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Current Knowledge about the New Drug Firibastat in Arterial Hypertension

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 hyperten...

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Detalles Bibliográficos
Autores principales: Hansen, Emma, Grimm, Daniela, Wehland, Markus
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8836050/
https://www.ncbi.nlm.nih.gov/pubmed/35163378
http://dx.doi.org/10.3390/ijms23031459
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author Hansen, Emma
Grimm, Daniela
Wehland, Markus
author_facet Hansen, Emma
Grimm, Daniela
Wehland, Markus
author_sort Hansen, Emma
collection PubMed
description 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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spelling pubmed-88360502022-02-12 Current Knowledge about the New Drug Firibastat in Arterial Hypertension Hansen, Emma Grimm, Daniela Wehland, Markus Int J Mol Sci Review 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. MDPI 2022-01-27 /pmc/articles/PMC8836050/ /pubmed/35163378 http://dx.doi.org/10.3390/ijms23031459 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Hansen, Emma
Grimm, Daniela
Wehland, Markus
Current Knowledge about the New Drug Firibastat in Arterial Hypertension
title Current Knowledge about the New Drug Firibastat in Arterial Hypertension
title_full Current Knowledge about the New Drug Firibastat in Arterial Hypertension
title_fullStr Current Knowledge about the New Drug Firibastat in Arterial Hypertension
title_full_unstemmed Current Knowledge about the New Drug Firibastat in Arterial Hypertension
title_short Current Knowledge about the New Drug Firibastat in Arterial Hypertension
title_sort current knowledge about the new drug firibastat in arterial hypertension
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8836050/
https://www.ncbi.nlm.nih.gov/pubmed/35163378
http://dx.doi.org/10.3390/ijms23031459
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