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Sitagliptin

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Sitagliptin, better known as Januvia, (1x70)

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Better Known as: Januvia

  • Marketed By: Merck & Co.
  • Major Indication: Hyperglycemia & Type II Diabetes
  • Drug Class: Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
  • Date of FDA Approval (Patent Expiration): 2006 (2017)
  • 2009 Sales: $2.4 Billion
  • Importance:
  • See Pharmaceutical Drugs for more information about other drugs and diseases.

Mechanism of Action

Pharmacokinetics

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

References


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David Canner, Alexander Berchansky
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