期刊文献+

肠促胰岛素相关药物的药代动力学/药效学模型研究进展 被引量:1

Review on pharmacokinetic/pharmacodynamic models of the related agents of incretin
原文传递
导出
摘要 肠促胰岛素是一类在食物刺激下由肠道L细胞分泌并能促使胰岛素分泌的激素,其主要包括胰高血糖素样肽-1(GLP-1)受体激动剂类似物和二肽基肽酶-4(DPP-4)抑制剂。药代动力学/药效学(PK/PD)结合模型可以为肠促胰岛素相关药物的治疗和临床研究提供有力的工具,同时,基于机制的模型可以更好地预测给药后的生理学特点和不同给药方案的治疗结果,有利于该类药物新药研发及给药方案的调整。本文主要针对GLP-1受体激动剂类似物和DPP-4抑制剂代表药物基于其作用机制的PK/PD模型进行综述。 Incretin is a hormone released from the L -cells in the gut wall under the stimulation of food and can promote the insulin secretion.The related agents used in the clinic mainly include two types , the gluca-gon-like peptide-1 ( GLP-1 ) receptor agonists and dipeptidyl pepti-dase -4 ( DPP -4 ) inhibitors.Pharmacokinetic/pharmacodynamic ( PK/PD) models of incretin related agents can be useful tools in optimal drug therapy in patients and support the design of future clinical trials.Meanwhile , a mechanism-based model can be more powerful at predic-ting physiological characteritics and the probability of successful outcome of anti -diabetic treatment for different dosage regimens of the drugs , which will be beneficial for new drugs development and dosage regimens regulation.The present review is focused on the mechanism -based PK/PD models of representative drugs which belong to GLP -1 receptor agonists and DPP-4 inhibitors.
作者 臧彦楠 方翼
出处 《中国临床药理学杂志》 CAS CSCD 北大核心 2015年第2期146-149,共4页 The Chinese Journal of Clinical Pharmacology
关键词 肠促胰岛素 胰高血糖素样肽-1受体激动剂类似物 二肽基肽酶-4抑制剂 药代动力学/药效学结合模型 incretin glucagon -like peptide -1 receptor agonists dipeptidyl peptidase -4 inhibitors pharmacokinetic/pharmacodynamic models
  • 相关文献

参考文献1

二级参考文献22

  • 1Weyer C, Bogardus C, Mott DM, Pratley RE. The natural history of insulin secretory dysfunction and insulin resistance in the pathogenesis of type 2 diabetes mellitus. J Clin Invest 1999; 104: 787-94.
  • 2BarnettAH. New treatments in type 2 diabetes:a focus on the incretin-based therapies. Clin Endocrinol (Oxf) 2009; 70: 343-53.
  • 3Drucker DJ. Enhancing incretin action for the treatment of type 2 diabetes. Diabetes Care 2003; 26: 2929-40.
  • 4Parkes DG, Jodka C, Smith P, Nayak S, Rinehart L, Gingerich R, et al. Pharmacokinetic actions of exendin-4 in the rat: comparison with glucagon-like peptide-1. Drug Develop Res 2001; 53: 260-7.
  • 5Zander M, Madsbad S, Madsen JL, Hoist JJ. Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and beta-cell function in type 2 diabetes: a parallel-group study. Lancet 2002; 359: 824-30.
  • 6Parkes DG, Pittner R, Jodka C, Smith P, YoungA. Insulinotropic actions of exendin-4 and glucagon-like peptide-1 in vivo and in vitro. Metabolism 2001; 50 583-9.
  • 7Stoffers DA, Kieffer TJ, Hussain MA, Drucker DJ, Bonner-Weir S, Habener JF, et al. Insulinotropic glucagon-like peptide-1 agonists stimulate expression of homeodomain protein IDX-1 and increase islet size in mouse pancreas. Diabetes 2000; 49: 741-8.
  • 8Goke R, Fehmann HC, Linn T, Schmidt H, Krause M, Eng J, et al. Exendin-4 is a high potency agonist and truncated exendin-(9-39)- amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting beta-cells, J Biol Chem 1993; 268: 19650-5.
  • 9Young AA, Gedulin BR, Bhavsar S, Bodkin N, Jodka C, Hansen B, et al. Glucose-lowering and insulin-sensitizing actions of exendin-4-studies in obese diabetic (ob/ob, db/db) mice, diabetic fatty Zucker rats, and diabetic rhesus monkeys (Macaca mulatta). Diabetes 1999; 48: 1026-34.
  • 10Mager DE, Abernethy DR, Egan JM, Elahi D. Exendin-4 pharmacodynamics: insights from the hyperglycemic clamp technique. J Pharmacol Exp Ther 2004; 311: 830-5.

共引文献8

同被引文献8

引证文献1

二级引证文献5

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部