GSK523338

GSK523338 is a fixed-dose combination drug candidate developed by GSK, consisting of the thiazolidinedione rosiglitazone and the HMG-CoA reductase inhibitor simvastatin. It was designed to simultaneously address glycemic control and hypercholesterolemia in patients with type 2 diabetes mellitus. Rosiglitazone acts as a selective agonist for the peroxisome proliferator-activated receptor-gamma (PPARγ), which improves insulin sensitivity by regulating the transcription of genes involved in glucose and lipid metabolism. Simvastatin inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis, thereby reducing LDL-cholesterol levels. The development of this combination was evaluated in clinical trials but was ultimately not pursued for commercialization, likely due to the evolving safety profile and cardiovascular concerns associated with rosiglitazone.

Other names

rosiglitazone + simvastatinrosiglitazone/simvastatin