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| Clinical data | |
|---|---|
| Trade names | Steglatro |
| Other names | PF-04971729, ertugliflozin l-pyroglutamic acid |
| AHFS/Drugs.com | Monograph |
| License data | |
| Pregnancy category | |
| Routes of administration | By mouth |
| Drug class | Antidiabetic agent |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | ~100% |
| Protein binding | 93.6% |
| Metabolism | UGT1A9,UGT2B7 |
| Metabolites | Glucuronides |
| Eliminationhalf-life | ~17 hours |
| Excretion | 41%faeces, 50% urine |
| Identifiers | |
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| CAS Number | |
| PubChemCID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.237.989 |
| Chemical and physical data | |
| Formula | C22H25ClO7 |
| Molar mass | 436.89 g·mol−1 |
| 3D model (JSmol) | |
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Ertugliflozin, sold under the brand nameSteglatro, is amedication used for the treatment oftype 2 diabetes.[3][4]
The most common side effects include fungal infections of the vagina and other infections of the female reproductive system.[4]
Ertugliflozin is asodium/glucose cotransporter 2 (SGLT2)inhibitor[3][4] and is in the class of drugs known asgliflozins.[5]
In the United States, it was approved by theFood and Drug Administration for use as a monotherapy and as a fixed dose combination with eithersitagliptin or withmetformin.[6] In the European Union, it was approved in March 2018, for use as a monotherapy or combination therapy.[7] A study published in September 2020, found that ertugliflozin to be essentially non-inferior toplacebo with respect to cardiovascular events.[8]
A combination withmetformin is sold under the brand name Segluromet and a combination withsitagliptin is sold under the brand name Steglujan.[1][9][10][11][12]
Ertugliflozin isindicated for the treatment of adults with insufficiently controlled type 2 diabetes as an adjunct to diet and exercise as monotherapy when metformin is considered inappropriate due to intolerance or contraindications or in addition to other medicinal products for the treatment of diabetes.[4]
A systematic review and meta-analysis of ertugliflozin, published in 2024, found it to have a good glycemic efficacy and a reassuring safety profile in managing type 2 diabetes.[13]
Under the US approval, ertugliflozin is contraindicated for people with severekidney failure,end-stage renal disease, anddialysis.[3] The European Union approval does not list any contraindications apart from hypersensitivity to the drug, which is standard for all drug approvals.[7]
Adverse effects in studies that were significantly more common under ertugliflozin than underplacebo includedmycosis of the genitals in both men and women, vaginal itch, increased urination, thirst,hypoglycaemia (low blood sugar), and weight loss under the higher dosing scheme.[3]
A rare but life-threatening side effect of gliflozins isketoacidosis; it occurred in three patients (0.1%) in ertugliflozin studies.[3] To lessen the risk of developing ketoacidosis (a serious condition in which the body produces high levels of blood acids called ketones) after surgery, the FDA has approved changes to the prescribing information for SGLT2 inhibitor diabetes medicines to recommend they be stopped temporarily before scheduled surgery.[14] Symptoms of ketoacidosis include nausea, vomiting, abdominal pain, tiredness, and trouble breathing.[14]
Up to sixfold clinical doses over two weeks, or 20-fold single doses, are tolerated by people without any toxic effects.[7]
Combining ertugliflozin withinsulin or insulin secretagogues (such assulfonylureas) may result in an increased risk for low blood sugar. Combination withdiuretics may result in a higher risk fordehydration andlow blood pressure. No clinically relevantpharmacokinetic interactions have been found in studies.[3][7]
After oral intake, ertugliflozin is practically completely absorbed from the gut and undergoes no relevantfirst-pass effect. Highestblood plasma concentrations are reached after one hour. When in circulation, 93.6% of the substance are bound toplasma proteins. Ertugliflocin is metabolised mainly toglucuronides by the enzymesUGT1A9 andUGT2B7.Cytochrome P450 enzymes play only a minor role in its metabolism.[3][7]
Theelimination half-life is estimated to be 17 hours. 40.9% are eliminated via thefeces (33.8% in unchanged form and 7.1% as metabolites) and 50.2% via the urine (1.5% unchanged and 48.7% as metabolites). The high proportion of unchanged substance in the feces is probably due tohydrolysis of the metabolites back to the parent substance.[3][7]
Ertugliflozin,ertugliflozin combined with metformin, andertugliflozin combined with sitagliptin were approved for medical use in the United States in December 2019,[9][11] and in the European Union in March 2018.[4][10][12]
This article incorporates text from this source, which is in thepublic domain.