[HTML][HTML] New approaches targeting the renin-angiotensin system: inhibition of brain aminopeptidase A, ACE2 ubiquitination, and angiotensinogen

E Lazartigues, C Llorens-Cortes, AHJ Danser - Canadian Journal of …, 2023 - Elsevier
Despite the availability of various therapeutic classes of antihypertensive drugs,
hypertension remains poorly controlled, in part because of poor adherence. Hence, there is …

Firibastat: an oral first-in-class brain aminopeptidase A inhibitor for systemic hypertension

J Khosla, WS Aronow, WH Frishman - Cardiology in Review, 2022 - journals.lww.com
Systemic hypertension is the leading cause of death and disability worldwide. The
management of hypertension is challenging in the high-risk patient population with high salt …

Efficacy and safety of Firibastat, a first-in-class brain aminopeptidase A inhibitor, in hypertensive overweight patients of multiple ethnic origins: A Phase 2, open-label …

KC Ferdinand, F Balavoine, B Besse, HR Black… - Circulation, 2019 - Am Heart Assoc
Background: Despite existing therapy, successful control of hypertension in the United
States is estimated at less than 50%. In blacks, hypertension occurs earlier, is more severe …

[HTML][HTML] Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: a review of clinical trials

SA Alomar, SA Alghabban, HA Alharbi… - Avicenna Journal of …, 2021 - thieme-connect.com
An unfortunate subset of hypertensive patients develops resistant hypertension in which
optimal doses of three or more first-line antihypertensive drugs fail to sufficiently control …

Targeting brain aminopeptidase A: a new strategy for the treatment of hypertension and heart failure

Y Marc, SE Boitard, F Balavoine, M Azizi… - Canadian Journal of …, 2020 - Elsevier
The pathophysiology of heart failure (HF) and hypertension are thought to involve brain
renin-angiotensin system (RAS) hyperactivity. Angiotensin III, a key effector peptide in the …

Targeting the degradation of angiotensin II with recombinant angiotensin-converting enzyme 2: prevention of angiotensin II–dependent hypertension

J Wysocki, M Ye, E Rodriguez… - …, 2010 - Am Heart Assoc
Angiotensin (Ang)-converting enzyme 2 (ACE2) cleaves Ang II to form Ang-(1-7). Here we
examined whether soluble human recombinant ACE2 (rACE2) can efficiently lower Ang II …

Firibastat: A Novel Brain Aminopeptidase Inhibitor–A New Era of Antihypertensive therapy

R Gupta, R Alcantara, T Popli, U Tariq, A Sood… - Current Problems in …, 2022 - Elsevier
Global incidence and prevalence of hypertension continues to increase and remains a
significant challenge. The ever-increasing number of cases are due to comorbid conditions …

Brain-selective overexpression of human angiotensin-converting enzyme type 2 attenuates neurogenic hypertension

Y Feng, H Xia, Y Cai, CM Halabi, LK Becker… - Circulation …, 2010 - Am Heart Assoc
Rationale: Angiotensin converting enzyme type 2 (ACE2) is a new member of the brain renin-
angiotensin system, that might be activated by an overactive renin-angiotensin system …

Aminopeptidase A inhibitors as centrally acting antihypertensive agents

L Bodineau, A Frugière, Y Marc, C Claperon… - Heart failure …, 2008 - Springer
Among the main bioactive peptides of the brain renin–angiotensin system, angiotensin
(Ang) II and AngIII exhibit the same affinity for the type 1 and type 2 Ang receptors. Both …

Brain angiotensin converting enzyme-2 in central cardiovascular regulation

M Mohammed, C Berdasco, E Lazartigues - Clinical Science, 2020 - portlandpress.com
The brain renin–angiotensin system (RAS) plays an important role in the regulation of
autonomic and neuroendocrine functions, and maintains cardiovascular homeostasis. Ang-II …