-tolerated for managing hypertension.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
- Neuroscience
Background:
- Hypertension is a major risk factor for cardiovascular disease.
- Current treatments include diuretics, ACE inhibitors, ARBs, and CCBs.
- Firibastat represents a new class of antihypertensive medication.
Purpose of the Study:
- To review current knowledge on firibastat for hypertension treatment.
- To investigate the mechanism of action of firibastat.
- To assess the safety and tolerability of firibastat.
Main Methods:
- Firibastat is a prodrug converted to active EC33 in the brain.
- EC33 inhibits aminopeptidase A, reducing angiotensin III production.
- Clinical trials in animals and humans were reviewed.
Main Results:
- Firibastat effectively lowers blood pressure by modulating the brain renin-angiotensin system.
- No severe adverse effects were reported in clinical trials.
- Firibastat demonstrated good tolerability and safety in hypertensive patients.
Conclusions:
- Firibastat is a promising new therapeutic agent for hypertension.
- Its unique mechanism targeting the brain RAS offers a novel approach.
- Further research may solidify its role in cardiovascular disease management.
Abstract:
Hypertension significantly increases the risk of cardiovascular disease. Currently, effective standard pharmacological treatment is available in the form of diuretics, ACE inhibitors, angiotensin II receptor blockers and calcium channel blockers. These all help to decrease blood pressure in hypertensive patients, each with their own mechanism. Recently, firibastat, a new first-in-class antihypertensive drug has been developed. Firibastat is a prodrug that when crossing the blood-brain barrier, is cleaved into two active EC33 molecules. EC33 is the active molecule that inhibits the enzyme aminopeptidase A. Aminopeptidase A converts angiotensin II to angiotensin III. Angiotensin III usually has three central mechanisms that increase blood pressure, so by inhibiting this enzyme activity, a decrease in blood pressure is seen. Firibastat is an antihypertensive drug that affects the brain renin angiotensin system by inhibiting aminopeptidase A. Clinical trials with firibastat have been performed in animals and humans. No severe adverse effects related to firibastat treatment have been reported. Results from studies show that firibastat is generally well tolerated and safe to use in hypertensive patients. The aim of this review is to investigate the current knowledge about firibastat in the treatment of hypertension.
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