GSK376501 + rosiglitazone

**GSK376501 + rosiglitazone** is a combination of two small molecules intended for metabolic and endocrine disorders, specifically type 2 diabetes. **GSK376501** is a selective partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ), developed by GSK, evaluated primarily for type 2 diabetes and obesity. Unlike full agonists like rosiglitazone, GSK376501 aims to provide glycemic benefits with potentially fewer side effects, such as less fluid retention or weight gain. **Rosiglitazone** is an established thiazolidinedione that acts as a full agonist at the same receptor (PPARγ), which improves insulin sensitivity but has had safety concerns regarding cardiovascular risk. The two drugs were studied in combination primarily in phase 1 trials to evaluate safety, metabolism, and pharmacokinetics in overweight subjects and those with type 2 diabetes. The combination attempts to harness the benefits of both partial and full PPARγ agonism.

Other names

GSK376501AGSK-376501AGSK 376501A