GW1516/GW501516

GW501516 (also known as GW-501,516, GW1516, GSK-516 and Endurobol) is a PPAR-delta receptor agonist that was previously investigated for drug use by GlaxoSmithKline. The drug was discovered to cause cancer in rats and GlaxoSmithKline has ceased development. It activates the same pathways activated through exercise, including PPARδ and AMP-activated protein kinase. It had been investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. GW501516 has a synergistic effect when combined with AICAR: the combination has been shown to significantly increase exercise endurance in animal studies more than either compound alone. In March 2013 WADA issued an alert for GW501516. The agency had then learned that athletes had been using GW501516. Below is the warning from WADA: It has come to WADA’s attention that the black market substance GW501516 is being sold to and used by some athletes. The side effect of this chemical compound is so serious that WADA is taking the rare step of warning \"cheats\" to ensure that there is complete awareness of the possible health risks to athletes who succumb to the temptation of using GW501516 for performance enhancement. GW501516 was a developmental drug that was withdrawn from research by the pharmaceutical company and terminated when serious toxicities were discovered in pre-clinical studies. Clinical approval has not, and will not be given for this substance. However, GW501516 has been available for some months on the black market, through the Internet and elsewhere. Anti-Doping authorities have already seen its use by athletes, as there are a number of positive cases. (Sources: Wikipedia, World Anti-Doping Agency)