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Multiple-Dose Pharmacokinetics of the Selective Nicotinic Receptor Partial Agonist, Varenicline, in Healthy Smokers

From the Departments of Clinical Pharmacokinetics and Pharmacodynamics (Dr Faessel, Dr Gibbs, Mr Rohrbacher), Medical and Developmental Sciences (Dr Faessel, Dr Gibbs, Dr Clark, Mr Rohrbacher, Dr Burstein), and Statistics (Dr Stolar), Pfizer Global Research and Development, Groton, Connecticut.

Varenicline is a novel and selective 4ß2 nicotinic acetylcholine receptor partial agonist developed for smoking cessation. The primary objectives of this double-blind, placebo-controlled, dose-escalation study were to determine the pharmacokinetics, safety, and tolerability of multiple oral doses of varenicline given as tablets once (1 mg, 2 mg, and 3 mg) or twice (1 mg) daily to healthy adult smokers. Within each dose level, 8 subjects were randomized to varenicline and 4 subjects to placebo. Varenicline was well tolerated at doses up to and including 2 mg daily. Dose-proportional increases in maximum observed plasma concentrations and area under the plasma concentration-time curve from time zero to the end of the dosing interval values were observed between the 1-mg and 2-mg daily doses of varenicline. Once- and twice-daily dosing resulted, on average, in an approximate 2- and 3-fold increase in varenicline systemic exposure, respectively, compared with single dose. There was no evidence of concentration- or time-dependent changes in the pharmacokinetics of varenicline upon repeat dosing.

Key Words: Varenicline • multiple dosing • pharmacokinetics

Address for reprints: Hélène M. Faessel, PharmD, PhD, Pfizer Global Research and Development, Eastern Point Road/MS 8260-2309, Groton, CT 06340; e-mail: Helene.M.Faessel{at}pfizer.com.

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