Cardarine (GW-501516) Analyzed Feature Image

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Introduction

Cardarine, also known as GW501516, is a SARM that was created by Ligand Pharmaceuticals and GlaxoSmithKline in 1992.

However, its classification as a SARM is a bit of a misinterpretation. A more accurate classification for cardarine is a peroxisome proliferator-activated receptor (PPAR) agonist, which are a group of transcription factors that regulate gene expression, cellular development, and energy metabolism.

This drug has been touted as one that can potentially treat metabolic and cardiovascular diseases, and is currently been studied for such purposes.

However, its use in the real-world is within athletic populations because of its apparent fat burning effects.

Does Cardarine Work?

May Protect Against Cancer

Cardarine has shown to have a high affinity and potency for the PPAR receptors [1].

Although it is most well-known for its potential ability to shed body fat, most of the studies on cardarine are actually assessing how it may impact cancer cell growth.

Studies have observed that cardarine triggers anti-inflammatory signaling pathways that are present in pancreatic cancer cells. Specifically, it does so by activating PPAR pathways, suppressing the activity of certain genes, and reducing the production of pro-inflammatory cytokines such as TNFα [2].

Based on lab studies, these mechanisms have induced cytotoxic effects on tumor cells, seen by decreases in cell viability and ultimately cell death [3].

Experts are now seriously considering the potential capacity for cardarine to induce apoptosis in cancer cells and it could potentially be a therapeutic drug for cancer treatment in the future.

May Treat Liver Injuries

In animal studies, administration of cardarine has also shown to treat liver injuries by enhancing the fibrotic response.

This is likely via an increased expression of various profibrotic and pro-inflammatory genes, which promote liver repair via signaling through p38 and JNK-MAPK pathways [4].

May Improve Body Composition

Other evidence suggests the protection of the liver may be due to an increased expression of the genes that regulate beta-oxidation (fat oxidation) and decrease the expression of the proteins involved in lipogenesis (fat storage) [5].

It is this mechanism that cardarine is also heavily linked to improving body composition and assisting weight loss. This is because the PPAR receptors can recruit the transcriptional coactivator PGC-1α, which, in turn, upregulates the expression of proteins involved in increasing energy expenditure and fat metabolism.

Based on its potential ability to increase calorie expenditure, it could help to create an energy deficit that is necessary for weight loss. Even better, as cardarine can increase fatty acid metabolism it can target body fat stores – which is very attractive to those concerned with their body composition [6].

However, some studies show no effects of cardarine on body weight, fat mass, or lean mass [7].

May Improve Endurance

Those who care about exercise performance, especially endurance, may also like these benefits of cardarine. Increasing PPARδ expression in skeletal muscle can reprogram muscle fibre types (more type 1 fibers) to enhance running endurance [8].

In fact, sport nutritionists will actively use dietary methods in order to strategically target and activate PPAR receptors and upregulate PGC1α to enhance endurance adaptations and improve training responses.

Cardarine treatment could therefore represent a viable drug to improve running endurance by increasing the levels of intermediate metabolites and enzymes in fatty acid oxidation pathways [9].

Cardarine Safety And Side Effects

The research on cardarine cannot confirm whether it is a safe compound to be taking.

Experts have found that cardarine may even increase HDL (“good”) cholesterol, lower LDL (“bad”) cholesterol, and reduce the amount of fat in the bloodstream [10] [11].

However, the first studies on cardarine had worrying results as it led to rapid cancer development in several animal organs, causing all research to be abandoned in 2007 [12]. Since, as previously mentioned, newer research has reported anti-cancer effects, which clearly leads to much confusion at this stage.

Further, the activation of PPAR receptors by cardarine has caused impaired bone formation and decreased bone mineral density in some animal studies – thought to be due to alterations in insulin sensitivity [13].

Is Cardarine Legal?

As cardarine is labelled as a SARM, it is currently stated in all countries to be “not for human consumption”.

Quite simply the research so far is not able to clarify the safety of SARMs, and so they have not yet been made available for by pharmaceutical companies.

Cardarine was also placed on the world anti-doping agency “Prohibited List” after they developed a test for its detection in 2009.

Multiple warnings have been made clear to athletes to avoid the use cardarine under any circumstances, as it may give them an unfair performance advantage over their opponents.

Conclusion

Cardarine is a peroxisome proliferator-activated receptor (PPAR) agonist, which can regulate gene expression, cellular development, and energy metabolism.

More research is needed to clarify its physiological effects, but current evidence suggests it has potential to prevent against liver injuries, certain cancers, and increase fat metabolism.

Although many people take the drug to lose fat, there is currently no studies to support that it can effectively increase fat loss in humans.

This SARM has also not confirmed its safety, and may have negative effects on insulin sensitivity, and bone mineral density.

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This article has been reviewed and fact-checked by a certified nutritionist, and only uses information from credible academic sources.