The Sound of Evolution
Dapagliflozin
Mechanism of action:
Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor (SGLT2 inhibitor). Under normal conditions, the proximal convoluted tubule of the kidney reabsorbs about 90% of filtered glucose through SGLT2, while the remaining 10% is absorbed by SGLT1. Dapagliflozin inhibits the function of SGLT2, preventing glucose from being reabsorbed and causing it to be excreted in the urine, thereby lowering blood glucose levels. It is also associated with osmotic diuresis and natriuresis, which can reduce blood pressure and decrease fluid volume.
Reference(s):
1. Obermeier M et al. (2010). In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans. Drug Metab Dispos.
2. Kasichayanula S et al. (2014). Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet.