Sitagliptin: Difference between revisions
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* Date of FDA Approval (Patent Expiration): 2006 (2017) | * Date of FDA Approval (Patent Expiration): 2006 (2017) | ||
* 2009 Sales: $2.4 Billion | * 2009 Sales: $2.4 Billion | ||
* Importance: | * Importance: One of the best selling treatments for Type II [[Diabetes]]. Often used in combination with Metformin, the first line anti-diabetic medication (Combination sold as Janumet). Has an excellent side-effect profile with a relatively low incidence of hypoglycemia an weight gain. Increasing evidence that all DPP-4 inhibitors can to certain malignant cancers.<ref>PMID:15735018</ref> | ||
* See [[Pharmaceutical Drugs]] for more information about other drugs and diseases. | * See [[Pharmaceutical Drugs]] for more information about other drugs and diseases. | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
[[Diabetes|Type II Diabetes]] is a chronic metabolic disorder caused by pancrease β-cell dysfunction, deficiency in insulin secretion or insulin resistance, and/or increased hepatic glucose production. Numerous complex systems are involved in this disorder, with several protein serving as therapeutic targets. 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. Sitagliptin 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. The result is controlled blood-glucose levels, a major concern for [[Diabetes|diabetics]]. | |||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||