Discovery and Development of Linagliptin, A Unique DPP-4 Inhibitor

来源 :2013第三届内分泌与代谢大会暨2013第二届糖尿病大会 | 被引量 : 0次 | 上传用户:rwteng
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  Linagliptin is a novel DPP-4 inhitor from a new structural class.It is a potent, selective and longacting DPP-4 inhibitor due to its tight binding to the enzyme and a slow Koff from the active site.Linagliptin has shown clinical efficacy which is comparable to other members of this class.Linagliptin is unique in its pharmacokinetic behaviour in that most of the compound is cleared unchanged via the bile and only 5 %is cleared via the kidney.Its pharmacokinetics is unchanged in all stages of kidney impairment, thus linagliptin is the only available DPP-4 inhibitor which can be used without dose reduction in all patients.
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