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

• DOI: 10.1128/aac.48.1.183-191.2004
• Publication Date: 2003-12-24T02:03:22Z
• Authors: Laurene H. Wang; Andrew A. Wiznia; Mobeen H. Rathore; Gregory E. Chittick; Saroj S. Bakshi; Patricia J. Emmanuel; Patricia M. Flynn
• Keywords: Emtricitabine; Regimen

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