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Antimicrobial Agents and Chemotherapy, January 2004, p. 183-191, Vol. 48, No. 1
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.1.183-191.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

Pharmacokinetics and Safety of Single Oral Doses of Emtricitabine in Human Immunodeficiency Virus-Infected Children

Laurene H. Wang,1 Andrew A. Wiznia,2 Mobeen H. Rathore,3 Gregory E. Chittick,1 Saroj S. Bakshi,4 Patricia J. Emmanuel,5 and Patricia M. Flynn6

Triangle Pharmaceuticals, Inc., Gilead Sciences, Inc., Durham, North Carolina,1 Jacobi Medical Center, Bronx Municipal Hospital Center, Bronx, New York,2 University of Florida Health Science Center, Jacksonville, Florida,3 North Shore University Hospital, Manhasset, New York,4 University of South Florida, Tampa, Florida,5 St. Jude Children's Research Hospital, Memphis, Tennessee6

Received 19 February 2003/ Returned for modification 24 April 2003/ Accepted 11 September 2003

Emtricitabine (FTC; Emtriva), a potent deoxycytidine nucleoside reverse transcriptase inhibitor, has recently been approved by the U.S. Food and Drug Administration for the treatment of human immunodeficiency virus (HIV) infection. In adults, FTC has demonstrated linear kinetics over a wide dose range, and FTC 200 mg once a day (QD) is the recommended therapeutic dose. A phase I open-label trial was conducted in children to identify an FTC dosing regimen that would provide comparable plasma exposure to that observed in adults at 200 mg QD. Two single oral doses of FTC (60 and 120 mg/m2, up to a maximum of 200 mg, in solutions) were evaluated in HIV-infected children aged <18 years old. Children >=6 years old also received a third dose of ~120 mg/m2 in capsules. A total of 25 children (two <2 years old, eight 2 to 5 years old, eight 6 to 12 years old, and seven 13 to 17 years old) received at least two doses of FTC. Single escalating oral doses of FTC were well tolerated and produced dose-proportional plasma drug concentrations in children. The FTC pharmacokinetics was comparable between adults and children 22 months to 17 years of age. The capsule formulation provided ~20% higher plasma FTC exposure than the solution formulation. Using plasma area under the concentration-time curve (AUC) data at the 120-mg/m2 dose, it is projected (based on dose proportionality) that a 6-mg/kg dose (up to a maximum of 200 mg) of FTC would produce plasma AUCs in children comparable to those in adults given a 200-mg dose (i.e., median of ~10 h·µg/ml). This pediatric FTC dose is being evaluated in long-term phase II therapeutic trials in HIV-infected children.

* Corresponding author. Mailing address: Gilead Sciences, Inc., 4 University Place, 4611 University Dr., Durham, NC 27707. Phone: (919) 294-7155. Fax: (919) 493-5790. E-mail: greg.chittick{at}Gilead.com.

Antimicrobial Agents and Chemotherapy, January 2004, p. 183-191, Vol. 48, No. 1
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.1.183-191.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.



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