Ertugliflozin is a drug for the treatment of type 2 diabetes.
It is a sodium/glucose cotransporter 2 (SGLT2) inhibitor and is in the class of drugs known as gliflozins.
Trade name Steglatro.
is a drug for the treatment of type 2 diabetes.
In the United States, it was approved by the Food and Drug Administration for use as a monotherapy and as a fixed dose combination with either sitagliptin or with metformin.
Pregnancy category. US: N (Not classified yet)
Routes of administration By mouth.
Bioavailability 100%.
Protein binding 93.6%.
Metabolism-UGT1A9, UGT2B7
Metabolites Glucuronides
Elimination half-life 17 hours
Excretion 41% faeces, 50% urine.
Most common side effects are fungal infections of the vagina and other infections of the female reproductive system.
A combination with metformin is available.
Use contraindicated for patients with severe kidney failure, end-stage renal disease, and dialysis.
Adverse effects: in studies that were mycosis of the genitals in both men and women, vaginal itch, increased urination, thirst, hypoglycaemia, and weight loss.
A rare but life-threatening side effect of gliflozins is ketoacidosis (0.1).
It should be stopped at least four days before scheduled surgery to prevent ketoacidosis.
Combining ertugliflozin with insulin or insulin secretagogues may result in an increased risk for low blood sugar.
Combination with diuretics may result in a higher risk for dehydration and low blood pressure.
After oral intake, it is almost completely absorbed from the gut and undergoes no relevant first-pass effect.
The highest blood plasma concentrations are reached after one hour.
93.6% of the drug is bound to plasma proteins.
It is metabolized mainly to glucuronides,
and cytochrome P450 enzymes have a minor role in its metabolism.
Its half-life is estimated to be 17 hours.
Elimination: 40.9% are eliminated via the feces, with 33.8% unchanged and 7.1% as metabolites.
50.2% of the drug is eliminated in the urine (1.5% unchanged and 48.7% as metabolites).
Ertugliflozin, ertugliflozin/metformin, and ertugliflozin/sitagliptin are approved for medical use.
In patients with type two diabetes with atherosclerotic cardiovascular disease this drug was shown to be non-inferior to placebo in outcome of death and cardiovascular disease, non-fatal myocardian infarction or.nonfatal stroke.