Etamicastat is a reversible dopamine-β-hydroxylase inhibitor that decreases noradrenaline levels in sympathetically innervated tissues and slows down sympathetic nervous system drive. It has been administered orally at doses up to 600 mg once daily for 10 days to male healthy volunteers.
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| "Etamicastat is a reversible dopamine-β-hydroxylase inhibitor that decreases noradrenaline levels in sympathetically innervated tissues and slows down sympathetic nervous system drive. " | ( Human disposition, metabolism and excretion of etamicastat, a reversible, peripherally selective dopamine β-hydroxylase inhibitor.
Almeida, L; Fernandes-Lopes, C; Loureiro, AI; Nunes, T; Rocha, JF; Soares-da-Silva, P; Wright, LC, 2014) | 2.1 |
| "Etamicastat is a dopamine β-hydroxylase (DβH) inhibitor currently in clinical development for the treatment of hypertension and heart failure." | ( Etamicastat, a novel dopamine β-hydroxylase inhibitor: tolerability, pharmacokinetics, and pharmacodynamics in patients with hypertension.
Almeida, L; Costa, R; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M, 2013) | 3.28 |
| "Etamicastat is a novel dopamine-ß-hydroxylase (DBH) inhibitor that is oxidized into BIA 5-965 and deaminated followed by oxidation to BIA 5-998, which represents 13% of total etamicastat and quantified metabolites." | ( Etamicastat, a new dopamine-ß-hydroxylase inhibitor, pharmacodynamics and metabolism in rat.
Bonifácio, MJ; Fernandes-Lopes, C; Igreja, B; Loureiro, AI; Soares-da-Silva, P; Wright, LC, 2014) | 2.57 |
| "Etamicastat is a novel, potent, and reversible peripheral dopamine-β-hydroxylase inhibitor that has been administered orally at doses up to 600 mg once daily for 10 days to male healthy volunteers and appears to be well tolerated." | ( Effect of food on the pharmacokinetic profile of etamicastat (BIA 5-453).
Almeida, L; Falcão, A; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M, 2011) | 2.07 |
| "Etamicastat is a new dopamine-β-hydroxylase (DβH) inhibitor currently in clinical development for the treatment of hypertension and heart failure." | ( Pharmacokinetics and tolerability of etamicastat following single and repeated administration in elderly versus young healthy male subjects: an open-label, single-center, parallel-group study.
Almeida, L; Falcão, A; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M, 2011) | 2.08 |
Etamicastat Tmax was 1 hour postdose, and mean t½ was 19 to 28 hours following repeated administration. Large interindividual variability dependent on the NAT2 acetylator status was found in the pharmacokinetic parameters of etamicast at and BIA 5-961.
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| " There was a high variability in pharmacokinetic parameters, attributable to different N-acetyltransferase-2 (NAT2) phenotype." | ( Safety, tolerability, and pharmacokinetics of etamicastat, a novel dopamine-β-hydroxylase inhibitor, in a rising multiple-dose study in young healthy subjects.
Almeida, L; Falcão, A; Igreja, B; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M; Wright, LC, 2010) | 0.62 |
| " Elimination was biphasic, characterized by a first short early elimination half-life followed by a longer elimination phase of 16 to 20 hours for etamicastat doses of 100 mg and above." | ( Single-dose tolerability, pharmacokinetics, and pharmacodynamics of etamicastat (BIA 5-453), a new dopamine β-hydroxylase inhibitor, in healthy subjects.
Almeida, L; Bonifácio, MJ; Falcão, A; Igreja, B; Loureiro, AI; Nunes, T; Rocha, JF; Soares-Da-Silva, P; Vaz-Da-Silva, M; Wright, LC, 2012) | 0.81 |
| " The statistical method for testing the effect of food on the pharmacokinetic parameters of interest was based upon the 90% confidence interval (CI) for the test/reference geometric mean ratio (GMR)." | ( Effect of food on the pharmacokinetic profile of etamicastat (BIA 5-453).
