GW501516

Metabolic / Fat Loss

Also known as: Cardarine, GW-501516, GW1516, Endurobol

PPAR AgonistsResearch phase: Phase 2 (abandoned)Regulatory: Not FDA-approved. Development abandoned due to carcinogenicity in rodents. WADA prohibited substance. Available as research chemical.

Mechanism

GW501516 (Cardarine) is a PPARdelta receptor agonist originally developed for metabolic disease that dramatically improves endurance and fat oxidation. It was abandoned during clinical development after rodent studies showed cancer development at high doses over extended periods. Despite this, it remains widely used in performance circles for its powerful effects on stamina and body composition. It is permanently banned by WADA.

Technical detail

GW501516 is a potent and selective PPARdelta (PPARδ) agonist (EC50 ~1 nM) that activates fatty acid oxidation gene programs in skeletal muscle and other tissues. It upregulates CPT1, ACOX1, and PDK4 expression, shifting substrate utilization from glucose to fatty acid oxidation. In preclinical models, it increased running endurance by 68% and reduced body fat without caloric restriction. GlaxoSmithKline and Ligand Pharmaceuticals terminated Phase 2 development after 2-year rodent carcinogenicity studies revealed dose-dependent increases in tumors across multiple organs (liver, bladder, stomach, skin, tongue, thyroid). The human cancer relevance remains debated.

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