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

• Published in: Clinical therapeutics Vol. 33; no. 6; pp. 776 - 791
• Main Authors: Nunes, Teresa, Rocha, José Francisco, Vaz-da-Silva, Manuel, Falcão, Amilcar, Almeida, Luis, Soares-da-Silva, Patricio
• Format: Journal Article
• Language: English
• Published: Bridgewater, NJ EM Inc USA 01.06.2011; Elsevier; Elsevier Limited
• Subjects: Adolescent; Adult; age effect; Age Factors; Aged; Area Under Curve; Arterial hypertension. Arterial hypotension; Arylamine N-Acetyltransferase - genetics; Benzopyrans - administration & dosage; Benzopyrans - adverse effects; Benzopyrans - pharmacokinetics; Biological and medical sciences; Blood and lymphatic vessels; Cardiology. Vascular system; Clinical trials; Dopamine; Dopamine beta-Hydroxylase - antagonists & inhibitors; dopamine-β-hydroxylase; dopamine-β-hydroxylase inhibition; Drug Administration Schedule; Drug dosages; Drug therapy; Enzyme Inhibitors - administration & dosage; Enzyme Inhibitors - adverse effects; Enzyme Inhibitors - pharmacokinetics; etamicastat; Genotype; Heart; heart failure; Heart failure, cardiogenic pulmonary edema, cardiac enlargement; Humans; Hypertension; Imidazoles - administration & dosage; Imidazoles - adverse effects; Imidazoles - pharmacokinetics; Infections; Internal Medicine; Isoenzymes - genetics; Male; Medical Education; Medical sciences; Metabolites; Older people; pharmacokinetics; Pharmacology. Drug treatments; Rodents; Time Factors; Young Adult; heart failure; dopamine-β-hydroxylase; age effect; dopamine-β-hydroxylase inhibition; pharmacokinetics; etamicastat; hypertension; Human; Hypertension; Heart failure; Imidazole derivatives; Dopamine β-monooxygenase; Healthy subject; Etamicastat; Enzyme; Toxicity; Single dose; Cardiovascular disease; Multiple dose; Heart disease; Oxidoreductases; Pharmacokinetics; Elderly; Age; Comparative study

Etamicastat is a new dopamine-β-hydroxylase (DβH) inhibitor currently in clinical development for the treatment of hypertension and heart failure. To evaluate the pharmacokinetics and tolerability of etamicastat after single and repeated administration in elderly subjects (aged ≥65 years) relative t...