Dipeptidyl Peptidase-4 Inhibitor Pharmacokinetics
From Proteopedia
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! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ||
| - | ! | + | ! 290 |
| - | ! | + | ! 330 |
| - | ! | + | ! 34 |
|- | |- | ||
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ||
! 85 | ! 85 | ||
! 87 | ! 87 | ||
| - | ! | + | ! 67 |
|- | |- | ||
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ||
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! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
| - | ! | + | ! 1610 |
| - | ! | + | ! 3470 |
| - | ! | + | ! 101 |
|- | |- | ||
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ||
! 3 | ! 3 | ||
! 18 | ! 18 | ||
| - | ! | + | ! 50 |
|- | |- | ||
! [[Pharmacokinetics#Clearance_.28Cl.29|Renal Clearance]] (L/h) | ! [[Pharmacokinetics#Clearance_.28Cl.29|Renal Clearance]] (L/h) | ||
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! 21.0 | ! 21.0 | ||
! 13.8 | ! 13.8 | ||
| + | |- | ||
| + | ! [[Pharmacokinetics#Volume_of_Distribution_.28Vd.29|Volume Distribution]] (L) | ||
| + | ! 71 | ||
| + | ! 198 | ||
| + | ! 151 | ||
|- | |- | ||
! Dosage (mg) | ! Dosage (mg) | ||
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! Metabolism | ! Metabolism | ||
| - | ! | + | ! Hydrolysis |
| - | ! | + | ! Hepatic (CYP3A4 & CYP2C8) |
| - | ! | + | ! Hepatic (CYP3A4) |
|} | |} | ||
For Pharmacokinetic Data References, see: [[Treatments:Dipeptidyl Peptidase-4 Inhibitor Pharmacokinetics|References]] | For Pharmacokinetic Data References, see: [[Treatments:Dipeptidyl Peptidase-4 Inhibitor Pharmacokinetics|References]] | ||
Current revision
| DPP4 Inhibitor Pharmacokinetics | ||||
|---|---|---|---|---|
| Parameter | Vildagliptin (Galvus) | Sitagliptin (Januvia) | Saxagliptin (Onglyza) | |
| Tmax (hr) | 1.75 | 1-4 | 2 | |
| Cmax (ng/ml) | 290 | 330 | 34 | |
| Bioavailability (%) | 85 | 87 | 67 | |
| Protein Binding (%) | 9 | 38 | 0 | |
| T1/2 (hr) | 2-3 | 12.4 | 2.5 | |
| AUC (ng/ml/hr) | 1610 | 3470 | 101 | |
| IC50 (nM) | 3 | 18 | 50 | |
| Renal Clearance (L/h) | 13.0 | 21.0 | 13.8 | |
| Volume Distribution (L) | 71 | 198 | 151 | |
| Dosage (mg) | 100 | 100 | 5 | |
| Metabolism | Hydrolysis | Hepatic (CYP3A4 & CYP2C8) | Hepatic (CYP3A4) | |
For Pharmacokinetic Data References, see: References
