SGLT-2 Inhibitors: Focus on Dapagliflozin

Abstract

Dapagliflozin (trade name FARXIGA) is a sodium-glucose cotransporter-2 (SGLT-2) inhibitor that has transcended its initial antidiabetic application to demonstrate benefits in cardiac and renal diseases. It was first approved by the food and department administration for type 2 diabetes in 2014. Since then, it has gained food and department administration approval for chronic kidney disease in 2021, heart failure with reduced ejection fraction in 2020, and heart failure with preserved ejection fraction in 2023. Thus, dapagliflozin plays a pivotal role in improving patient outcomes. By competitive binding to renal SGLT-2 cotransporters, dapagliflozin effectively prevents glucose and sodium reabsorption, leading to glucosuria. Its pharmacokinetic profile involves minimal cytochrome P450-induced metabolism, rapid absorption with an 18-hour duration of action, and stable effects. Clinical trials have revealed dapagliflozin’s efficacy in glycemic control without the risk of hypoglycemia, making it an advantageous choice for patients insufficiently managed on other antidiabetic drugs. Comparative analysis with other SGLT-2 inhibitors suggests dapagliflozin’s potential superiority in preventing heart failure. Compared to empagliflozin, it has more extended effects, contributing to stable sodium diuresis, reduced blood pressure fluctuations, and potentially lower cardiovascular disease risks. However, it leads to less urinary glucose excretion compared with canagliflozin. Dapagliflozin has specific contraindications, such as type 1 diabetes and end-stage chronic kidney disease. Adverse effects include an increased risk of genital infections, urinary tract infections, and Fournier’s gangrene. A nuanced understanding of dapagliflozin’s benefits and limitations is imperative for informed clinical decision-making in the management of diabetes and its complications.