What is GW501516 / Cardarine?
GW501516, commonly known as Cardarine, is a synthetic compound originally developed as a potential treatment for metabolic and cardiovascular diseases. Despite being marketed as a “selective androgen receptor modulator” (SARM) in supplement circles, GW501516 is actually a peroxisome proliferator-activated receptor delta (PPARδ) agonist, not a true SARM. It was developed by GlaxoSmithKline and Ligand Pharmaceuticals in the 1990s but never completed clinical trials due to serious safety concerns.
GW501516 is banned by the World Anti-Doping Agency (WADA) and is not approved by the FDA for human consumption. It is classified as a research chemical and is illegal to sell as a dietary supplement in many countries, including the United States.
Health benefits & uses
Evidence grade: Limited – All evidence comes from animal studies or incomplete human trials.
Preliminary research suggested GW501516 might offer several metabolic benefits, including improved fat oxidation, enhanced endurance, and better glucose tolerance. However, no completed human clinical trials have established safety or efficacy for any therapeutic use.
Animal studies indicated potential for:
- Increased fat burning and weight loss
- Enhanced endurance and exercise performance
- Improved insulin sensitivity
- Better lipid profiles
These findings have never been validated in properly controlled human studies, and the compound’s development was halted due to cancer risks observed in animal testing.
How it works
GW501516 activates PPARδ receptors, which are involved in regulating fat metabolism and energy expenditure. When activated, these receptors promote the expression of genes involved in fatty acid oxidation, potentially shifting the body’s energy utilization from glucose to fat. This mechanism theoretically could enhance endurance and promote fat loss.
The compound also appears to influence muscle fiber composition, potentially increasing the proportion of slow-twitch muscle fibers that are more efficient at burning fat for energy during prolonged exercise.
Dosage
No safe or effective dosage has been established for humans. GW501516 is not approved for human consumption, and there is no recommended daily allowance (RDA) or upper limit (UL) because it is not a recognized nutrient or approved medication.
Underground usage typically reports doses of 10-20mg daily, but these are based on anecdotal reports rather than scientific evidence. Any use should only occur under strict medical supervision as part of approved research protocols.
Food sources
GW501516 does not occur naturally in food sources. It is a synthetic compound created exclusively in laboratories. There are no dietary sources of this substance.
Safety & side effects
GW501516 poses serious safety risks and is considered dangerous for human consumption. Clinical development was terminated when animal studies revealed increased cancer rates, particularly colorectal, liver, bladder, stomach, and thyroid cancers.
Reported side effects and safety concerns include:
- Cancer risk – Multiple tumor types in animal studies
- Liver toxicity
- Cardiovascular complications
- Hormonal disruption
- Unknown long-term effects on human physiology
The FDA has issued warning letters to companies selling GW501516, emphasizing that it is not safe for human consumption and cannot be legally marketed as a dietary supplement.
Interactions
Due to limited human research, comprehensive interaction data is unavailable. However, potential interactions may include:
Medications:
- Diabetes medications – may affect blood glucose levels
- Blood thinners – potential cardiovascular effects
- Liver-metabolized drugs – due to hepatotoxicity risk
Supplements:
- Other PPARδ agonists
- Fat-burning compounds
- Performance-enhancing substances
Who should be cautious
Everyone should avoid GW501516 due to its banned status and cancer risk. Particular caution applies to:
- Athletes subject to drug testing
- Individuals with cancer history or risk factors
- People with liver disease
- Those with cardiovascular conditions
- Pregnant or breastfeeding women
- Adolescents and young adults
- Anyone taking prescription medications
Frequently asked questions
Is Cardarine legal to buy and use?
No, GW501516/Cardarine cannot be legally sold as a dietary supplement in the United States and many other countries. It’s banned by WADA for athletic competition and is considered unsafe for human consumption by regulatory agencies.
Why was Cardarine development stopped?
Clinical development was halted when animal studies showed increased cancer rates across multiple organ systems. The risk-benefit profile was deemed unacceptable for human use.
Are there safer alternatives for fat loss and endurance?
Yes, evidence-based approaches include proper nutrition, regular exercise, adequate sleep, and FDA-approved supplements when appropriate. Consult healthcare providers for safe, effective strategies.
What should I do if I’ve already used Cardarine?
Discontinue use immediately and consult a healthcare provider. Discuss any concerning symptoms and consider appropriate monitoring based on your usage history and risk factors.
Can Cardarine be detected in drug tests?
Yes, WADA-accredited laboratories can detect GW501516 and its metabolites. Use can result in positive drug tests and competition bans for athletes.
Classification:
Typical dose: — · Studied up to: —
References
Authoritative profile & live regulatory status: GW501516 / Cardarine on SupplementIndex →