Saxagliptin
Chemical compound / From Wikipedia, the free encyclopedia
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Saxagliptin, sold under the brand name Onglyza, is an oral hypoglycemic (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class.[1][2] Early development was solely by Bristol-Myers Squibb; in 2007 AstraZeneca joined with Bristol-Myers Squibb to co-develop the final compound and collaborate on the marketing of the drug.
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Trade names | Onglyza |
Other names | BMS-477118 |
AHFS/Drugs.com | Professional Drug Facts |
MedlinePlus | a610003 |
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Routes of administration | By mouth (tablets) |
Drug class | DPP-4 inhibitors |
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Bioavailability | ~75% (Tmax = 2 h) |
Protein binding | negligible |
Metabolism | Liver (CYP3A4 and CYP3A5) |
Elimination half-life | 2.5 h (saxagliptin), 3.1 h (main metabolite) |
Excretion | 22% (Bile duct), 75% (Urine) |
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Formula | C18H25N3O2 |
Molar mass | 315.417 g·mol−1 |
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In April 2016, the U.S. FDA added a warning about increased risk of heart failure.[3] This was based on data in an article that concluded "DPP-4 inhibition with saxagliptin did not increase or decrease the rate of ischemic events, though the rate of hospitalization for heart failure was increased. Although saxagliptin improves glycemic control, other approaches are necessary to reduce cardiovascular risk in patients with diabetes."[4]