Cardarine (GW-501516) an end of an era?

Update: 06/07/2020

It turns out it is not the end of an era but the beginning of another. Phoenix Gen research has re-engineered the compound to comply with the new government rules. Essentially they altered the molecular structure to represent a unique deriavitive that is not covered by Cardarine legislation. It is called Nano-G-0742-PPAR and works similarly to GW501-516. You can get it from Bear Supplements currently.

Updated: 11/26/2018

The End of Cardarine (GW-501516)?

Well it seems the TGA has reclassified Cardarine as a schedule 10 product. A schedule 10 product is a substance of such danger to health as to warrant prohibition of sale, supply and use so this miracle of weight-loss and fat burning is no longer available to Australians through legitimate sites. You will now have to use black market sites if you wanted to continue using the product as the decision was implemented on June 1 2018.

The TGA Decision on Cardarine (GW 501516)

The TGA which is also know as the Therapeutic Goods Administration received an application to reclassify the product as a schedule 9 substance (prohibited). Whom the applicant is or why the delegates went beyond the recommended classifications are questions for another time, what is important is that at some point in 2017 the TGA recieved this advise:

The applicant’s reasons for the request are:

  • Cardarine is known for its experimental status and it is not being approved for human use.
  • Cardarine GW-501516 is readily available for purchase in Australia through online suppliers, based in Australia and overseas. It is also available through compounding pharmacies and anti-ageing clinics.
  • The lack of regulation allows suppliers to advertise these substances freely and make unproven assertions about the efficacy and safety of the substances. They are administered without reliable advice on appropriate dosage, frequency of administration, and exact content. The products are being positioned as a cutting-edge alternative to steroids on bodybuilding forums and black-market sites.
  • The substances are being used by athletes and gym users for the enhancement of sporting performance and aesthetics.
  • Scheduling these substances aims to protect public health from the potential adverse impacts of these unapproved substances. The unregulated supply poses potentially serious health concerns. They are administered without reliable advice on appropriate dosage, frequency of administration, and exact content.
  • Cardarine (GW501516) may be a potential carcinogen and its effect on humans has not been systematically investigated.
  • The Australian Sports Anti-Doping Authority (ASADA) has advised that cardarine has been seized at the border by the Australian Border Force as a prohibited import on multiple occasions.
  • If Cardarine GW 501516 was marketed, it would require careful regulatory scrutiny. Therefore, in an open, unregulated illicit market, cardarine warrants a listing in the Poisons Standard.
  • Cardarine (GW-501516) has been identified as a substance of abuse with potential carcinogenic effects, and should be considered for a Schedule 9 entry.

Did you get all that? Because its worth looking at in closer detail:

Cardarine is known for its experimental status and it is not being approved for human use.
No evidence supplied as to why this is the case. Basically it isn’t approved so it can’t be approved some incredible circular logic.

 

Cardarine is readily available for purchase in Australia through online suppliers, based in Australia and overseas. It is also available through compounding pharmacies and anti-ageing clinics.
Its not approved but is used widely. Not sure what point they are trying to make.

The lack of regulation allows suppliers to advertise these substances freely and make unproven assertions about the efficacy and safety of the substances. They are administered without reliable advice on appropriate dosage, frequency of administration, and exact content. The products are being positioned as a cutting-edge alternative to steroids on bodybuilding forums and black-market sites.
The answer of course is not to regulate the supply to ensure efficacy and safety but to ban them so that they reside only on black market sites which is the issue they are trying to address.

The substances are being used by athletes and gym users for the enhancement of sporting performance and aesthetics.
No shit, thats because they work amazingly well for that purpose.

Scheduling these substances aims to protect public health from the potential adverse impacts of these unapproved substances. The unregulated supply poses potentially serious health concerns. They are administered without reliable advice on appropriate dosage, frequency of administration, and exact content.
They already said this (it feels a little like the padding you would do to reach a word count for an essay) and the scheduling proposed will ensure the problem they are addressing becomes worse as only the unscrupulous will be able to provide the product now.

