Vildagliptin: Difference between revisions
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<applet load="" size="480" color="" frame="true" spin="on" Scene ="Vildagliptin/Vilda/ | <applet load="" size="480" color="" frame="true" spin="on" Scene ="Vildagliptin/Vilda/3" align="right" caption="Vildagliptin, better known as Galvus"/> | ||
===Better Known as: Galvus=== | ===Better Known as: Galvus=== | ||
* Marketed by: Novartis | * Marketed by: Novartis | ||
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===Mechanism of Action=== | ===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 [[Carbohydrate Metabolism|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.<ref>PMID:17073841</ref> 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]] | 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 [[Carbohydrate Metabolism|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.<ref>PMID:17073841</ref> 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=== | ===Pharmacokinetics=== | ||