Cardarine – GW501516
Cardarine GW501516 was developed in the 1990s as a potential treatment for cardiovascular disease, obesity, and diabetes. However, it was discontinued in 2007 after it was linked to the rapid development of cancer during trials on mice.
It has since become popular among the weight-lifting community for boosting metabolism, enhancing fat loss, and increasing muscle growth.
Athletes considering Cardarine should be aware of its proponents and why it has been banned from sanctioned sports.
In this ultimate review we are going to outline everything you need to know about Cardarine in Australia.
What is Cardarine GW501516?
GW501516 also known as GW1516, GW501, GW516 belongs to a family of drugs that act on the peroxisome proliferator-activated receptor (PPAR agonist). Most commonly known as Cardarine or Endurobol, it is an oral, bioactive drug that interacts directly with cell tissues.
PPAR agonists were originally designed to help reduce triglycerides and blood sugar levels. Cardarine GW1516 was developed in a collaboration of GlaxoSmithKline and Ligand Pharmaceuticals. Ligand went on to develop LGD4033 (Ligandrol), an oral selective androgen receptor modulator (SARM) for treating muscle wasting and osteoporosis.
How does Cardarine work?
Although Cardarine has previously been referred to as a SARM (selective androgen receptor modulator), it is not. SARMs were first developed in the 1940s to mimic testosterone. They work by activating the androgen receptors in specific tissues such as bone and muscle, which causes an increase in muscle mass.
Cardarine, on the other hand, is a PPAR-delta activator, which means it doesn’t act directly on androgen receptors. PPARs are activated by polyunsaturated fatty acids and fibrates and are used to regulate the breakdown of fats and lipoprotein synthesis. They can also help to modulate inflammatory responses of the liver and other tissues, and are involved in the regulation of other cell types, including adipose cells.
PPARs main proponent of action is to bind to peroxisome proliferator-activated receptors, which allows it to change the function of the gene and how energy is produced. PPARDs work at the gene level and affect skeletal muscle metabolism.
Cardarine works by activating AMP-activated protein kinase, glucose uptake, and fatty acid oxidation in skeletal muscle. In this way, it can reverse metabolic abnormalities in obese and pre-diabetic individuals by stimulating fatty acid oxidation, burning fat, and increasing glucose uptake in skeletal muscle tissue, which changes the body’s metabolism to burn fat for energy instead of muscle or carbohydrates.
In other words, Cardarine forces skeletal muscle to use fat rather than carbohydrates as an energy source. It’s said to boost stamina, endurance, workout capacity, and fat loss within just days of usage, particularly for overweight or unfit athletes.
This has made it highly desirable for athletes seeking to enhance their endurance or to boost fat loss. Like other PPARs, Cardarine has a significant effect on endurance, allowing the user to push harder and longer without becoming fatigued. One laboratory study showed that PPARD activation appeared to nearly double the performance of running endurance in untrained adult mice.
While stimulants can cause a sharp spike in energy and a potential crash later on, Cardarine has the opposite effect: it allows the user to “rev up” their energy output without actually causing their heart rate to spike.
Also unlike SARMs, Cardarine has no influence on blood testosterone levels, so the side-effects of excessive testosterone levels caused by other drugs will not be experienced.
Unsurprisingly, PPARs are considered highly desirable for cardio activity such as running or boxing. They are also revered by bodybuilders and weight lifters who find they can work out for longer without becoming tired or experiencing muscle weakness.
Cardarine in the Media
Cardarine (Feb 2018 tga.gov.au)
Date: February 05, 2018
Cardarine began gaining popularity during the 2000s. It was after the 2008 Beijing Olympics that its wide usage was discovered and subsequently became a banned substance by almost all doping commissions. It was officially banned by the World Anti-Doping Agency in 2009.
Prior to the 2008 Olympics, Cardarine was not controlled by regulations or detected by standard tests. When concerns were raised that it was being used as an ergogenic performance-enhancing drug, a urine test was developed and made available to the International Olympic Committee. The World Anti-Doping Agency (WADA) developed a test for Cardarine and other related PPARδ modulators, and subsequently added all of these drugs to the prohibited list.
Cardarine continues to be endorsed by bodybuilders and other endurance athletes and is still promoted on supplement websites. In 2011 it was reported to cost $1000 for 10g. In 2012, WADA changed Cardarine’s categorization from a gene doping compound to a “hormone and metabolic modulator”.
In 2013, the World Anti-Doping Agency published an alert that Cardarine was being sold on the black market as an endurance booster and was being abused by athletes. At the time, the drug’s prevalence was uncertain, as were the specific health concerns of the substance that prompted the alert.
A number of athletes have tested positive for Cardarine over the last decade. Most recently, heavyweight boxer Jarrell “Big Baby” Miller was tested positive ahead of the WBA, IBF, and WBO heavyweight title at Madison Square Garden in June 2019. As a notoriously heavy boxer weighing in at a reported 315 pounds, Miller is in the largest weight class in boxing.
