Empagliflozin

Products

Empagliflozin is commercially available in the form of film-coated tablets. It was approved in the EU, the United States, and many countries in 2014 (Jardiance). Empagliflozin is also combined fixed with metformin (Jardiance Met) as well as with linagliptin (Glyxambi). Trijardy XR is a fixed combination of empagliflozin, linagliptin, and metformin.

Structure and properties

Empagliflozin (C23H27ClO7, Mr = 450.9 g/mol) is an -glucoside that is stable to α-glucosidases in the intestine. It has structural similarities to phlorizin, a nonspecific SGLT inhibitor from apple tree bark and a precursor of modern agents.

Effects

Empagliflozin (ATC A10BX12) has antidiabetic and antihyperglycemic properties. It is a competitive, potent, and selective inhibitor of sodiumglucose 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. SGLT1, which is also found in the intestine, is not inhibited by empagliflozin.

Indications

For the treatment of type 2 diabetes mellitus.

Dosage

According to the professional information. Tablets are taken once daily, regardless of meals.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Drug-drug interactions have been described with diuretics, insulins, and insulin secretagogues such as sulfonylureas. Empagliflozin is glucuronidated and is a substrate of OAT, OATP, P-glycoprotein, and BCRP. In contrast, it does not interact with CYP450.

Adverse effects

The most common potential adverse effects include increased urination, thirst, hypoglycemia in combination with other antidiabetic agents, vaginal thrush, vulvovaginitis, balanitis, genital tract infections, and urinary tract infections. The side effects are a result of increased glucose concentrations in the urine.