Differences in kidney-specific DPP-4 inhibition by linagliptin and sitagliptin

Diabetes Res Clin Pract. 2018 Sep:143:199-203. doi: 10.1016/j.diabres.2018.07.009. Epub 2018 Jul 18.

Abstract

The two dipeptidyl peptidase (DPP)-4 inhibitors, linagliptin and sitagliptin, were shown to exert different binding kinetics in vitro. Twenty-four hours after oral dosing particularly in vivo inhibition of renal-specific DPP-4 activity was more sustained in Sprague Dawley rats after exposure to linagliptin than it was after sitagliptin.

MeSH terms

  • Animals
  • Dipeptidyl Peptidase 4 / blood
  • Dipeptidyl Peptidase 4 / metabolism
  • Dipeptidyl-Peptidase IV Inhibitors / pharmacology*
  • Kidney / drug effects*
  • Kidney / enzymology
  • Linagliptin / pharmacology*
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Sitagliptin Phosphate / pharmacology*

Substances

  • Dipeptidyl-Peptidase IV Inhibitors
  • Linagliptin
  • Dipeptidyl Peptidase 4
  • Sitagliptin Phosphate