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Binding to dipeptidyl peptidase-4 determines the disposition of linagliptin (BI 1356) – investigations in DPP-4 deficient and wildtype rats by Silke Retlich; Barbara Withopf; Andreas Greischel; Alexander Staab; Ulrich Jaehde; Holger Fuchs is a Medicine article available to read on EtoBox.
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## Abstract Linagliptin (BI 1356) is a novel dipeptidyl peptidase‐4 (DPP‐4) inhibitor in clinical development for the treatment of type 2 diabetes. It exhibits non‐linear pharmacokinetics and shows concentration‐dependent plasma protein binding to its target, DPP‐4. The aim of this study was to investigate the impact of saturable binding of linagliptin to plasma and tissue DPP‐4 by comparing the pharmacokinetics of linagliptin in wildtype and DPP‐4 deficient Fischer rats using non‐compartmental and model‐based data analysis. The non‐compartmental analysis revealed a significantly reduced __AUC__ in DPP‐4 deficient rats compared with wildtype rats when single intravenous doses ⩽1 mg/kg were administered, but the exposure was similar in both strains at higher doses. The terminal half‐lives were significantly shorter in DPP‐4 deficient rats compared with wildtype rats. For doses ⩽1 mg/kg, DPP‐4 deficient rats exhibited linear pharmacokinetics, whereas the pharmacokinetics of wildtype rats was non‐linear. In the model‐based analysis these differences could be accounted for by assuming concentration‐dependent protein binding in the central and one peripheral compartment in wildtype rats
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- Author
- Silke Retlich; Barbara Withopf; Andreas Greischel; Alexander Staab; Ulrich Jaehde; Holger Fuchs
- Publisher
- John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0142-2782)
- Published
- 2009
- Language
- EN
- Field
- Medicine (Health Sciences)