title: Development of the sodium-glucose co-transporter 2 inhibitor dapagliflozin for the treatment of patients with type 2 diabetes mellitus.
abstract: Dapagliflozin is a highly selective sodium-glucose co-transporter 2 inhibitor developed for the treatment of Type 2 diabetes mellitus. Its inhibition of sodium-glucose co-transporter 2 blocks glucose reabsorption in the proximal tubule of the kidney, increasing renal glucose excretion via the urine, resulting in reduction of glycated hemoglobin, fasting plasma glucose and postprandial plasma glucose in patients with Type 2 diabetes mellitus. The pharmacokinetics and pharmacodynamics of dapagliflozin are suitable for once-daily dosing. Dapagliflozin improves glycemic control when used as monotherapy and when used in combination with other antidiabetic treatments. Throughout all phases of clinical studies, dapagliflozin was generally well tolerated. Increased events suggestive of urinary tract and genital infections have been reported; most resolved with conventional treatment. Unexpected numerical imbalances between dapagliflozin and comparator were noted for breast and bladder cancers. The potential for increased cancer risk with dapagliflozin needs to be further assessed.
authors: University of Rochester, School of Medicine, Rochester, NY 14642, USA. johngerich@compuserve.com
authors: John E
authors: JE
authors: Gerich
authors: Arnaud
authors: A
authors: Bastien
mesh_terms: D000818:Animals; D001559:Benzhydryl Compounds; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000378:metabolism; D055808:Drug Discovery / Q000379:methods; D005960:Glucosides / Q000627:therapeutic use*; D006801:Humans; D051297:Sodium-Glucose Transporter 2 / Q000378:metabolism; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D016896:Treatment Outcome
chemical_list: D001559:Benzhydryl Compounds; D005960:Glucosides; C089180:SLC5A2 protein, human; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; C529054:dapagliflozin