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Antimicrobial Agents and Chemotherapy, June 2002, p. 1734-1740, Vol. 46, No. 6
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.6.1734-1740.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Dose Range Study of Pharmacokinetics, Safety, and Preliminary Antiviral Activity of Emtricitabine in Adults with Hepatitis B Virus Infection

Departments of Medicine and Transplantation, California Pacific Medical Center,¹ Prince of Wales Hospital and the Chinese University of Hong Kong, Hong Kong, People's Republic of China,² Veterans Hospital,³ California Pacific Medical Center Research Institute,⁴ ViRx Inc., San Francisco, California,⁵ Rush-Presbyterian-St. Lukes Medical Center, Chicago, Illinois,⁶ Triangle Pharmaceuticals, Inc., Durham, North Carolina⁷

Received 11 October 2001/ Returned for modification 7 January 2002/ Accepted 11 March 2002

A multicenter, open-label study was performed to evaluate the safety, anti-hepatitis B virus (anti-HBV) activity, and pharmacokinetics of emtricitabine therapy administered once daily for 8 weeks to patients infected with HBV. Clinical and virologic evaluations were completed at the baseline; at 7, 14, 28, 42, and 56 days during treatment; and at 24, 48, and 28 days posttreatment. Forty-nine patients were enrolled in five dose cohorts (doses of 25, 50, 100, 200, and 300 mg, all of which were administered once daily [q.d.]). Peak plasma emtricitabine concentrations occurred within 1.5 h following dosing. Plasma emtricitabine concentrations (maximum concentrations of drug in plasma and areas under the concentration-time curves) increased nearly dose proportionally over the 25- to 300-mg dose range, with relatively small intersubject variabilities. The plasma half-life of emtricitabine ranged from 6 to 9 h. HBV DNA levels were measured by the Digene HBV Hybrid Capture II assay. Viral suppression (reduction in log₁₀ serum HBV DNA levels) occurred in all dose cohorts. All doses demonstrated potent and rapid antiviral activities, with a trend toward a greater suppression with daily doses of 100 mg or greater. At 2 months, the median change in the serum HBV DNA level from the baseline level ranged from -1.7 log₁₀ for the 25-mg dose administered q.d. to -3.3 log₁₀ for the 300 mg dose administered q.d. Emtricitabine was well tolerated over the 2-month dosing period. These results support further clinical development of emtricitabine for the treatment of chronic hepatitis B infection.

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