Title |
Randomised, Double-Blind, Placebo-Controlled, Dose-Escalating Phase I Study of QGC001, a Centrally Acting Aminopeptidase A Inhibitor Prodrug
|
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Published in |
Clinical Pharmacokinetics, December 2013
|
DOI | 10.1007/s40262-013-0125-y |
Pubmed ID | |
Authors |
Fabrice Balavoine, Michel Azizi, Damien Bergerot, Nadia De Mota, Rémi Patouret, Bernard P. Roques, Catherine Llorens-Cortes |
Abstract |
Inhibition of brain aminopeptidase A (APA), which converts angiotensin II into angiotensin III, has emerged as a novel antihypertensive treatment, as demonstrated in several experimental animal models. QGC001 (originally named RB150) is a prodrug of the specific and selective APA inhibitor EC33, and as such it is the prototype of a new class of centrally acting antihypertensive agents. Given by the oral route in hypertensive rats, it enters the brain and generates EC33, which blocks the brain renin-angiotensin system activity and normalises blood pressure. The aim of the present study was to evaluate the safety, pharmacokinetics and pharmacodynamic effects of QGC001 in humans. |
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Demographic breakdown
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