title: 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 (t1/2) 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 t1/2of 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.
authors.affiliation: a Department of Drug Discovery and Development , Harrison School of Pharmacy, Auburn University , AL , USA and.
authors.forename: Ranjeet Prasad
authors.initials: RP
authors.lastname: Dash
authors.affiliation: a Department of Drug Discovery and Development , Harrison School of Pharmacy, Auburn University , AL , USA and.
authors.forename: R Jayachandra
authors.initials: RJ
authors.lastname: Babu
authors.affiliation: b Zydus Research Centre , Ahmedabad , Gujarat , India.
authors.forename: Nuggehally R
authors.initials: NR
authors.lastname: Srinivas
mesh_terms: D001786:Blood Glucose; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000493:pharmacokinetics*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D005960:Glucosides / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D007004:Hypoglycemic Agents / Q000493:pharmacokinetics*; D011720:Pyrazoles / Q000493:pharmacokinetics*; D051297:Sodium-Glucose Transporter 2
chemical_list: D001786:Blood Glucose; D019086:Bridged Bicyclo Compounds, Heterocyclic; D005960:Glucosides; D007004:Hypoglycemic Agents; D011720:Pyrazoles; C089180:SLC5A2 protein, human; D051297:Sodium-Glucose Transporter 2; C570288:ertugliflozin; C516973:sergliflozin; C532127:remogliflozin etabonate
keywords: Clinical pharmacokinetics; ertugliflozin; remogliflozin; sergliflozin