Firibastat (RB150; QGC001) is an orally active, blood-brain barrier-permeant prodrug composed of two molecules of disulfide-linked aminopeptidase A (APA; glutamyl aminopeptidase) active-site inhibitor EC33 (Ki = 300 nM) that are released via the action of brain reductase in the brain. Firibastat exhibits antihypertensive efficacy in vivo (Blood pressure reduction ED50 = 30 mg/kg via p.o. in spontaneously hypertensive rats).
Orally active, brain-permeant precursor of the aminopeptidase A (APA; glutamyl aminopeptidase) active-site inhibitor EC33 with antihypertensive efficacy in vivo.
Aminopeptidase A contributes to biochemical, anatomical and cognitive defects in Alzheimer's disease (AD) mouse model and is increased at early stage in sporadic AD brain
Acta Neuropathologica, 141(6), 823-839 (2021)
Effects of firibastat in combination with enalapril and hydrochlorothiazide on blood pressure and vasopressin release in hypertensive DOCA-salt rats
Biomedicine and Pharmacotherapy, 40, 111682-111682 (2021)
Orally active aminopeptidase A inhibitors reduce blood pressure: a new strategy for treating hypertension
Hypertension, 51(5), 1318-1325 (2008)
Central antihypertensive effects of chronic treatment with RB150: an orally active aminopeptidase A inhibitor in deoxycorticosterone acetate-salt rats
Journal of Hypertension, 36(3), 641-650 (2018)
Brain ACE2 activation following brain aminopeptidase A blockade by firibastat in salt-dependent hypertension
Clinical Science (London, England : 1979), 135(6), 775-791 (2021)
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