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

Meyers, Charles D. ; Amer, Ahmed ; Majumdar, Tapan ; Chen, Jin

Journal of Clinical Pharmacology, September 2015, Vol.55(9), pp.1031-1041 [Peer Reviewed Journal]

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  • Title:
    Pharmacokinetics, pharmacodynamics, safety, and tolerability of pradigastat, a novel diacylglycerol acyltransferase 1 inhibitor in overweight or obese, but otherwise healthy human subjects
  • Author: Meyers, Charles D. ; Amer, Ahmed ; Majumdar, Tapan ; Chen, Jin
  • Description: 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 pradigastat administered at single and multiple doses in overweight or obese healthy subjects. In single-dose cohorts (n=72), subjects were randomized sequentially to receive single doses of pradigastat (1, 3, 10, 30, 100, or 300mg) or placebo under fasted condition and prior to breakfast. In multiple-dose cohorts (n=106), subjects were randomized to receive pradigastat (1, 5, 10, or 25mg) or placebo prior to breakfast for 14 days. Following a single oral dosing, pradigastat was absorbed slowly, with a median tmax of 10 hours and eliminated slowly with a long half-life. With multiple oral doses, a 10- to17-fold higher systemic exposure was observed. Pradigastat treatment (single and multiple...
  • Is Part Of: Journal of Clinical Pharmacology, September 2015, Vol.55(9), pp.1031-1041
  • Identifier: ISSN: 0091-2700 ; E-ISSN: 1552-4604 ; DOI: 10.1002/jcph.509
  • Subjects: Dgat1 Inhibitor ; Pradigastat ; Pharmacokinetics ; Pharmacodynamics ; Triglyceride

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