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Saxagliptin, better known as Onglyza, (3bjm)

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DPP4 Inhibitor Pharmacokinetics
Parameter Vildagliptin
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


  1. Wesley UV, McGroarty M, Homoyouni A. Dipeptidyl peptidase inhibits malignant phenotype of prostate cancer cells by blocking basic fibroblast growth factor signaling pathway. Cancer Res. 2005 Feb 15;65(4):1325-34. PMID:15735018 doi:10.1158/0008-5472.CAN-04-1852
  2. Barnett A. DPP-4 inhibitors and their potential role in the management of type 2 diabetes. Int J Clin Pract. 2006 Nov;60(11):1454-70. PMID:17073841 doi:10.1111/j.1742-1241.2006.01178.x
  3. Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, Hickey GJ, Kowalchick JE, Leiting B, Lyons K, Marsilio F, McCann ME, Patel RA, Petrov A, Scapin G, Patel SB, Roy RS, Wu JK, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE. (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin -7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem. 2005 Jan 13;48(1):141-51. PMID:15634008 doi:10.1021/jm0493156
  4. Metzler WJ, Yanchunas J, Weigelt C, Kish K, Klei HE, Xie D, Zhang Y, Corbett M, Tamura JK, He B, Hamann LG, Kirby MS, Marcinkeviciene J. Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation. Protein Sci. 2008 Feb;17(2):240-50. PMID:18227430 doi:17/2/240

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