GW-501516 was studied as a drug by GlaxoSmithKline. It is a Peroxisome proliferator-activated receptor delta (PPARδ) receptor antagonist and was found to cause cancer in rats. Since then, further development was stopped by GlaxoSmithKline. It was seen as a possible cure to for cardiovascular disease, obesity, dyslipidemia, and diabetes. It was found out to have a synergistic effect when combined with AICAR, or AICA ribonucleutide; in animal studies, the resulting combination was shown as having an interesting effect – it remarkably increases exercise endurance.
GW-501516 was first discovered in a collaborative research between Ligand Pharmaceuticals and GSK which kicked off in 1992. The first phase of trials, in 2000, was for the treatment of hyperlidimia. It was followed by phase I/II in 2002. Ligand Pharmaceuticals earned $1 million payment because GSK wanted to continue development of the compound. GSK had done two phase II clinical studies before ceasing development in 2007.
The Peroxisome proliferator-activated receptors present in GW-501516 are said to have an effect on nuclear hormone receptors linked to glucose and lipid metabolism. It works at the gene level and impacts the metabolism of the muscle. Based on this, GW-501516 is not in the same category with restricted drugs that is akin to steroids because of the way the drug works in the body.
Tests involving GW-501516 was first conducted on mice. This resulted in increased muscle mass, decreased fat mass build-up, and increased glucose tolerance. Later on, more studies were done that demonstrated that there was a potential of developing a kind of tumor. There were three initial studies done by GSK on GW-501516 – two phase ones and a single phase two. The first phase I trial was brought to an end for reasons not explicitly stated. The second phase I trial was completed, as well as the phase II trial. In Australia, the use of GW-501516 was assessed in the treatment of high blood cholesterol; this was marked as the fourth phase.
A lot of people buy GW-501516, but the World Anti-Doping Agency, or WADA, has been warning them against the purchase of such drugs. WADA has been the leader in the charge opposing GW-501516 and put out an advisory in March 2013 highlighting the probable health risks that can be caused by GW-501516. This was more aimed towards those who buy GW-501516 in the black market. The advisory also sought to serve as an eye-opener to the athletes who buy and use GW-501516 as an endurance booster. Since 2009, WADA’s prohibited drug list has had peroxisome proliferator-activated receptors on it. PPARs have also been prohibited from in and out of competition by the Australian Sports Anti-Doping Authority.
WADA was not the only one taking action against GW-501516; the NCAA has also thrown itself into the mix and has stated that it would work together with the Committee on Competitive Safeguards and Medical Aspects of Sport to discern where the drug falls on their banned substances list. These organizations know for sure that GW-501516 is not easily obtained, meaning that the black market is the only place where they can be purchased and that the drug will be in short supply sooner or later. They also hope that that the increased price for the drug would discourage people that buy GW-501516.
In spite of the fact that governing bodies such as WADA and NCAA have issued warnings regarding GW-501516 and the still unclear possible health risks that may exist, there are still some who continue to buy GW-501516. It is no secret that there has been a history of illegal drugs and performance enhancing drugs on the black market and GW-501516 is up there. The question is though, should the substance really be treated with such negativity despite having proven benefits and unconfirmed downsides?