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Cardarine

GW-1516, GW501516

Grade D: Preclinical or anecdotal only

TL;DR: Cardarine (GW501516) is a synthetic PPAR-delta agonist originally developed by GlaxoSmithKline for dyslipidemia. The endurance and fat-loss claims it is sold under derive from animal studies and the preclinical exercise-mimetic literature (review PMID 29765854). Human data are limited to small, short-term studies measuring lipid biomarkers such as HDL and triglycerides in healthy or dyslipidemic volunteers (PMID 17110604), which are pharmacology endpoints, not endurance or body-composition efficacy. No randomized controlled efficacy trial in humans has been published, and clinical development was halted in 2007.

Key Takeaways

  • Grade D: Preclinical or anecdotal only
  • Not FDA approved: Not FDA-approved for any indication; never approved for human use. Development was halted by GlaxoSmithKline in 2007. Prohibited at all times in sport by WADA.
  • Compounding: Not an FDA-approved drug and not eligible for legal pharmacy compounding. It is sold only as an unregulated research chemical.

Mechanism

Cardarine (GW501516) is a synthetic PPAR-delta agonist. In animal models it shifts skeletal-muscle fuel use toward fat oxidation, the basis for its marketed endurance and fat-loss claims; these effects have not been demonstrated as clinical efficacy in humans.

Evidence

Cardarine (GW501516) is a synthetic PPAR-delta agonist originally developed by GlaxoSmithKline for dyslipidemia. The endurance and fat-loss claims it is sold under derive from animal studies and the preclinical exercise-mimetic literature (review PMID 29765854). Human data are limited to small, short-term studies measuring lipid biomarkers such as HDL and triglycerides in healthy or dyslipidemic volunteers (PMID 17110604), which are pharmacology endpoints, not endurance or body-composition efficacy. No randomized controlled efficacy trial in humans has been published, and clinical development was halted in 2007.

Safety and risks

GlaxoSmithKline discontinued cardarine in 2007 after long-term rodent studies found it caused tumors to develop rapidly across multiple organs in both mice and rats. That carcinogenicity signal is reinforced by independent peer-reviewed studies showing PPAR-delta activation by cardarine promotes cancer, including acceleration of KRAS-mutant pancreatic carcinogenesis (PMID 35562376), enhancement of colitis-associated colorectal cancer (PMID 30391747), and promotion of tumor immune escape (PMID 39993702). In humans, a 2024 case report documented reversible gynecomastia and hypogonadism in a man using a commercial cardarine-containing supplement (PMID 39145153); that product was also adulterated with undisclosed hormones, so cardarine cannot be isolated as the sole cause. Cardarine is not FDA-approved, is prohibited in sport by WADA, and is sold only as an unregulated research chemical not legally permitted in supplements, foods, or medicines.

Interactions

No human interaction data exist.

Compounding legality

Not an FDA-approved drug and not eligible for legal pharmacy compounding. It is sold only as an unregulated research chemical.

Sources

  1. Differential effects of selective- and pan-PPAR agonists on experimental steatohepatitis and hepatic macrophages(☆). (2020) other
  2. Reversible Gynecomastia and Hypogonadism Due to Usage of Commercial Performance-Enhancing Supplement Use. (2024) observational
  3. Testing for GW501516 (cardarine) in human hair using LC/MS-MS and confirmation by LC/HRMS. (2020) other
  4. Five Novel Polymorphs of Cardarine/GW501516 and Their Characterization by X-ray Diffraction, Computational Methods, Thermal Analysis and a Pharmaceutical Perspective. (2024) other
  5. Rapid acceleration of KRAS-mutant pancreatic carcinogenesis via remodeling of tumor immune microenvironment by PPARδ. (2022) other
  6. GW501516 facilitated tumor immune escape by inhibiting phagocytosis. (2025) other
  7. The disordering effect of SARMs on a biomembrane model. (2024) other
  8. Novel Solid Forms of Cardarine/GW501516 and Their Characterization by X-Ray Diffraction, Thermal, Computational, FTIR, and UV Analysis. (2025) other
  9. SARMs, Metabolic Modulators and Growth Hormone Secretagogues in Suspected Illegal Medicines, Bought as Sport Performance Enhancers: A Retro- and Prospective Study Within the GEON. (2025) other
  10. PPARβ/δ upregulates the insulin receptor β subunit in skeletal muscle by reducing lysosomal activity and EphB4 levels. (2024) other
  11. PPARβ/δ contributes to the antidiabetic effect and the increase in GDF15 caused by metformin. (2026) other
  12. A screening method for the quantitative determination of selective androgen receptor modulators (SARMs) in capsules by high resolution (19)F- and (1)H-NMR spectroscopy. (2024) other
  13. PPARβ/δ attenuates hepatic fibrosis by reducing SMAD3 phosphorylation and p300 levels via AMPK in hepatic stellate cells. (2024) other
  14. Estradiol contributes to sex differences in resilience to sepsis-induced metabolic dysregulation and dysfunction in the heart via GPER-1-mediated PPARδ/NLRP3 signaling. (2024) other
  15. PPARβ/δ agonist GW501516 inhibits TNFα-induced repression of adiponectin and insulin receptor in 3T3-L1 adipocytes. (2019) other
  16. PPARδ agonist enhances colitis-associated colorectal cancer. (2019) other
  17. Molecular and nanoscale evaluation of N-cadherin expression in invasive bladder cancer cells under control conditions or GW501516 exposure. (2020) other
  18. [Effects of GW501516 on the proliferation of pulmonary artery smooth muscle cells induced by hypoxia and its mechanisms]. (2022) other
  19. Fatty acid metabolism suppresses neonatal cardiomyocyte proliferation by increasing PDK4 and HMGCS2 expression through PPARδ. (2025) other
  20. Selective PPARδ Agonist GW501516 Protects Against LPS-Induced Macrophage Inflammation and Acute Liver Failure in Mice via Suppressing Inflammatory Mediators. (2024) other
  21. Inhibitory Effect of PPARδ Agonist GW501516 on Proliferation of Hypoxia-induced Pulmonary Arterial Smooth Muscle Cells by Regulating the mTOR Pathway. (2023) other
  22. The Role of PPARδ Agosnist GW501516 in Rats with Gestational Diabetes Mellitus. (2020) other
  23. Exercise in a Pill: The Latest on Exercise-Mimetics. (2017) review
  24. Peroxisome Proliferator-Activated Receptor Delta Agonist (PPAR- δ) and Selective Androgen Receptor Modulator (SARM) Abuse: Clinical, Analytical and Biological Data in a Case Involving a Poisonous Combination of GW1516 (Cardarine) and MK2866 (Ostarine). (2021) other
  25. GW501516-Mediated Targeting of Tetraspanin 15 Regulates ADAM10-Dependent N-Cadherin Cleavage in Invasive Bladder Cancer Cells. (2024) other
  26. Triglyceride:high-density lipoprotein cholesterol effects in healthy subjects administered a peroxisome proliferator activated receptor delta agonist. (2007) rct

Cardarine is Not FDA approved. PeptideGrids presents evidence and regulatory status for informational purposes only. We do not sell, supply, source, or help anyone obtain this compound, and we provide no dosing or administration guidance. This is not medical advice; consult a licensed clinician. Full disclaimer.

Last reviewed June 2, 2026 by PeptideGrids editorial team (independently audited).