IR@PKUHSC  > 北京大学第三临床医学院  > 心血管内科
学科主题临床医学
Pharmacokinetic Study of Saxagliptin in Healthy Chinese Subjects
Li, Haiyan2,3; Yang, Li4; Tou, Conrad K. P.5; Patel, Chirag G.6; Zhao, June1
刊名CLINICAL DRUG INVESTIGATION
2012
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
WOS记录号WOS:000305815900005
资助机构AstraZeneca ; Bristol-Myers Squibb
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/59683
专题北京大学第三临床医学院_心血管内科
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
推荐引用方式
GB/T 7714
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.
APA Li, Haiyan,Yang, Li,Tou, Conrad K. P.,Patel, Chirag G.,&Zhao, June.(2012).Pharmacokinetic Study of Saxagliptin in Healthy Chinese Subjects.CLINICAL DRUG INVESTIGATION,32(7),465-473.
MLA Li, Haiyan,et al."Pharmacokinetic Study of Saxagliptin in Healthy Chinese Subjects".CLINICAL DRUG INVESTIGATION 32.7(2012):465-473.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Li, Haiyan]的文章
[Yang, Li]的文章
[Tou, Conrad K. P.]的文章
百度学术
百度学术中相似的文章
[Li, Haiyan]的文章
[Yang, Li]的文章
[Tou, Conrad K. P.]的文章
必应学术
必应学术中相似的文章
[Li, Haiyan]的文章
[Yang, Li]的文章
[Tou, Conrad K. P.]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。