Single- and multiple-dose pharmacokinetics and tolerability of telcagepant, an oral calcitonin gene-related peptide receptor antagonist, in adults.
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| Abstract |
Telcagepant is a novel, orally active, and selective calcitonin gene-related peptide receptor antagonist being developed for acute treatment of migraine with and without aura. Three separate clinical studies were conducted to evaluate the pharmacokinetics and tolerability of telcagepant following single oral doses in healthy young and elderly men and women and multiple oral doses in men. Telcagepant was rapidly absorbed with a time to maximum concentration of approximately 1.5 hours. The terminal half-life was approximately 6 hours. A greater than dose-proportional increase was observed in the area under the plasma concentration versus time curve from zero to infinity. Following twice-daily dosing, with each dose separated by 2 hours, steady state was achieved in approximately 3 to 4 days with an accumulation ratio of approximately 2. There were no clinically meaningful pharmacokinetic differences when compared across age and gender. Telcagepant was generally well tolerated up to single doses of 1200 mg and multiple doses of 400 mg twice daily.
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| Authors | Tae H Han, Rebecca L Blanchard, John Palcza, Jacqueline B McCrea, Tine Laethem, Kenneth Willson, Yang Xu, Susan Ermlich, Janet Boyle, Christopher Lines, Maria Gutierrez, Luc Van Bortel, Alan J Xiao, Simon Sinclair, Lisa Hickey, Deborah Panebianco, M Gail Murphy |
| Journal | Journal of clinical pharmacology (J Clin Pharmacol) Vol. 50 Issue 12 Pg. 1367-76 (Dec 2010) ISSN: 1552-4604 [Electronic] England |
| PMID | 20173082 (Publication Type: Clinical Trial, Phase I, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't) |
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