Vildagliptin
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Better Known as: Galvus
- Marketed by: Novartis
- Major Indication:
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- 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
For Pharmacokinetic Data References, see: References |
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References
- ↑ 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