Cardarine (GW501516): Research, Benefits, and Clinical Studies

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Abstract

Cardarine (GW501516) is a PPARδ (Peroxisome Proliferator-Activated Receptor Delta) agonist developed in the 1990s by GlaxoSmithKline (GSK) and Ligand Pharmaceuticals. It was originally studied for metabolic disorders, cardiovascular disease, and obesity.

Cardarine is not a SARM (Selective Androgen Receptor Modulator), though it is often marketed alongside SARMs. Instead, it works by activating PPARδ pathways, which regulate fat metabolism, endurance, and energy utilization.

Mechanism of Action

• Activates PPARδ receptors in skeletal muscle.
• Shifts metabolism toward fatty acid oxidation, sparing glycogen and improving stamina.
• Increases HDL cholesterol and reduces triglycerides in some studies.
• Mimics some effects of endurance training at the cellular level.

Research and Clinical Studies

1. Endurance and Fat Metabolism:
   • Narkar VA, et al. PPARδ activation promotes running endurance by enhancing oxidative metabolism in skeletal muscle. Cell. 2008.
   • Mice treated with GW501516 ran 60–70% longer than controls.
   • PubMed PMID: 18460331
2. Lipid and Metabolic Effects in Humans:
   • Oliver WR, et al. A selective PPARδ agonist reduces atherogenic dyslipidemia in humans. Proc Natl Acad Sci USA. 2001.
   • Reported improvements in HDL and triglyceride profiles.
   • PubMed PMID: 11226258
3. Safety Concerns (Cancer Risk):
   • Preclinical long-term rodent studies found increased cancer development at high doses.
   • Due to these findings, clinical development was discontinued by GSK.

Potential Benefits (Research Context Only)

• Increased endurance and stamina.
• Enhanced fat metabolism and weight management.
• Improved lipid profile (higher HDL, lower triglycerides).
• Possible cardiovascular benefits (in early trials).

Risks and Limitations

• Not FDA-approved and discontinued due to safety concerns.
• Cancer risk observed in rodent studies at high, prolonged exposure.
• Listed on WADA banned substances list (World Anti-Doping Agency).
• Still classified strictly as a research chemical.

CARDARINE FAQ

1. What is Cardarine (GW501516)?
Cardarine is a PPARδ agonist studied for endurance, fat metabolism, and cardiovascular health, but discontinued due to safety concerns.

2. Is Cardarine a SARM?
No — Cardarine is not a SARM. It is a PPARδ activator, but often grouped with SARMs in research markets.

3. Does Cardarine improve endurance?
Yes — animal studies showed significant improvements in running capacity and fat metabolism.

4. Is Cardarine safe?
Long-term animal studies suggested a potential cancer risk, which halted human clinical trials.

5. Is Cardarine FDA-approved?
No — Cardarine is a research chemical only and not approved for human use.

6. Where can I find Cardarine research studies?

• Narkar VA, Cell. 2008. PubMed 18460331
• Oliver WR, PNAS. 2001. PubMed 11226258

Conclusion

Cardarine (GW501516) shows strong preclinical evidence for boosting endurance and fat metabolism by activating PPARδ pathways. However, due to safety concerns and cancer findings in rodent studies, it was discontinued in human trials. It remains a research-only compound and is not FDA-approved for medical use.

NOT FOR HUMAN USE. FOR RESEARCH USE ONLY