Cardarine
GW-501516 / GW / Endurobol, GW-0742 · PPAR-delta agonist (unapproved)
What it is
An abandoned GlaxoSmithKline drug candidate that shifts muscle fuel metabolism toward fat oxidation — known for rodent endurance findings, and for why development stopped. GW-0742 is a closely related compound from the same program.
What human evidence shows
Early human trials showed lipid changes; the endurance results the marketing quotes are rodent data. Development was terminated after long-term rodent studies produced tumors at multiple sites; human relevance and any safe exposure threshold are unknown.
Risks
The carcinogenicity finding is THE risk: multi-site tumors in both sexes of both rodent species, with no human long-term data to bound it. Community reassurance about doses and durations is exposure math without a human dataset behind it. WADA-banned with long detection windows.
Legal status
US: not FDA-approved for human use; unscheduled. The FDA has warned about this product category, and marketing it for human use may violate the FD&C Act.
Evidence base
substantial literature
Real human evidence: randomised trial reports, or review-level evidence backed by at least one human trial report.
- phase 3/4
- 0
- randomised
- 4
- reviews
- 0
- human trials
- 6
Counts are of published papers, not distinct trials, and measure how much research exists — not whether this works or is safe for you.
Research (12)
- Roles of the peroxisome proliferator-activated receptors (PPARs) in the pathogenesis of nonalcoholic fatty liver disease (NAFLD)Pharmacol Res · 2023
- GW-501516 GlaxoSmithKline/LigandCurr Opin Investig Drugs · 2006
- Differential effects of selective- and pan-PPAR agonists on experimental steatohepatitis and hepatic macrophages(☆)J Hepatol · 2020
- Anti-inflammatory effects and improved metabolic derangements in ob/ob mice by a newly synthesized prenylated benzopyran with pan-PPAR activityPharmacol Res · 2023
- PPARdelta activator GW-501516 has no acute effect on glucose transport in skeletal muscleAm J Physiol Endocrinol Metab · 2006
- Testing for GW501516 (cardarine) in human hair using LC/MS-MS and confirmation by LC/HRMSDrug Test Anal · 2020
- Effects of the PPAR-beta agonist GW501516 in an in vitro model of brain inflammation and antibody-induced demyelinationJ Neuroinflammation · 2009
- PPARδ agonist enhances colitis-associated colorectal cancerEur J Pharmacol · 2019
- GW501516 facilitated tumor immune escape by inhibiting phagocytosisEur J Pharmacol · 2025
- Exercise Pills: At the Starting LineTrends Pharmacol Sci · 2015
- Recent Updates on Peroxisome Proliferator-Activated Receptor δ Agonists for the Treatment of Metabolic SyndromeMed Chem · 2016
- GLP-1 receptor agonist protects glucose-stimulated insulin secretion in pancreatic β-cells against lipotoxicity via PPARδ/UCP2 pathwayCell Mol Life Sci · 2025
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