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Entecavir Pharmacokinetics, Safety, and Tolerability After Multiple Ascending Doses in Healthy Subjects

From Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey (Mr Bifano, Mr Olsen, Dr Smith, Dr Zhang, Dr Grasela, Dr LaCreta) and Novartis Pharmaceuticals Corporation, East Hanover, New Jersey (Dr Yan).

A double-blind, placebo-controlled, multiple oral dose escalation study was conducted to investigate the pharmacokinetics, safety, and tolerability of entecavir in healthy subjects. Eight subjects were assigned to each of the 3 dose panels (0.1 mg, 0.5 mg, and 1 mg or matched placebo once daily for 14 days). Blood and urine samples were collected for pharmacokinetic analyses. Entecavir was rapidly absorbed, with peak plasma concentration occurring within 1 hour of dosing. Steady-state plasma concentrations of entecavir were achieved by 10 days following the initial dose. At steady state, the mean area under the plasma concentration-time curve over 1 dosing interval, increased approximately proportional to dose. Entecavir had a mean terminal half-life ranging from 128 to 149 hours and an effective half-life of approximately 24 hours. Elimination was predominantly through renal excretion, with mean urinary recovery ranging from 62% to 73%. Entecavir was safe and well tolerated when administered at doses ranging from 0.1 mg to 1 mg/d for 14 days.

Key Words: Entecavir • pharmacokinetics • healthy subject

Address for reprints: Marc Bifano, MS, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000; e-mail: marc.bifano{at}bms.com.

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