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Sara Abdulrahman Alomar, Sarah Ali Alghabban, HadeelAbdulaziz Alharbi, Mehad Fahad Almoqati, Yazid Alduraibi, Ahmed Abu-Zaid1. Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: a review of clinical trials
Avicenna Journal of Medecine/Volume 11/Issue 1/January 2021
DOI: 10.4103/ajm.ajm_117_20https://doi.org/10.1016/j.bbadis.2020.166037Canadian Journal of Cardiology 36 (2020) 721e731
doi: https://doi.org/10.1016/j.cjca.2020.03.005
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Q. Gao et al. Newt drug targets for hypertension: A literature review. BBA-Molecular Basis of Disease. Volume 1867, Issue 3, 1 March 2021, 166037
https://doi.org/10.1016/j.bbadis.2020.166037Canadian Journal of Cardiology 36 (2020) 721e731
doi: https://doi.org/10.1016/j.cjca.2020.03.005
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Azizi M, Courand PY, Denolle T, Delsart P, Zhygalina V, Amar L, Lantelme P, Mounier-Vehier C, De Mota N, Balavoine F, Llorens-Cortes C. A pilot double-blind randomised placebo-controlled crossover pharmacodynamic study of the centrally active aminopeptidase A inhibitor, firibastat, in hypertension.
J Hypertens. 2019 Aug;37(8):1722-1728.
doi: 10.1097/HJH.0000000000002092.
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Ferdinand KC, Balavoine F, Besse B, Black HR, Desbrandes S, Dittrich HC, Nesbitt SD. Efficacy and Safety of Firibastat, A First-in-Class Brain Aminopeptidase A Inhibitor, in Hypertensive Overweight Patients of Multiple Ethnic Origins.
Circulation. 2019 Jul 9;140(2):138-146. doi: 10.1161/CIRCULATIONAHA.119.040070.
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Keck M, De Almeida H, Compère D, Inguimbert N, Flahault A, Balavoine F, Roques B, Llorens-Cortes C. NI956/QGC006, a Potent Orally Active, Brain-Penetrating Aminopeptidase A Inhibitor for Treating Hypertension.
Hypertension. 2019 Jun;73(6):1300-1307.
doi: 10.1161/HYPERTENSIONAHA.118.12499.
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Keck M, Hmazzou R, Llorens-Cortes C. Orally Active Aminopeptidase A Inhibitor Prodrugs: Current State and Future Directions.
Curr Hypertens Rep. 2019 May 21;21(7):50.
doi: 10.1007/s11906-019-0957-4.
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Boitard SE, Marc Y, Keck M, Mougenot N, Agbulut O, Balavoine F, Llorens-Cortes C. Brain renin-angiotensin system blockade with orally active aminopeptidase A inhibitor prevents cardiac dysfunction after myocardial infarction in mice.
J Mol Cell Cardiol. 2019 Feb;127:215-222.
doi: 10.1016/j.yjmcc.2018.12.008
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Leenen FHH., Ahmad M., Marc Y, Llorens-Cortes C. Specific inhibition of brain angiotensin III formation as a new strategy for prevention of heart failure after myocardial infarction.
J Cardiovasc Pharmacol. 2019 Feb;73(2):82-91.
doi: 10.1097/FJC.0000000000000638
EN SAVOIR PLUSScientific Conferences
European Society of Cardiology 2019
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Boitard-Joanne S, Marc Y, Keck M, Mougenot N, Agbulut O, Balavoine F, LlorensCortes C. Brain reninangiotensin system blockade with firibastat, an orally active, central acting aminopeptidase A inhibitor prodrug prevents cardiac dysfunction after myocardial infarction in mice.
Abstract P4473
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Keck M, De Almeida H, Compere D, Inguimbert N, Flahault A, Balavoine F, Roques BP, Llorens-Cortes C. NI956/QGC006, a potent orally active, brainpenetrating aminopeptidase A inhibitor prodrug for treating hypertension.
Abstract P4481
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Llorens-Cortes C, Marc Y, Hmazzou R, Keck M, Flahault A, Roques BP, Balavoine F, Azizi M. Centralacting aminopeptidase A inhibitors for new treatment of hypertension: from discovery to clinical trial.
Abstract P4554
EN SAVOIR PLUSAmerican Heart Association 2018
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Ferdinand KC, Balavoine F, Besse B, Black HR, Desbrandes S, Dittrich HC, Nesbitt SD. Efficacy and Safety of a Novel Antihypertensive Pharmacotherapy Approach in a High-Risk Diverse Population
Circulation. 2018;138:e766, December 2018
EN SAVOIR PLUSEuropean Society of Hypertension 2017
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Azizi, M.; Courand, P.; Denolle, T.; Zhygalina, V.; Delsart, P.; Amar, L.; Lantelme, P.; Deplanque, D.; Mounier-Vehier, C.; Balavoine, F.; Madonna, O.; Llorens-Cortes, C. A randomized double-blind placebo controlled crossover study to compare QGC001, a brain aminopeptidase A inhibitor, with placebo in patients with grade I/II essential hypertension.
J Hypertens. 35:e36, September 2017.
EN SAVOIR PLUSEuropean Society of Hypertension 2016
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Hmazzou, R.; Flahault, A.; Marc, Y.; Llorens-Cortes, C. Mode of action of RB150, an aminopeptidase A inhibitor prodrug as a centrally-acting antihypertensive agent in DOCA-salt hypertensive rats.
J Hypertens. 34:e75, September 2016.
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Marc, Y.; Hmazzou, R.; Flahault, A.; Llorens-Cortes, C. Central antihypertensive effects of chronic treatment with RB150/QGC001, an orally active aminopeptidase A inhibitor prodrug in DOCA-salt hypertensive rats.
J Hypertens. 34:e103, September 2016.
EN SAVOIR PLUSEuropean Society of Hypertension 2014
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Balavoine, F., Azizi, M., Bergerot, D., De Mota, N., Patouret, R., Roques, B.P., Llorens-Cortes, C. Safety, tolerability, pharmacokinetics and pharmacodynamics of multiple ascending doses of QGC001, a centrally-acting aminopeptidase A inhibitor, in healthy volunteers.
J Hypertens. 32:e82, September 2014.
EN SAVOIR PLUSEuropean Society of Hypertension 2013
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Balavoine, F., Kousignian, Bergerot, D., De Mota, N., Chassard, D., Segard, L., Roques, B.P., Llorens-Cortes, C., Azizi, M. Safety, tolerability, pharmacokinetics and pharmacodynamics of QGC001, a centrally-acting aminopeptidase A inhibitor, in healthy volunteers.
J Hypertens. 31:e114, September 2013.
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