Pharmacokinetics, pharmacodynamics, safety, and tolerability of pradigastat, a novel diacylglycerol acyltransferase 1 inhibitor in overweight or obese, but otherwise healthy human subjects

• Published in: Journal of clinical pharmacology Vol. 55; no. 9; p. 1031
• Main Authors: Meyers, Charles D, Amer, Ahmed, Majumdar, Tapan, Chen, Jin
• Format: Journal Article
• Language: English
• Published: England 01.09.2015
• Subjects: Acetates - administration & dosage; Acetates - adverse effects; Acetates - pharmacokinetics; Adolescent; Adult; Aminopyridines - administration & dosage; Aminopyridines - adverse effects; Aminopyridines - pharmacokinetics; Area Under Curve; Diacylglycerol O-Acyltransferase - antagonists & inhibitors; Dose-Response Relationship, Drug; Double-Blind Method; Female; Half-Life; Humans; Male; Middle Aged; Overweight; Young Adult; triglyceride; pharmacokinetics; DGAT1 inhibitor; pharmacodynamics; pradigastat

Pradigastat is a potent and selective inhibitor of diacylglycerol acyltransferase 1, an enzyme highly expressed in the small intestine that plays a key role in postprandial triglyceride synthesis. This first-in-human study evaluated the pharmacokinetics, pharmacodynamics, safety, and tolerability of...