Cardarine (GW-501516)

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What Is Cardarine (GW-501516)?

Cardarine also known as GW-501516 or Endurobol is a synthetic PPARδ receptor agonist originally developed in the 1990s by Ligand Pharmaceuticals and GlaxoSmithKline (GSK). It was initially researched as a potential treatment for metabolic conditions including dyslipidaemia, obesity and cardiovascular disease.^[1]

Although often grouped with SARMs, Cardarine is not a selective androgen receptor modulator. It does not bind to androgen receptors and does not directly influence testosterone or other hormones. Both WADA and USADA classify it separately as a metabolic modulator under section S4.5 of the Prohibited List.^[2][3]

How Does Cardarine Work?

GW-501516 activates the PPARδ receptor with high selectivity (over 1,000-fold vs PPARα and PPARγ).^[1] In animal models, this activation upregulates genes involved in fatty acid oxidation and energy expenditure, essentially shifting the body’s fuel preference from glucose towards stored fat.^[1][4]

A 2015 study published in Scientific Reports (Nature) demonstrated that GW-501516 treatment in mice increased running endurance and raised the proportion of oxidative muscle fibres. The researchers concluded that the compound promotes fatty acid consumption while reducing glucose utilisation a mechanism distinct from exercise itself.^[4]

What Happened in Human Trials

A small number of short-term human trials were completed before the development was halted.

• Phase I (n=24, 2 weeks): GW-501516 at 2.5-10 mg/day significantly improved HDL cholesterol and reduced triglycerides in healthy volunteers. Published in Arteriosclerosis, Thrombosis, and Vascular Biology, 2007.^[5]
• Phase II (n=268, 12 weeks): At 10 mg/day, GW-501516 increased HDL cholesterol by up to 16.9 %, reduced LDL cholesterol by 7.3 %, triglycerides by 16.9 %, and free fatty acids by 19.4 %. No adverse events were reported during the study period. Published in the same journal, 2012.^[6]

These results were verified and peer-reviewed. However, the trial durations were short (2-12 weeks) and participant numbers were small, meaning they cannot establish long-term safety.^[6][7]

Why Was Development Stopped? Safety & Side Effects

Important safety information: GSK abandoned all clinical development of GW-501516 in 2007 after long-term preclinical studies showed that the compound caused cancer to develop rapidly across multiple organs including the liver, bladder, stomach, skin, thyroid, tongue, testes, ovaries and uterus in both rats and mice.^[1][8] The PPARδ activation pathway itself is believed to be the mechanism responsible.^[1] No regulatory authority anywhere in the world has approved Cardarine for human use.

Some proponents have pointed out that the doses used in animal studies were higher than those typically used in humans. However, the human equivalent dose was only roughly 5-10× the commonly discussed 10-20 mg range a very narrow safety margin by pharmaceutical standards, and one GSK judged unacceptable.^[8][9] In 2013, WADA issued a rare public health warning, stating that “clinical approval has not, and will not be given for this substance.”^[2] In Australia, Cardarine was reclassified as a Schedule 10 poison in 2018.^[7]

No long-term human safety data are available. The cancer risk identified in animal models has never been adequately studied in humans because the preclinical findings made further trials unethical.^[7][8]

Capsules vs Liquid Which Format to Buy

When you buy Cardarine in the UK, you’ll typically find two formats. Capsules (10 mg per cap, 60 or 90 count) are the most popular because they are pre-dosed, portable, and convenient. Liquid solutions (10 mg/ml with a calibrated dropper) are suitable for researchers who require finer measurement control. Both contain the same compound at the same purity; the difference is pu y practical.

What to Check Before You Buy Cardarine in the UK

GW-501516 is an unregulated research compound; therefore, its quality varies between suppliers. Before purchasing, look for the following:

• Independent third-party COA not just in-house analysis
• HPLC purity report confirming compound identity and concentration
• Heavy metals screening for lead, mercury, arsenic and cadmium
• Batch-level traceability linking each product to its specific lab report

Legal Status in the UK

GW-501516 is not a controlled substance under UK law (Misuse of Drugs Act 1971 / Psychoactive Substances Act 2016) and can be legally purchased and possessed. However, it is not approved for human use by the MHRA or any global regulator, cannot be legally marketed as a food supplement or medicine, and is banned in all WADA-governed sports under section S4.5. Multiple athletes have received suspensions for positive GW-501516 tests.^[1][2][3]

Cardarine FAQ

Is Cardarine a SARM?No. Cardarine (GW-501516) is a PPARδ receptor agonist. It does not bind to androgen receptors and is classified separately from SARMs by both WADA and USADA.^[2][3]

Has Cardarine ever been tested on humans?Yes, in short-term Phase I and Phase II trials (2-12 weeks, up to 268 participants). These trials showed improved lipid profiles and no adverse events during the study periods. However, no long-term human safety study has been conducted.^[5][6]

Why was Cardarine removed from clinical development?GlaxoSmithKline stopped all development in 2007 after long-term animal studies showed rapid cancer development in multiple organs in both rats and mice.^[1][8]

Does Cardarine suppress testosterone?GW-501516 is a non-hormonal compound that does not interact with androgen receptors. The limited human trial data showed no testosterone suppression, which is consistent with its PPARδ mechanism of action.^[6]

Is Cardarine legal in the UK?GW-501516 is not a controlled substance in the UK and can be legally purchased and possessed. It is, however, not approved for human use, cannot be sold as a supplement or medicine, and is prohibited by WADA in competitive sport.^[2][3]

Is Cardarine banned in sports?Yes. It has been on the WADA Prohibited List since 2009 (section S4.5, PPARδ agonists) and is banned at all times. Athletes across cycling, boxing and athletics have received suspensions for positive tests.^[1][2][10]

References

1. [1] GW501516 Wikipedia. Development history, mechanism, cancer findings, athlete sanctions. en.wikipedia.org
2. [2] WADA “WADA Issues Alert on GW501516.” Official 2013 health warning. wada-ama.org
3. [3] USADA “What Should Tested Athletes Know About GW1516?” usada.org
4. [4] Chen W. et al. “A metabolomic study of the PPARδ agonist GW501516 for enhancing running endurance in Kunming mice.” Sci. Rep. 2015; 5:9884. PubMed
5. [5] Sprecher DL et al. “Triglyceride:HDL-C effects in healthy subjects administered a PPARδ agonist.” Arterioscler. Thromb. Vasc. Biol. 2007; 27(2):359-365. PubMed
6. [6] Olson EJ et al. “Lipid effects of PPARδ agonist GW501516 in subjects with low HDL cholesterol.” Arterioscler. Thromb. Vasc. Biol. 2012; 32(9):2289-2294. PubMed
7. [7] Healthy Male (Andrology Australia) “What is cardarine or GW1516 and what are its side effects?” Includes Australian Schedule 10 classification. healthymale.org.au
8. [8] PMC “PPARβ/δ: a potential in pulmonary hypertension blighted by cancer risk.” Pulm. Circ. 2019. PMC
9. [9] Michigan Medicine “High fat diet, unregulated athletic exercise endurance enhancers linked to risk of pancreatic cancer.” michiganmedicine.org
10. [10] WADA The Prohibited List. GW1516 listed under S4.5 Metabolic Modulators. wada-ama.org
11. [11] DrugBank Cardarine (DB05416). Pharmacology and drug classification. drugbank.com
12. [12] Healthline “Cardarine: Benefits, Side Effects, Dosage, and More.” healthline.com