Rosiglitazone.
Rosiglitazone, a potent thiazolidinedione oral antidiabetic agent recently approved in the US, differs structurally from pioglitazone and troglitazone (other approved thiazolidinediones), with greater PPAR gamma binding affinity and antihyperglycaemic potency in preclinical models. Clinical data on more than 4500 patients with type 2 diabetes show that rosiglitazone is a safe, effective monotherapy or combination therapy, producing significant reductions in haemoglobin A1c and fasting plasma glucose under different dosing regimens. Unlike troglitazone, which has been associated with idiosyncratic hepatotoxicity and rare cases of liver failure and death, rosiglitazone has shown a low incidence of liver abnormalities in more than 3500 patient-years of exposure. No significant food or drug interactions have been reported. Particularly effective as first-line therapy, rosiglitazone is a useful addition to the roster of oral antidiabetic agents.