Products
Ertugliflozin was approved in the United States in 2017 and in the EU and many countries in 2018 in film-coated tablet form (Steglatro). The agent is also combined fixed with sitagliptin (Steglujan) and with metformin (Segluromet).
Structure and properties
Ertugliflozin (C22H25ClO7, Mr = 436.9 g/mol) is present in the drug as ertugliflozin-L-pyroglutamic acid, a white powder that is very sparingly soluble in water.
Effects
Ertugliflozin has antihyperglycemic and antidiabetic properties. It is a selective inhibitor of sodium–glucose co-transporter 2 (SGLT2). This transporter is responsible for the reabsorption of glucose at the proximal tubule of the nephron. Inhibition leads to increased excretion of the sugar via the urine. The mechanism of action is independent of insulin, unlike other antidiabetic agents. Ertugliflozin is specific for SGLT2 and does not inhibit SGLT1, which is responsible for glucose absorption in the intestine.
Indications
For the treatment of type 2 diabetes.
Dosage
According to the professional information. Tablets are taken once daily in the morning, independent of meals. This information refers to monotherapy.
Contraindications
- Hypersensitivity
- Severe kidney disease
Full precautions can be found in the drug label.
Interactions
Ertugliflozin is glucuronidated by UGT1A9 and UGT2B7 to inactive metabolites. The contribution of CYP450 isozymes to metabolism is small. The risk for hypoglycemia is increased when combined with an insulin or agents that promote insulin secretion (insulin secretagogues).
Adverse effects
The most common potential adverse effects include genital fungal infections.
