Pharmacokinetics and pharmacodynamics of the vasopeptidase inhibitor, omapatrilat in healthy subjects

• Published in: British journal of clinical pharmacology Vol. 56; no. 4; pp. 395 - 406
• Main Authors: Liao, Wei‐chi, Vesterqvist, Ole, Delaney, Carol, Jemal, Mohammed, Ferreira, Irene, Ford, Neville, Swanson, Brian, Uderman, Howard
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Science Ltd 01.10.2003; Blackwell Science; Blackwell Science Inc
• Subjects: Administration, Oral; Adult; angiotensin converting enzyme; Angiotensin-Converting Enzyme Inhibitors - blood; Angiotensin-Converting Enzyme Inhibitors - pharmacokinetics; Angiotensin-Converting Enzyme Inhibitors - pharmacology; Antihypertensive agents; Atrial Natriuretic Factor - blood; Atrial Natriuretic Factor - urine; Biological and medical sciences; blood pressure; Blood Pressure - drug effects; Cardiovascular system; Cyclic GMP - blood; Cyclic GMP - urine; Dose-Response Relationship, Drug; Double-Blind Method; Half-Life; Humans; Male; Medical sciences; Middle Aged; Neprilysin - antagonists & inhibitors; neutral endopeptidase; omapatrilat; pharmacodynamics; pharmacokinetics; Pharmacokinetics and Pharmacodynamics; Pharmacology. Drug treatments; Pyridines - blood; Pyridines - pharmacokinetics; Pyridines - pharmacology; Renin - blood; Thiazepines - blood; Thiazepines - pharmacokinetics; Thiazepines - pharmacology; vasopeptidase inhibitor; Human; blood pressure; Healthy subject; Enzyme; Toxicity; pharmacodynamics; Single dose; Oral administration; Enzyme inhibitor; vasopeptidase inhibitor; neutral endopeptidase; Dose activity relation; Multiple dose; Peptidases; angiotensin converting enzyme; Peptidyl-dipeptidase A; Endopeptidase; Phase I trial; Omapatrilat; Hydrolases; Peptidyl-dipeptidases; Antihypertensive agent; Pharmacokinetics; ACE inhibitor

Aims  To determine the pharmacokinetics, pharmacodynamics and tolerability of omapatrilat, a vasopeptidase inhibitor, in healthy subjects. Methods  The effects of oral omapatrilat were evaluated in healthy men in two double‐blind, placebo‐controlled, dose‐escalation trials. In a single‐dose study, s...