Sitagliptin
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| Pronunciation | /sɪtəˈɡlɪptɪn/ ⓘ |
| Trade names | Januvia, Zituvio, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a606023 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | 87% |
| Protein binding | 38% |
| Metabolism | Liver (CYP3A4- and CYP2C8-mediated) |
| Elimination half-life | 8 to 14 h |
| Excretion | Kidney (80%) |
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| ECHA InfoCard | 100.217.948 |
| Chemical and physical data | |
| Formula | C16H15F6N5O |
| Molar mass | 407.320 g·mol−1 |
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Sitagliptin, sold under the brand name Januvia among others, is an anti-diabetic medication used to treat type 2 diabetes. It is in the dipeptidyl peptidase-4 (DPP-4) inhibitor class and works by increasing the production of insulin and decreasing the production of glucagon by the pancreas. In the United Kingdom it is listed as less preferred than metformin or a sulfonylurea. It is taken by mouth. It is also available in the fixed-dose combination medication sitagliptin/metformin (Janumet, Janumet XR).
Common side effects include headaches, swelling of the legs, and upper respiratory tract infections. Serious side effects may include angioedema, low blood sugar, kidney problems, pancreatitis, and joint pain. Whether use in pregnancy or breastfeeding is safe is unclear.
Sitagliptin was developed by Merck & Co. and approved for medical use in the United States in 2006. In 2022, it was the 86th most commonly prescribed medication in the United States, with more than 7 million prescriptions. It is available as a generic medication, but not in the United States.