Title: Pharmacokinetics, pharmacodynamics, and safety of a prostaglandin D2 receptor antagonist
Authors: Lai, E ×
Wenning, L A
Crumley, T M
De Lepeleire, I
Liu, F
de Hoon, Jan
Van Hecken, Anne
Depré, Marleen
Hilliard, D
Greenberg, H
O'Neill, G
Metters, K
Gottesdiener, K G
Wagner, J A #
Issue Date: Jun-2008
Publisher: Mosby
Series Title: Clinical Pharmacology and Therapeutics vol:83 issue:6 pages:840-847
Abstract: Laropiprant is a selective antagonist of the prostaglandin D(2) (PGD(2)) receptor subtype 1 (DP1). Three double-blind, randomized, placebo-controlled studies evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of laropiprant in healthy male volunteers. Single doses up to 900 mg and multiple doses up to 450 mg were generally well tolerated. Laropiprant exhibited dose-proportional pharmacokinetics. Oral absorption is rapid (T(max)=0.8-2.0 h) and the terminal half-life is approximately 12-18 h. The pharmacokinetics of laropiprant was not affected by food. Single doses of 6 mg and higher were effective in suppressing PGD(2)-induced cyclic AMP accumulation in platelets, demonstrating laropiprant target engagement with DP1. Laropiprant has detectable off-target antagonist effects at the thromboxane A(2) receptor but no clinically significant effect on collagen-induced platelet aggregation or bleeding times with multiple doses up to 200 mg.
ISSN: 0009-9236
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Clinical Pharmacology Centre (-)
× corresponding author
# (joint) last author

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