Understanding GW-501516

One of the most controversial substances that hit the pharmaceutical world is gw-501516. In 1992, research collaboration was initiated between GlaxoSmithKline (GSK) and Ligand Pharmaceuticals to discover the truth regarding the claims being associated with this substance.

Gw-501516 is a Peroxisome proliferator-activated receptors-delta or PPARDs receptor agonists.

GW-501516An agonist in simpler terms is a substance that can cause a physiological response to a certain muscle or tissue of the body. In this case, Gw-501516 is said to have the ability to activate the same responses of the muscles as when one exercises. Imagine drinking a drug with a mechanism of action similar to that of exercising? It would certainly be the dream drug of all weight watchers and dieters all over the world. One can eat and not exercise and still have the equivalent results of exercise. Not only that, problems on obesity and other health-related medical conditions of obesity would be remedied.

Another claim is the increase in production of the genes responsible for endurance of the muscles. Therefore, if this claim is true, a person can have an enhanced capacity to endure muscle activities and would be able to perform better than usual. In their experiment, GW-501516 was introduced into the embryos of the lab mice. The untrained mice were able to double their running endurance. This claim, of course, attracted the athletes.

Lastly, this substance was found to have the capability to modify the expressions of proteins specifically involved in energy expenditure. What is the significance of this? The mode of action would result to increased fatty metabolism in skeletal muscle plus increase in high density lipoprotein HDL (the good cholesterol) while it lowers the low density lipoprotein, LDL (the bad cholesterol). Simply put, this substance can be a breakthrough to put a stop to cholesterol-related problems such as heart attack, stroke and type 2 diabetes, among other things.

It was not a surprise that high hopes were raised with the emergence of this substance. However, the results in the experiments revealed that the mice developed numerous tumors when large doses of GW-501516 were given. GSK immediately halted the clinical testing and altogether abandoned the researches being made.

Nevertheless, this event did not stop other people in using the substance to enhance their physical functions, especially the athletes. Having the foresight that something like this would occur, the World Anti-Doping Agency (WADA) therefore included it as one of the prohibited drugs to be used in its list. Formerly, there was no standard test that can detect the presence of this substance in the body but later on, a urine test was approved to determine its presence. It was submitted to the International Olympic Committee and was used during the screening of athletes.

Some of the athletes who were tested positive of this drug were the four riders from Costa Rica last December 2012. Three of them were given a two-year suspension. The fourth rider received a 12-year suspension as it was recorded that it was his second doping violation already. Russian cyclist Valery Kaykov was likewise suspended after a positive result of the drug was revealed. The latest addition to the list is Venezuelan Miguel Ubeto.

Up to the present, the trading of this banned drug cannot be totally stopped as it could be purchased legally for biochemical studies and researches. The fact remained though. There was never any approval of this substance for human consumption by any research or study. No firm or government establishment has given the go signal to use this product for whatever purpose by humans. One has to take full responsibility for any untoward event that may happen due to its use.