Sitagliptin
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.
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
-
^
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.
-
^ U.S. Food and Drug
Administration (October 17, 2006).
FDA Approves New Treatment for Diabetes.
Press release. Retrieved on
2006-10-17.
-
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.
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