GSK0660

GSK0660 is a potent and selective small molecule that functions as an antagonist and inverse agonist of peroxisome proliferator-activated receptor beta/delta (PPARβ/δ). It exhibits significantly lower activity against PPARα and PPARγ. Developed by GSK Plc, GSK0660 has been investigated in preclinical studies for its potential therapeutic applications, including neuroprotection in Parkinson's disease models, efficacy against retinal neovascularization, and enhancement of antitumor immunotherapy by reducing PD-L1 expression. It has also been shown to inhibit the proliferation and differentiation of human retinal microvascular endothelial cells. While GSK0660 is rapidly cleared in vivo and does not accumulate in the blood, its limited bioavailability led to the development of related compounds with improved pharmacokinetic properties, suggesting it is primarily a research tool.