Products
Saxagliptin is commercially available in the form of film-coated tablets (Onglyza). It was approved in many countries after sitagliptin (Januvia) and vildagliptin (Galvus) as the 3rd active ingredient from the gliptins group in February 2010. Since 2012, two additional combination products with metformin have been registered (Duoglyze, Kombiglyze XR). Kombiglyze XR entered the market in February 2013. In 2017, a combination with dapagliflozin was released (Qtern). Qtrilmet is a fixed-dose combination with metformin and dapagliflozin.
Structure and properties
Saxagliptin (C18H25N3O2, Mr = 315.41 g/mol) is present in drugs as saxagliptin hydrochloride, a white to slightly yellow or brown crystalline powder that is sparingly soluble in water.
Effects
Saxagliptin (ATC A10BH03) has antidiabetic properties. The effects are due to selective and competitive inhibition of dipeptidyl peptidase-4 (DPP-4). Saxagliptin promotes insulin synthesis and release from pancreatic beta cells, improves beta cell sensitivity to glucose, and increases its uptake into tissues. It reduces glucagon secretion from alpha cells, resulting in decreased glucose production in the liver see also under Gliptins.
Indications
As monotherapy or in combination with other antidiabetic agents for the treatment of type 2 diabetes mellitus.
Dosage
According to the SmPC. Tablets are taken once daily and independently of meals (monotherapy).
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Saxagliptin is metabolized by CYP3A4/5. Corresponding interactions with CYP inhibitors and inducers are possible.
Adverse effects
The most common potential adverse effects include colds, urinary tract infections, gastroenteritis, sinusitis, headache, vomiting, and edema. Like other gliptins, saxagliptin can rarely cause pancreatitis.