Cardarine may be a potential carcinogen and its effect on humans has not been systematically investigated.
Firstly why not investigate the potential carcinogenic effects, secondly everything is potentially a carcinogen these days and if this a legitimate concern how are cigarettes still legal?

The Australian Sports Anti-Doping Authority (ASADA) has advised that cardarine has been seized at the border by the Australian Border Force as a prohibited import on multiple occasions.
Not sure how this is relevant is we already know it has widespread use.

If Cardarine was marketed, it would require careful regulatory scrutiny. Therefore, in an open, unregulated illicit market, cardarine warrants a listing in the Poisons Standard.
More circular logic.

Cardarine has been identified as a substance of abuse with potential carcinogenic effects, and should be considered for a Schedule 9 entry.
More padding.

So basically we have to ban it because we can’t legalise and regulate it because it is banned or something like that. It’s interesting that they don’t comment on health issues raised by the product other than a possible carcinogenic link, a product widely used for such horrible reasons as improved sporting performance (which really means better quality of living) and aesthetics (improved mental health).

What Is Cardarine GW-501516?

Cardarine is a chemical drug developed in the 1990s that works as a peroxisome proliferator-activated receptor (PPAR) agonist. Originally designed to treat metabolic and cardiovascular diseases it was never brought through to medical use by GSK.

Many studies have been performed that have shown some significant benefits to the heart, skeletal muscles and the processing of fat. It’s the chemical binding to PPAR in muscle tissues that brings about these benefits.

 

How Does Cardarine Work?

Once Cardarine binds with PPARs in the body it causes the release of a protein that boosts glucose processing in muscle tissues. This natural physiological reaction also results in a significant increase in the processing of body fat stored in muscles and under the skin.

Essentially the body produces more energy from blood sugars and fat that is then available to enhance performance and an increased muscle production.

 

>What Are The Benefits of GW-501516?

Numerous studies have been performed and are still ongoing about the benefits from Cardarine use. While the drug has not been further developed there are plenty of studies to base some conclusions on for what the physiological triggers and effects are.

Here are some of the main findings from studies that are listed below:

 

1 – Positive Cardio Vascular Effects

Studies have shown that the original idea for the drug has shown very positive effects on mitigating heart disease. One of the main noted effects was the reduction in atherosclerosis, which is the build-up of plaque in arteries (S 1).

 

2 –Helps Break Down Fat

Increased metabolic rates and the boosted performance of muscles has the effect of an increased energy production through proteins. Energy is sourced both from blood sugars and body fat resulting in a reduced BMI (S 3).

 

3 – Protects From Liver Damage

This is achieved by the liver switching to fatty acid processing and a reduction in glucose synthesis. It doesn’t reverse damage, but offers protection from damage (S 4).

 

4 – Helps Build Muscles

The PPARs that are bound are predominantly found in muscle tissues and the protein that is released causes increased glucose and fat processing in muscle fibres. The effect is a faster build-up of lean muscle mass (S 5, 6).

 

5 – No Increase In Testosterone

Unlike many other SARM and PPAR supplements, Cardarine doesn’t cause a boost in testosterone levels. This usually has significant side effects including mood swings, that are not present with this drug (S 7).

 

What Are The Side Effects of Cardarine GW501516?

Since its introduction in the 1990s, many countless clinical studies have been performed. The majority have shown very few, if any, negative effects. The drug was abandoned because very high doses in mice was showing increased cancer development.

However, as the above benefits show, other studies have found extremely positive effects in both humans and animals. At this stage it is unknown whether the drug will be further developed as other replacements have taken priority for the original developers (GSK).

Cited studies:

https://pubchem.ncbi.nlm.nih.gov/compound/317318-70-0#section=Top

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2602589/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4421799/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3519722/

https://www.ncbi.nlm.nih.gov/pubmed/25943561

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2706130/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2907129/

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