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学科主题: 临床医学
题名:
Pharmacokinetic Study of Saxagliptin in Healthy Chinese Subjects
作者: Li, Haiyan2,3; Yang, Li4; Tou, Conrad K. P.5; Patel, Chirag G.6; Zhao, June1
刊名: CLINICAL DRUG INVESTIGATION
发表日期: 2012
卷: 32, 期:7, 页:465-473
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: RANDOMIZED CONTROLLED-TRIAL ; TYPE-2 DIABETES-MELLITUS ; IMPROVES GLYCEMIC CONTROL ; DIPEPTIDYL PEPTIDASE-4 INHIBITOR ; COMBINATION THERAPY ; METFORMIN ; EFFICACY ; SAFETY ; SULFONYLUREA ; MANAGEMENT
英文摘要:

Background and Objectives: The pharmacokinetics of some medications may be affected by differences in race and ethnicity, which can lead to suboptimal outcomes. The present study was conducted to assess the single- and multiple-dose pharmacokinetics of saxagliptin in healthy Chinese subjects living in China.

Methods: This was an open-label, 9-day study conducted at the Drug Clinical Trial Center, Peking University Third Hospital, Beijing, China. Sixteen healthy Chinese subjects of both sexes between 21 and 33 years of age were administered saxagliptin 5 mg orally on day 1, then once daily on days 3-7. Pharmacokinetic variables for saxagliptin (primary outcome) and its active metabolite, 5-hydroxy saxagliptin (secondary outcome), after single and multiple oral doses of saxagliptin were assessed. Safety was also assessed.

Results: Saxagliptin was absorbed rapidly (median time to reach maximum concentration [t(max)]: 0.5 and 1 hour on days 1 and 7, respectively), and its pharmacologically active metabolite, 5-hydroxy saxagliptin, appeared in plasma (median t(max): 1.0 and 1.5 hours, respectively). Plasma exposure to 5-hydroxy saxagliptin was approximately 2- to 3-fold higher than exposure to saxagliptin. Plasma concentration-time profiles for saxagliptin and 5-hydroxy saxagliptin were similar on days 1 and 7, with no evidence of drug accumulation on repeated dosing. The elimination half-lives (t(1/2)) for saxagliptin and 5-hydroxy saxagliptin were approximately 3 and 4 hours, respectively, with renal excretion as the primary route of elimination. After single and multiple dosing, 54.48% and 52.60%, respectively, of the administered saxagliptin dose was recovered in urine as unchanged drug or 5-hydroxy saxagliptin. Saxagliptin was generally well tolerated. Six (37.5%) subjects experienced an adverse event (AE). All AEs were mild in intensity and judged by the investigator as not related to the study medication. There were no deaths, serious AEs, discontinuations due to AEs, or other clinically significant AEs during this study.

Conclusion: Saxagliptin 5 mg (single dose and once-daily doses for 5 days) was generally well tolerated; the pharmacokinetics of saxagliptin and 5-hydroxy saxagliptin in healthy Chinese subjects were consistent with previous assessments in the saxagliptin clinical development program.

Trial Registration: ClinicalTrials.gov identifier: NCT00770302.

语种: 英语
项目资助者: AstraZeneca ; Bristol-Myers Squibb
WOS记录号: WOS:000305815900005
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59683
Appears in Collections:北京大学第三临床医学院_心血管内科_期刊论文

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作者单位: 1.AstraZeneca, Strateg Dev, Wilmington, DE 19850 USA
2.Peking Univ, Hosp 3, Dept Cardiol, Beijing 100871, Peoples R China
3.Peking Univ, Hosp 3, Drug Clin Trial Ctr, Beijing 100871, Peoples R China
4.Peking Univ, Dept Pharm, Hosp 3, Beijing 100871, Peoples R China
5.AstraZeneca, Biostat & Informat, Wilmington, DE 19850 USA
6.Bristol Myers Squibb R&D, Discovery Med & Clin Pharmacol, Cardiovasc & Metab Dis, Princeton, NJ USA

Recommended Citation:
Li, Haiyan,Yang, Li,Tou, Conrad K. P.,et al. Pharmacokinetic Study of Saxagliptin in Healthy Chinese Subjects[J]. CLINICAL DRUG INVESTIGATION,2012,32(7):465-473.
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