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QuickView for Saxagliptin (compound)

Name: saxagliptin
PubChem Compound ID: 11243969
Molecular formula: C18H25N3O2
Molecular weight: 315.41 g/mol
Name: saxagliptin
Name (isomeric): DB06335
Drug Type: small molecule
BMS-477118; Onglyza
Brand: Onglyza
CAS number: 361442-04-8
Indication: Investigated for use/treatment in diabetes mellitus type 2.Z\
Mechanism of Action:
Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor antidiabetic for the treatment of Type 2 diabetes. DPP-4 inhibitors are a class of compounds that work by affecting the action of natural hormones in the body called incretins. Incretins decrease blood sugar by increasing consumption of sugar by the body, mainly through increasing insulin pr...
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Absorption: Following the 5 mg once daily dose, the median time to maximum concentration is 2 hours.
Route of elimination: Following a single 50 mg dose of 14C-saxagliptin, 24%, 36%, and 75% of the dose was excreted in the urine as saxagliptin, its active metabolite, and total radioactivity, respectively. A total of 22% of the administered radioactivity was recovered in feces representing the fraction of the saxagliptin dose excreted in bile and/or unabsorbed drug from the gastrointestinal tract.
Half Life: 2.5 hours
Clearance: Renal clearance = 230 mL/min
Drug interaction:
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Saxagliptin. Limit saxagliptin dose to 2.5 mg/day and monitor for increased saxagliptin levels/effects (e.g., hypoglycemia) with concomitant administration of a strong CYP3A4 inhibitor (e.g., ketoconazole). Monitor for decreased saxagliptin levels/effects with discontinuation of concomitant CYP3A4 inhibitor.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of saxagliptin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of saxagliptin if voriconazole is initiated, discontinued or dose changed.
Somatropin recombinantSomatropin may antagonize the hypoglycemic effect of saxagliptin. Monitor for changes in fasting and postprandial blood sugars.