Sitagliptin

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Sitagliptin
Systematic (IUPAC) name
(3R)-3-amino-1-[9-(trifluoromethyl)- 1,4,7,8-tetrazabicyclo[4.3.0]nona-6,8-d ien-4-yl]- 4-(2,4,5-trifluorophenyl)butan-1-one
Identifiers
CAS number	?
ATC code	?
PubChem	4369359
Chemical data
Formula	C₁₆H₁₅N₅F₆O
Mol. weight	407.314 g/mol
Pharmacokinetic data
Bioavailability	87%
Protein binding	38%
Metabolism	Hepatic (CYP3A4- and CYP2C8-mediated)
Half life	8 to 14 hours^[1]
Excretion	Renal (80%)^[1]
Therapeutic considerations
Pregnancy cat.	B(US)
Legal status	℞-only(US)
Routes	Oral

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 along side of metformin for control of type II diabetes mellitus. The benefit of this medicine is expected to be its lower side-effects of hypoglycemia 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) on the pancreas at the level of release of glucagon (diminishes its release) and a the level of insulin (increases its synthesis and release) until blood glucose levels are restored toward normal, in which case the protein/enzyme-enzyme inhibitor becomes less effective and the amounts of insulin released diminishes thus diminishing the "overshoot" of hypoglycemia seen in other oral hypoglycemic agents.

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.

[edit] See also

[edit] 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.

[edit] External links

Merck Announces FDA Acceptance of New Drug Application for JANUVIA™ - Merck press release.
The race to get DPP-4 inhibitors to market - Forbes.com
Sitagliptin - glucagon.com
About DPP-4 - glucagon.com

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Oral antidiabetic drugs (A10B) edit
Biguanides:	Metformin
Sulfonylureas:	Chlorpropamide, glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide
Alpha-glucosidase inhibitor:	Acarbose, Miglitol
Thiazolidinediones (TZD):	Pioglitazone, Rosiglitazone, Troglitazone
Meglitinides:	Nateglinide, Repaglinide, Mitiglinide
Dipeptidyl peptidase-4 (DPP-4) inhibitors:	Saxagliptin, Sitagliptin, Vildagliptin