Dipeptidyl Peptidase-4 Inhibitor Pharmacokinetics

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(New page: {| class="wikitable" border="0px" width="100%" style="text-align:center" |- ! colspan="5" align="center"| DPP4 Inhibitor Pharmacokinetics |- ! Parameter ! Vildagliptin<br/>(Galvus...)
Current revision (10:17, 13 December 2010) (edit) (undo)
 
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|-
|-
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
-
! [[Vildagliptin]]<br/>(Galvus)
+
! 1.75
-
! [[Sitagliptin]]<br/>(Januvia)
+
! 1-4
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 2
|-
|-
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
-
! [[Vildagliptin]]<br/>(Galvus)
+
! 290
-
! [[Sitagliptin]]<br/>(Januvia)
+
! 330
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 34
|-
|-
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
-
! [[Vildagliptin]]<br/>(Galvus)
+
! 85
-
! [[Sitagliptin]]<br/>(Januvia)
+
! 87
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 67
|-
|-
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
-
! [[Vildagliptin]]<br/>(Galvus)
+
! 9
-
! [[Sitagliptin]]<br/>(Januvia)
+
! 38
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 0
|-
|-
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
-
! [[Vildagliptin]]<br/>(Galvus)
+
! 2-3
-
! [[Sitagliptin]]<br/>(Januvia)
+
! 12.4
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 2.5
|-
|-
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
-
! [[Vildagliptin]]<br/>(Galvus)
+
! 1610
-
! [[Sitagliptin]]<br/>(Januvia)
+
! 3470
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 101
|-
|-
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
-
! [[Vildagliptin]]<br/>(Galvus)
+
! 3
-
! [[Sitagliptin]]<br/>(Januvia)
+
! 18
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 50
|-
|-
-
! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
+
! [[Pharmacokinetics#Clearance_.28Cl.29|Renal Clearance]] (L/h)
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! [[Vildagliptin]]<br/>(Galvus)
+
! 13.0
-
! [[Sitagliptin]]<br/>(Januvia)
+
! 21.0
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 13.8
 +
|-
 +
! [[Pharmacokinetics#Volume_of_Distribution_.28Vd.29|Volume Distribution]] (L)
 +
! 71
 +
! 198
 +
! 151
|-
|-
! Dosage (mg)
! Dosage (mg)
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! [[Vildagliptin]]<br/>(Galvus)
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! 100
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! [[Sitagliptin]]<br/>(Januvia)
+
! 100
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! 5
|-
|-
! Metabolism
! Metabolism
-
! [[Vildagliptin]]<br/>(Galvus)
+
! Hydrolysis
-
! [[Sitagliptin]]<br/>(Januvia)
+
! Hepatic (CYP3A4 & CYP2C8)
-
! [[Saxagliptin]]<br/>(Onglyza)
+
! Hepatic (CYP3A4)
|}
|}
-
For Pharmacokinetic Data References, see: [[Treatments:AChE Inhibitor References|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

Proteopedia Page Contributors and Editors (what is this?)

David Canner

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