Pharmacokinetics of single- and multiple-dose emtricitabine in healthy male Chinese volunteers.

Abstract

Emtricitabine (FTC) is used for the treatment of HIV infection and pre-exposure chemoprophylaxis. It is often used in combination with tenofovir disoproxil fumarate (TDF). This study was designed to evaluate FTC pharmacokinetics in healthy male Chinese volunteers. Sixty subjects were recruited into this single-centre, randomised, open-label study and randomly received single (groups A, B and C) or multiple oral doses (once daily for 6 days; groups D, E and F) of 200-mg FTC capsules alone (A and D), or combined with 300-mg TDF tablets (B and E), or 200 mg of FTC plus 300 mg of TDF with a high-fat diet (C and F), respectively. FTC was well-tolerated in all groups. After a single dose, there were no differences in the mean AUC0-∞ values; however, there were significant differences in the mean Tmax values (1.05, 1.40 and 2.10 h for groups A, B and C, respectively; p < 0.05). In the multiple-dose study, our results were significantly different from published t1/2 values following single-dose FTC.

• Authors: Wen-Li Han, Jing-Chuan Shang, Bo Yan, Rui Tan, Wen-Xiang Huang, Xiao-Ni Zhong, Jun-Qing Yang, Ai-Long Huang
• Journal: Pharmacology (Pharmacology) Vol. 93 Issue 3-4 Pg. 166-71 ( 2014) ISSN: 1423-0313 [Electronic] Switzerland
• PMID: 24802019 (Publication Type: Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
• Copyright: © 2014 S. Karger AG, Basel.

Chemical References

• 9-(2-((bis(pivaloyloxymethoxy)phosphinoyl)methoxy)propyl)adenine
• Anti-HIV Agents
• Phosphorous Acids
• Deoxycytidine
• Emtricitabine
• Adenine

Topics

• Adenine (administration & dosage, analogs & derivatives, pharmacology)
• Adult
• Anti-HIV Agents (administration & dosage, adverse effects, pharmacokinetics)
• Area Under Curve
• Deoxycytidine (administration & dosage, adverse effects, analogs & derivatives, pharmacokinetics)
• Diet, High-Fat
• Drug Administration Schedule
• Emtricitabine
• Food-Drug Interactions
• Half-Life
• Humans
• Male
• Phosphorous Acids (administration & dosage, pharmacology)
• Young Adult