Etamicastat (BIA 5-453) is a potent and reversible peripheral dopamine-β-hydroxylase (DβH) inhibitor[1].
Upon intraperitoneal administration to NMRi mice, Etamicastat (100 mg/ kg) leads to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control)[2].Etamicastat (50 mg/kg) is rapidly absorbed into the systemic circulation reaching a maximum concentration at 4 h post-administration, representing 29% of total Etamicastat and quantified metabolites, using AUC0-t as a measure of systemic exposure[2].
[1]. Vaz-da-Silva M, et al. Effect of food on the pharmacokinetic profile of Etamicastat (BIA 5-453). Drugs R D. 2011;11(2):127-36. [2]. Loureiro AI, et al. Etamicastat, a new dopamine-?-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94.