Name: | sitagliptin |
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PubChem Compound ID: | 11476287 |
Molecular formula: | C16H16ClF6N5O |
Molecular weight: | 443.774 g/mol |
Name: | sitagliptin |
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Name (isomeric): | DB01261 |
Drug Type: | small molecule |
Synonyms: |
Sitagliptan; Sitagliptin phosphate; MK-0431
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Brand: | Xelevia, Januvia (Merck & Co.), Januvia |
Brand name mixture: | Janumet(Sitagliptin + metformin) |
Category: | Dipeptidyl-Peptidase IV Inhibitors, Hypoglycemic Agents |
CAS number: | 486460-32-6 |
Indication: | For use as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. Also for use in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin or a PPARγ agonist (e.g., thiazolidinediones) when the single agent alone, with diet and exercise, does not provide adequate glycemic control. |
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Pharmacology: |
Sitagliptin is an orally-active member of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. 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 pancrea...
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Mechanism of Action: |
Sitagliptin is a highly selective DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones, thereby increasing the concentration and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotrop...
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Absorption: | Rapidly absorbed following oral administration, with an absolute bioavailability of 87%. |
Protein binding: | The fraction of sitagliptin reversibly bound to plasma proteins is low (38%). |
Biotransformation: | Sitagliptin does not undergo extensive metabolism. In vitro studies indicate that the primary enzyme responsible for the limited metabolism of sitagliptin was CYP3A4 (oxidation), with contribution from CYP2C8. |
Route of elimination: | Approximately 79% of sitagliptin is excreted unchanged in the urine with metabolism being a minor pathway of elimination. Following administration of an oral [14C]sitagliptin dose to healthy subjects, approximately 100% of the administered radioactivity was eliminated in feces (13%) or urine (87%) within one week of dosing. Elimination of sitagliptin occurs primarily via renal excretion and involves active tubular secretion. |
Half Life: | 12.4 hours |
Clearance: | renal cl=350 mL/min [Healthy subjects receiving 100 mg oral dose] |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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