Luhan Pharmachem Co., Ltd.

What is Vildagliptin?

Vildagliptin (previously identified as LAF237, view trade names Zomelis, Galvus) is an oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucagon release by the alpha cells of the islets of Langerhans in the pancreas.

Vildagliptin has been shown to reduce hyperglycemia in type 2 diabetes mellitus.

Novartis has since withdrawn its intent to submit vildagliptin to the FDA, as of July 2008. The Food and Drug Administration had demanded additional clinical data before it could approve vildagliptin including extra evidence that skin lesions and kidney impairment seen during an early study on animals have not occurred in human trials.

While the drug is still not approved for use in the US, it was approved in February 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions.

Indications of Vildagliptin

Vildagliptin is used to reduce hyperglycemia in type 2 diabetes mellitus.

Pharmacodynamics

Vildagliptin belongs to a class of orally active antidiabetic drugs (DPP-IV inhibitors) that appear to have multiple functional benefits beyond simple blood-glucose control. One of these is a potential protective effect on pancreatic beta cells, which deteriorate in diabetes. Vildagliptin appears to be safe, very well tolerated, and efficacious. Following a meal, gut incretin hormones are released. The most important incretin hormones are GLP-1 and glucose-dependent insulinotropic polypeptide (GIP). These hormones, secreted in the human small intestine, are responsible for insulin release due to increased glucose levels. In contrast to agents that promote insulin secretion via glucose-independent mechanisms, GLP-1’s dependence on glucose concentration is considered beneficial due to a lower risk of hypoglycemia. GLP-1 also inhibits glucagon secretion and increases beta cell mass by stimulating proliferation and neogenesis. However, the clinical utility of GLP-1 is limited by its short half-life (2 minutes). GLP-1 is rapidly degraded by the proteolytic enzyme DPP-IV. To enhance GLP-1 activity, inhibition of the DPP-IV enzyme is emerging as a novel therapeutic approach in the treatment of diabetes. Administration of vildagliptin enhances GLP-1’s ability to produce insulin in response to elevated concentrations of blood glucose, inhibit the release of glucagon following meals, slow the rate of nutrient absorption into the bloodstream, slow the rate of gastric emptying, and reduce food intake.

What is the mechanism of action?

Vildagliptin inhibits dipeptidyl peptidase-4 (DPP-4). This in turn inhibits the inactivation of GLP-1 by DPP-4, allowing GLP-1 to potentiate the secretion of insulin in the beta cells. Dipeptidyl peptidase-4’s role in blood glucose regulation is thought to be through degradation of GIP and the degradation of GLP-1.

What are the side effects of Vildagliptin?

Common: More than 1 in 100 people who take Vildagliptin

decreased blood sugar levels – very low blood sugar levels may lead to loss of consciousness, impairment of brain function, convulsions or death. If your blood sugar levels are low or you are having warning signs of low blood sugar levels you will need to have some sugar.

• feeling dizzy
• gastro-oesophageal reflux
• headaches
• increased sweating
• nausea – this has only been reported when Vildagliptin has been taken in combination with metformin
• oedema of the extremities
• tremors
• weakness
• weight gain

Storage

Store Vildagliptin below 30 degrees Celsius protected from moisture.

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.