[Rosiglitazone (BRL-49653)].

Article Details

Citation

Kameda N, Okuya S, Oka Y

[Rosiglitazone (BRL-49653)].

Nihon Rinsho. 2000 Feb;58(2):401-4.

PubMed ID
10707565 [ View in PubMed
]
Abstract

Rosiglitazone, a thiazolidinedion antidiabetic agent, improves insulin resistance in patients with type 2 diabetes mellitus. Rosiglitazone binds to PPAR-gamma with high affinity and the in vivo antidiabetic potency of rosiglitazone is correlated with its high biding affinity. In animal models of insulin resistence, rosiglitazone decreased plasma glucose, triglyceride and insulin levels and also prevented diabetic nephropathy and pancreatic islet cell degeneration. In clinical trials in patients with type 2 diabetes mellitus, rosiglitazone, 2 to 12 mg/day (as a single daily dose or 2 divided daily doses), improved glycemic control as demonstrated, by decreases in fasting plasma glucose and HbA1C levels. Rosiglitazone did not appear to increase the risk of hypoglycemia and there was no evidence of hepatotoxicity in pre-clinical trials.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
RosiglitazonePeroxisome proliferator-activated receptor gammaProteinHumans
Yes
Agonist
Details