GW1516 works by activating PPAR and by stimulating AMP-activated protein kinase. Activation of PPAR and AMP-activated protein kinase leads to a significant increase in endurance and faster oxidation or melting of fat respectively. It is also known as GW-501516 and GSK-516. Unlike ordinary workouts alone and usage of other catabolic drugs, usage of this substance does not promote loss of muscle mass. When AMP-activated protein kinase is stimulated, the energy needed for workout is drawn from the oxidation of fat rather than the loss of muscle protein and carbohydrates. Upon activation of PPAR, the skeletal muscle metabolism is enhanced, thus increasing endurance. In one experiment conducted, mice that have been treated with the said drug had a low fat accumulation despite being fed with a high-fat diet.
This drug was especially tailored by GlaxoSmithKline to address the widespread obesity. However, due to the negative findings of independent clinical studies that lead to the discovery of GW501516 as a causative substance for various organ tumors and cancers among controlled groups of mice, GlaxoSmithKline has stopped its production. The company also does not authorize the sale of the drug.
Test Phases with the Drug
GW-501516 has undergone phase I, II and IV tests under GlaxoSmithKline. Under the phase I study, scientists determined the effects of the drug to patients with heart problems. Phase I studies have been terminated and phase II and IV were classified as incomplete.
What is AICAR?
GW-5156 is often used with AICAR. Unlike the former drug, AICAR has been tested since 1980’s. It stimulates AMP-activated protein kinase activities. AICAR also belongs to WADA’s list of banned substances.
People’s Opinions on the Ban
A lot of people are discrediting the findings on GW1516 issued by the Word Anti-Doping Agency (WADA) simply because they find WADA scientifically inaccurate. Previously, only registered performance enhancing drugs were banned but recently WADA has also banned substances on their clinical and pre-clinical trial stage. WADA has also banned clinical approval to the said drug. The exact statement of WADA indicates that the substance has been banned because “side effect of this compound is so serious…” WADA has then since issued no elaboration of the term “serious” nor has it conducted further clinical studies to test, verify and report effects of the substance. Another independent study has shown that large dosage of the injected drug has resulted to liver fibrosis in mice subjects. Users dismiss this study on the premise of the term “large dosage”; the analogy to humans seem unclear because the administration of the drug is different from its administration among humans, which is oral, and that rodents have different metabolic functions than humans. Also, they claim that a little sacrifice for tangible results is normal with drugs. No registered drug in the market presents absolutely zero side effects.
In another study published in 2009, oral intake of GW-501516 at any dosage resulted in other forms of cancer. Male Han Wistar rats were “given 0, 5, 15 or 30 mg/kg/day for the first 6 weeks of the study. For the remainder of the study males were given 0, 5, 20 or 40 mg/kg/day.” Female rats were given 0, 3, 10 or 20 mg/kg/day for the entire study. The result after 104 days yielded various cancer in the liver, stomach, bladder, skin, thyroid, testes, ovaries and uterus. This seems like a very convincing study, but so far no recorded person has reported about acquiring cancer mainly due to this drug.
GW1516 is being sold as Endurobol in the black market and is detectable up to 40 days from the first dosage. The said drug is also available for sale from research chemical retailers meant for experiments and not for human use. Body builders start with a 5mg dosage spaced 12 hours twice a day.