Vildagliptin: Difference between revisions

From Proteopedia
Jump to navigation Jump to search
David Canner (talk | contribs)
No edit summary
David Canner (talk | contribs)
No edit summary
Line 1: Line 1:
<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="" align="right" caption="Vildagliptin, better known as Galvus, ([[___]])"/>
<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Vildagliptin/Vilda/1" align="right" caption="Vildagliptin, better known as Galvus"/>
===Better Known as: Galvus===
===Better Known as: Galvus===
* Marketed By:
* Marketed by: Novartis
* Major Indication:
* Major Indication:  
* Drug Class:
* Drug Class:
* Date of FDA Approval (Patent Expiration):
* Date of FDA Approval (Patent Expiration):

Revision as of 16:06, 13 December 2010

Vildagliptin, better known as Galvus

Drag the structure with the mouse to rotate

Better Known as: Galvus

  • Marketed by: Novartis
  • Major Indication:
  • Drug Class:
  • Date of FDA Approval (Patent Expiration):
  • 2009 Sales:
  • Importance:
  • See Pharmaceutical Drugs for more information about other drugs and diseases.

Mechanism of Action

Dipeptidyl Peptidase-4 (DPP-4) is an antigenic membrane serine exopeptidase that cleaves proline dipeptides form the N-terminal end of protein substrates. DPP-4 plays a major role in glucose metabolism as it is responsible for the degradation of incretins, most notably Glucagon-like peptide-1 (GLP-1) and Glucose-dependent insulinotropic polypeptide (GIp). Incretins are a group of gastrointestinal hormones that stimulate insulin biosynthesis and inhibit glucagon secretion after consuming high glucose meals. Since Diabetes is typically caused by a deficiency in insulin secretion or by increased hepatic glucose production, preventing incretin degradation is a viable treatment for diabetics. Vildagliptin is a competitive inhibitor of DPP-4. By inhibiting DPP-4 and subsequently preventing the enzymatic degradation of GLP-1 and GIP, these incretins are able to potentiate the secretion of insulin and suppress the release of glucagon by the pancreas, resulting in controlled blood-glucose levels.[1] Although no crystal structure of Vildagliptin bound DPP-4 has been solved, it is believed to bind in a similar fashion to Sitagliptin and Saxagliptin

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

  1. 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


Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

David Canner