Almeida, L; Falcão, A; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M, 2011) | 0.62 |
| " Large interindividual variability dependent on the NAT2 acetylator status was found in the pharmacokinetic parameters of etamicastat and BIA 5-961." | ( Pharmacokinetics and tolerability of etamicastat following single and repeated administration in elderly versus young healthy male subjects: an open-label, single-center, parallel-group study.
Almeida, L; Falcão, A; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M, 2011) | 0.85 |
| "The pharmacokinetic profile of etamicastat was not significantly different in these small groups of healthy young versus elderly adult male volunteers." | ( Pharmacokinetics and tolerability of etamicastat following single and repeated administration in elderly versus young healthy male subjects: an open-label, single-center, parallel-group study.
Almeida, L; Falcão, A; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M, 2011) | 0.93 |
| " Etamicastat Tmax was 1 hour postdose, and mean t½ was 19 to 28 hours following repeated administration." | ( Etamicastat, a novel dopamine β-hydroxylase inhibitor: tolerability, pharmacokinetics, and pharmacodynamics in patients with hypertension.
Almeida, L; Costa, R; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M, 2013) | 2.74 |
| "Etamicastat was well tolerated and showed a pharmacokinetic profile consistent with a once-daily regimen." | ( Etamicastat, a novel dopamine β-hydroxylase inhibitor: tolerability, pharmacokinetics, and pharmacodynamics in patients with hypertension.
Almeida, L; Costa, R; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M, 2013) | 3.28 |
| " Though P-gp-mediated efflux may contribute to the limited brain penetration of etamicastat, the low permeability along with the pharmacokinetic properties of etamicastat may be perceived as the main contributors for its peripheral selectivity, which is advantageous for a cardiovascular drug candidate." | ( Role of P-glycoprotein and permeability upon the brain distribution and pharmacodynamics of etamicastat: a comparison with nepicastat.
Bonifácio, MJ; Fernandes-Lopes, C; Igreja, B; Loureiro, AI; Pires, N; Soares-da-Silva, P; Wright, LC, 2015) | 0.86 |
The absolute oral bioavailability of etamicastat was 64% of the administered dose. Despite its lower bioavailability and higher clearance, as compared to nepicastat, etamicstat showed preferential distribution to peripheral tissues and high plasma free fraction (15%)
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| " Furthermore, the high interspecies and intraspecies differences in N-acetylation should be taken into consideration when evaluating the in vivo bioavailability of etamicastat." | ( N-acetylation of etamicastat, a reversible dopamine-β-hydroxylase inhibitor.
Bonifácio, MJ; Fernandes-Lopes, C; Loureiro, AI; Soares-da-Silva, P; Wright, LC, 2013) | 0.93 |
| " The absolute oral bioavailability of etamicastat was 64% of the administered dose." | ( Etamicastat, a new dopamine-ß-hydroxylase inhibitor, pharmacodynamics and metabolism in rat.
Bonifácio, MJ; Fernandes-Lopes, C; Igreja, B; Loureiro, AI; Soares-da-Silva, P; Wright, LC, 2014) | 2.12 |
| " The calculated oral bioavailability for etamicastat was 46." | ( Distribution and pharmacokinetics of etamicastat and its N-acetylated metabolite (BIA 5-961) in dog and monkey.
Loureiro, AI; Soares-da-Silva, P, 2015) | 0.96 |
| " Despite its lower bioavailability and higher clearance, as compared to nepicastat, etamicastat showed preferential distribution to peripheral tissues and high plasma free fraction (15." | ( Role of P-glycoprotein and permeability upon the brain distribution and pharmacodynamics of etamicastat: a comparison with nepicastat.
Bonifácio, MJ; Fernandes-Lopes, C; Igreja, B; Loureiro, AI; Pires, N; Soares-da-Silva, P; Wright, LC, 2015) | 0.86 |