Comparative pharmacokinetics of three SGLT-2 inhibitors sergliflozin, remogliflozin and ertugliflozin: an overview

Abstract

1. Several sodium-glucose cotransporter-2 (SGLT-2) inhibitors are in clinical use for the management of type 2 diabetes. The objectives of the current review were: (a) to provide a comparative pharmacokinetics including absorption, distribution, metabolism and excretory (ADME) profiles of three SGLT-2 inhibitors namely: sergliflozin, remogliflozin and ertugliflozin; (b) to provide some perspectives on possible developmental issues.

2. Based on the half-life (t_1/2) values observed in humans, the rank order of the three SGLT-2 inhibitors was ertugliflozin (16 h) > remogliflozin (2–4 h) > sergliflozin (1–1.5 h). Therefore, while once a day dosing of ertugliflozin is possible, the other two drugs need to be dosed more frequently. Perhaps, the short t_1/2 of sergliflozin may have contributed for its discontinuation.

3. Although there was paucity of published data on the metabolism, transporter related and excretory aspects for sergliflozin, the other two drugs provided a differentiating profile. However, the compiled data suggested that there may be a minimal or no risk of pharmacokinetic drug interaction issues associated with any of the reviewed drugs.

4. Because of the crowded development pipeline and approved SGLT-2 inhibitors, the safety and efficacy of sergliflozin, remogliflozin and ertugliflozin appear to be a key from differentiation perspective.

Keywords:

• Clinical pharmacokinetics
• ertugliflozin
• remogliflozin
• sergliflozin

Declaration of interest

The authors have no conflicts of interest or competing interests relevant to the content of the review article.