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Single‐ and Multiple‐Dose Pharmacokinetics and Tolerability of Telcagepant, an Oral Calcitonin Gene‐Related Peptide Receptor Antagonist, in Adults
Author(s) -
Han Tae H.,
Blanchard Rebecca L.,
Palcza John,
McCrea Jacqueline B.,
Laethem Tine,
Willson Kenneth,
Xu Yang,
Ermlich Susan,
Boyle Janet,
Lines Christopher,
Gutierrez Maria,
Bortel Luc,
Xiao Alan J.,
Sinclair Simon,
Hickey Lisa,
Panebianco Deborah,
Murphy M. Gail
Publication year - 2010
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270010361741
Subject(s) - pharmacokinetics , tolerability , medicine , dosing , oral administration , calcitonin gene related peptide , endocrinology , gastrin releasing peptide , antagonist , pharmacology , receptor , adverse effect , neuropeptide , bombesin
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.