Objective: Peroxisome proliferator-activated receptor-δ-induced upregulation in skeletal muscle fatty acid oxidation would predict the modulation of lipid/lipoproteins VSports手机版. .

Methods and results: GW501516 (2. 5, 5. 0, or 10. 0 mg) or placebo was given for 12 weeks to patients (n=268) with high-density lipoprotein (HDL) cholesterol <1. 16 mmol/L. Fasting lipids/apolipoproteins (apos), insulin, glucose, and free fatty acid were measured; changes from baseline were calculated and assessed. A second smaller exploratory study (n=37) in a similar population was conducted using a sequence of 5 and 10 mg dosing for the assessment of lipoprotein particle concentration. GW501516 demonstrated HDL cholesterol increases up to 16 V体育安卓版. 9% (10 mg) and apoA-I increases up to 6. 6%. Reductions were observed in low-density lipoprotein (LDL) cholesterol (-7. 3%), triglycerides (-16. 9%), apoB (-14. 9%), and free fatty acids (-19. 4%). The exploratory study showed significant reductions in the concentration of very LDL (-19%), intermediate-density lipoprotein (-52%), and LDL (-14%, predominantly a reduction in small particles), whereas the number of HDL particles increased (+10%; predominantly medium and large HDL). .

Conclusions: GW501516 produced significant changes in HDL cholesterol, LDL cholesterol, apoA1, and apoB V体育ios版. Fewer very LDL and larger LDL support a transition toward less atherogenic lipoprotein profiles. These data are consistent with peroxisome proliferator-activated receptor-δ being a potentially important target for providing cardiovascular protection in metabolic syndrome-like patients. .