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Sitagliptin
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Sitagliptin |
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Systematic (IUPAC) name |
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(3R)-3-amino-1-[9-(trifluoromethyl)- |
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Identifiers |
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? |
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Chemical data |
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Pharmacokinetic data |
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87% |
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38% |
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8 to 14 hours[1] |
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Therapeutic considerations |
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B(US) |
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Oral |
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Sitagliptin, previously identified as MK-0431, is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. This enzyme-inhibiting drug is to be used either alone or in combination with metformin or a thiazolidinedione for control of type 2 diabetes mellitus. The benefit of this medicine is expected to be its lower side-effects (e.g., less hypoglycemia, less weight gain) in the control of blood glucose values. The drug works to diminish the effects of a protein/enzyme (by the inhibition of this protein/enzyme) that results in a reduced amount of release of glucagon (diminishes its release) and increased release of insulin (increases its synthesis and release) until blood glucose levels are restored toward normal, in which case the the amounts of insulin released and glucagon suppressed diminishes thus diminishing the "overshoot" of hypoglycemia seen with some other oral hypoglycemic agents. One of the big advantages of sitagliptin is that it can be taken as a pill - it does not need to be injected.
Sitagliptin works by inhibiting the inactivation of the incretin GLP-1 and GIP by DPP-4. By preventing GLP-1 and GIP inactivation, GLP-1 and GIP are able to potentiate the secretion of insulin and suppress the release of glucagon by the pancreas.
Sitagliptin incorporates a beta amino acid moiety that allows for a more favorable fit into the active site of DPP-4. The trifluorophenyl moiety also fits into a hydrophobic region of the active site.
It was approved by the U.S. Food and Drug Administration (FDA) on October 17, 2006.[2] Sitagliptin is marketed as Januvia® by Merck & Co. Januvia. Januvia helps to control blood sugar levels people with type 2 diabetes, along with diet and exercise. It works by regulating the levels of insulin your body produces after eating.
On April 2, 2007, FDA approval for the drug Janumet® was announced. Janumet® is a combination of Januvia® and metformin.
See also
References
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^ a b Herman G, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, Snyder K, Hilliard D, Tanen M, Tanaka W, Wang A, Zeng W, Musson D, Winchell G, Davies M, Ramael S, Gottesdiener K, Wagner J (2005). "Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses.". Clin Pharmacol Ther 78 (6): 675-88. PMID 16338283.
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^ U.S. Food and Drug Administration (October 17, 2006). FDA Approves New Treatment for Diabetes. Press release. Retrieved on 2006-10-17.
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Herman G, Bergman A, Liu F, Stevens C, Wang A, Zeng W, Chen L, Snyder K, Hilliard D, Tanen M, Tanaka W, Meehan A, Lasseter K, Dilzer S, Blum R, Wagner J (2006). "Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects.". J Clin Pharmacol 46 (8): 876-86. PMID 16855072.
The information on this web site is intended for information purposes only and is not intended as a substitute for medical advice. Before starting any weight loss program, it is recommended that you consult your physician or other health care professional.