| Content Provider |
World Health Organization (WHO)-Global Index Medicus |
| Author |
Hu, Chao-Ying Liu, Yan-Mei Liu, Yun Chen, Qian Wang, Wei Wu, Kai Dong, Jie Li, Jie Jia, Jing-Ying Lu, Chuan Sun, Shi-Xuan Yu, Chen Li, Xuening |
| Description |
Country affiliation: China Author Affiliation: Hu CY ( Department of Clinical Pharmacology, Zhong Shan Hospital, Fudan University, Shanghai, China); Liu YM ( Phase I Clinical Research Unit, Shanghai Xuhui Central Hospital, Shanghai, China.); Liu Y ( Phase I Clinical Research Unit, Shanghai Xuhui Central Hospital, Shanghai, China.); Chen Q ( Phase I Clinical Research Unit, Shanghai Xuhui Central Hospital, Shanghai, China.); Wang W ( Phase I Clinical Research Unit, Shanghai Xuhui Central Hospital, Shanghai, China.); Wu K ( Clinical Development, GlaxoSmithKline R&D China, Shanghai, China.); Dong J ( Clinical Development, GlaxoSmithKline R&D China, Shanghai, China.); Li J ( Clinical Development, GlaxoSmithKline R&D China, Shanghai, China.); Jia JY ( Phase I Clinical Research Unit, Shanghai Xuhui Central Hospital, Shanghai, China.); Lu C ( Phase I Clinical Research Unit, Shanghai Xuhui Central Hospital, Shanghai, China.); Sun SX ( Phase I Clinical Research Unit, Shanghai Xuhui Central Hospital, Shanghai, China.); Yu C ( Phase I Clinical Research Unit, Shanghai Xuhui Central Hospital, Shanghai, China.); Li X ( Department of Clinical Pharmacology, Zhong Shan Hospital, Fudan University, Shanghai, China. Electronic address: clab001@126.com.) |
| Abstract |
BACKGROUND: Tenofovir disoproxil fumarate (TDF) has been approved worldwide for the treatment of adults with chronic hepatitis B and, in combination with other antiretroviral agents, HIV-1 infection. Although its use for the treatment of HIV has been approved by the Chinese State Food and Drug Administration, there are no data on the pharmacokinetic profile of TDF in Chinese individuals. OBJECTIVES: This study aimed to investigate the pharmacokinetic properties and tolerability of TDF in healthy Chinese subjects. METHODS: This open-label, single- and multiple-dose study was conducted in healthy Chinese volunteers. Subjects received TDF 300 mg once daily, administered as a single dose (day 1) and multiple doses (days 4-10). Multiple plasma samples were collected over time, and the concentrations of TDF were determined using LC-MS/MS. Pharmacokinetic parameters were estimated using a noncompartmental model. Tolerability was determined using clinical evaluation and monitoring of adverse events (AEs). RESULTS: Fourteen volunteers were enrolled (7 men, 7 women; mean age, 24.6 years). TDF was rapidly absorbed; median Tmax was 0.75 hour, and t½ was ~21 hours with single dosing. The mean ratio of AUC0-τ steady state/AUC0-24 single dose was 1.55. The pharmacokinetic properties of TDF were consistent between the single dose and multiple doses, and between men and women. No serious AEs were reported, and there were no discontinuations due to AEs. CONCLUSIONS: There was an accumulation of approximately 55% in tenofovir exposure in healthy Chinese between multiple dose and single dose. TDF exhibited a pharmacokinetic profile similar to that of healthy Western subjects in a historical comparison. TDF was generally well tolerated in these healthy Chinese subjects. ClinicalTrials.gov identifier: NCT01480622. |
| File Format |
HTM / HTML |
| ISSN |
01492918 |
| Issue Number |
12 |
| Volume Number |
35 |
| e-ISSN |
1879114X |
| Journal |
Clinical Therapeutics |
| Language |
English |
| Publisher |
Elsevier |
| Publisher Date |
2013-12-01 |
| Publisher Place |
United States |
| Access Restriction |
One Nation One Subscription (ONOS) |
| Subject Keyword |
Discipline Pharmacology Adenine Analogs & Derivatives Anti-retroviral Agents Pharmacokinetics Therapeutic Use Organophosphonates Administration & Dosage Adverse Effects Administration, Oral Adult Asian Continental Ancestry Group Dose-response Relationship, Drug Drug Administration Schedule Female Humans Male Middle Aged Tenofovir Young Adult Clinical Trial Journal Article Research Support, Non-u.s. Gov't |
| Content Type |
Text |
| Resource Type |
Article |
| Subject |
Pharmacology Pharmacology (medical) |
