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.
Highlights
Academic Editor: Arterial hypertension is one of the major risk factors in the development of cardiovascular disease
RB150 is well tolerated in healthy volunteers with a single oral administration up to 1250 mg
Firibastat is an aminopeptidase A (APA) inhibitor that inhibits the conversion of angiotensin II (Ang-II) to angiotensin III (Ang-III), and the systemic effects of Ang-III
Summary
Academic Editor: Arterial hypertension is one of the major risk factors in the development of cardiovascular disease. It is estimated by the World Health Organization (WHO) that 47% of ischemic heart disease cases and 54% of strokes are the consequence of hypertension (HT) [1]. Most often HT does not cause any symptoms, but the risk of serious cardiovascular complications such as myocardial infarction or stroke increases if a patient has high, uncontrolled blood pressure [2]. By lowering blood pressure (BP), the risks associated with HT can be reduced. Quantum Genomics is a biopharmaceutical company that over the past few years, has developed the new first-inclass drug firibastat as a treatment for HT. This review will investigate the current knowledge about firibastat in HT, its mechanisms of action and pharmacological effects
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