GW501516, also known as Cardarine or Endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-δ) agonist extensively researched for its effects on fat burning, muscle production, endurance enhancement, and potential therapeutic applications. Here are some key points based on research findings:

1. Metabolic and Performance Benefits:

   • GW501516 promotes the change from glucose to lipid utilization in the body, increasing fat-burning capacity and muscle production¹.
   • It's often abused for performance enhancement among athletes, despite being prohibited by the World Anti-Doping Agency (WADA) since 2009¹.

2. Health Implications:

   • Although it has shown positive effects on reducing inflammation and improving insulin sensitivity, particularly in high-fructose diet-induced metabolic disturbances², its development as a therapeutic drug was halted due to its tumorigenic effects observed in clinical trials³.
   • Studies suggest anti-cancer properties in certain models, inhibiting cell proliferation and promoting apoptosis in nasopharyngeal carcinoma cells⁴.

3. Regulatory Status and Risks:

   • It is categorized under prohibited substances by WADA due to its potential for misuse and associated health risks¹.
   • Clinical reports indicate severe health issues, such as liver damage and rhabdomyolysis, among individuals abusing GW501516⁵.

4. Research and Clinical Trials:

   • Research on rodents shows the drug can improve markers of liver health and reduce inflammation².
   • Despite these benefits, safety concerns have led to its prohibition and caution among the scientific community³.

Footnotes

1. Pascal Kintz, "Testing for GW501516 (cardarine) in human hair using LC/MS-MS and confirmation by LC/HRMS," PubMed ↩ ↩² ↩³

2. D’Angelo C Magliano, "Short-term administration of GW501516 improves inflammatory state in white adipose tissue and liver damage in high-fructose-fed mice," PubMed ↩ ↩²

3. Martin Weihrauch, "Pharmacological targeting of exercise adaptations in skeletal muscle," NCBI ↩ ↩²

4. Yangyang Ji, "PPARβ/δ Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma," NCBI ↩

5. Pascal Kintz, "Peroxisome Proliferator-Activated Receptor Delta Agonist (PPAR- δ) and Selective Androgen Receptor Modulator (SARM) Abuse," NCBI ↩