Rosiglitazone, a potent thiazolidinedione oral antidiabetic agent recently
approved in the tlS, differs structurally from pioglitazone and troglitazon
e (other approved thiazolidinediones), with greater PPAR gamma binding affi
nity 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 r
eductions in haemoglobin A(1c) and fasting plasma glucose under different d
osing regimens. Unlike troglitazone, which has been associated with idiosyn
cratic hepatotoxicity and rare cases of liver failure and death, rosiglitaz
one has shown a low incidence of liver abnormalities in more than 3500 pati
ent-years of exposure. No significant food or drug interactions have been r
eported. Particularly effective as first-line therapy, rosiglitazone is a u
seful addition to the roster of oral antidiabetic agents.