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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

R. G. Gish,1 N. W. Y. Leung,2 T. L. Wright,3 Huy Trinh,4 W. Lang,5 H. A. Kessler,6 L. Fang,7 L. H. Wang,7 J. Delehanty,7 A. Rigney,7 E. Mondou,7* A. Snow,7 and F. Rousseau7

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.


* Corresponding author. Mailing address: Triangle Pharmaceuticals, Inc., 4 University Place, 4611 University Dr., Durham, NC 27707. Phone: (919) 402-2221. Fax: (919) 493-5925. E-mail: Mondouen@tripharm.com.


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.




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Copyright © 2002 by the American Society for Microbiology. All rights reserved.