GW501516 Research Studies
GlaxoSmithKline undertook two phases I and one phase II clinical trials in developing Cardarine. Reports indicated that a Phase I clinical trial was terminated, but no reason is given. This trial was to determine the efficacy of the drug in treating patients with heart disease, as well as other potential markers of drug activity, including levels of lipids and proteins in participants’ blood.
In 2006, GSK stopped clinical development of GW501516 when long-term animal studies revealed that the drug caused toxicities, including a variety of cancers.
According to the Australian Therapeutic Goods Administration site, a phase IV clinical study was completed in Australia in 2008 to assess the application of GW5015156 in treating high blood cholesterol in insulin resistance and obesity. No adverse events were reported by the authors for the phase IV trials. The authors also cited two earlier clinical studies that showed no significant adverse effect of the drug, including liver or muscle responses in participants treated with GW501516.
Evidence of fat-burning
Cardarine was first developed as a fat-burner. As a PPAR-delta, it has been shown to activates a number of genes involved in burning fat and increasing energy use. A small study involving just 13 men with high abdominal fat and high LDL cholesterol levels were given 2.5 mg of Cardarine a day for six weeks. The results showed decreased triglycerides, fatty acids, and VLDL proteins.
Cardarine was also shown to increase HDL cholesterol in two studies involving 305 patients with low HDL. The participants who were given Cardarine also experienced reduced LDL, triglycerides, and apoB.
Another small study with 12 participants showed Cardarine increased HDL and increased the body’s use of fat as an energy source, boosting fat-burning.
While these studies suggest that Cardarine may be effective in supporting fat-burning mechanisms and reducing harmful blood cholesterol, the current scope of evidence is considered poor quality.
Evidence of reducing obesity
Cardarine may help to reduce symptoms of metabolic syndrome. A study involving six overweight volunteers showed a decrease in liver fat by 20%, while insulin levels were reduced by 11% The participants also experienced a reduction in blood lipids by around 23-30%, including (triglycerides by 30% and LDL by 23%.
A similar study involving obese monkeys showed that those treated with Cardarine had higher HDL cholesterol and lower triglycerides, insulin, and LDL cholesterol levels.
Evidence of supporting blood vessels
Studies in mice have shown Cardarine was able to prevent oxidative damage in blood vessels. It also appeared to reduce the risk of arterial plaque by boosting levels of nitric oxide, which protects and relaxes the blood vessels.
Yet another study involving mice showed that low doses of PPARs can reduce tissue damage and inflammation in the mice’s arteries. Researchers suggested that this could help reduce the risk of heart disease and other cardiovascular complications.
GW1516 Anecdotal Evidence
There are many anecdotal accounts of Cardarine’s benefits, particularly among the bodybuilding community.
One user of GW1516 in Australia says that it will very quickly “boost your stamina to an unbelievable level” and that you will be able to work out “for very long durations which will ultimately improve your cardiovascular health”. He also claims that this will “burn your fat faster than ever and you will start coming back to your original shape in absolutely no time.”
Other reports describe Cardarine as a ‘miracle cure’ for obesity because it could cause the body to burn fat directly, while others claim that their usual cardio sessions feel much easier and they are able to significantly increase the pace without getting tired.
Some suppliers of Cardarine in Australian say that bodybuilders and athletes described it as “the ultimate endurance enhancement.”
Sarms Reviewer #6 says :
around week 7 I saw my abs for the first time all while never losing any weight on my major lifts….Cardarine also boosted my cardio sessions which made them easier to complete and less time consuming.
Is Cardarine Legal in Australia?
Although the Australian Therapeutic Goods Administration states that Cardarine is not approved for human use, the substance is still legal to purchase in Australia.
In June 2018 the Therapeutic Goods Administration (TGA) included GW1516 in the Poisons Standard under Schedule 10. This schedule is reserved for substances of such danger to health as to warrant the prohibition of sale, supply, and use.
However, it should be noted that the lack of regulation allows suppliers to advertise Cardarine freely and make unproven assertions about its efficacy and safety. It is able to be administered without reliable advice on appropriate dosage, frequency of administration, and exact content.
At present, Cardarine and similar products are widely promoted as a “cutting-edge alternative” to steroids on bodybuilding forums and black-market sites.
Users are warned that they risk health complications and adverse effects as well as a positive drug test.
Cardarine Dosage & How to Use?
According to most users’ reports found online, the most effective cardarine GW501516 dosage is between 10 to 20mg per day. One should take full dosage one to two hours before exercising.
Other suppliers recommend starting with 10 mg Cardarine/Endurobol per day to boost endurance, while higher dosages promote greater fat loss.
Cardarine’s half-life is about 24 hours, so a single intake daily is usually sufficient. Those who wish to split the dose can take one morning and one evening. Cardarine is best taken 45 minutes to 1 hour before training. In most cases, a cycle will last from around 4 to 8 weeks, and the maximum application cycle is 12-14 weeks.
NOTE: Suppliers warn that taking Cardarine is at their own risk and that users should consult with their healthcare professional first. The recommended daily dose should not be exceeded, and users should be healthy adults over the age of 18 years.