| Title : Binding to dipeptidyl peptidase-4 determines the disposition of linagliptin (BI 1356)--investigations in DPP-4 deficient and wildtype rats - Retlich_2009_Biopharm.Drug.Dispos_30_422 |
| Author(s) : Retlich S , Withopf B , Greischel A , Staab A , Jaehde U , Fuchs H |
| Ref : Biopharmaceutics & Drug Disposition , 30 :422 , 2009 |
|
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 |
| PubMedSearch : Retlich_2009_Biopharm.Drug.Dispos_30_422 |
| PubMedID: 19771584 |
| Inhibitor | Linagliptin |
Retlich S, Withopf B, Greischel A, Staab A, Jaehde U, Fuchs H (2009)
Binding to dipeptidyl peptidase-4 determines the disposition of linagliptin (BI 1356)--investigations in DPP-4 deficient and wildtype rats
Biopharmaceutics & Drug Disposition
30 :422
Retlich S, Withopf B, Greischel A, Staab A, Jaehde U, Fuchs H (2009)
Biopharmaceutics & Drug Disposition
30 :422