[2] In 2007, research was published showing that high doses of GW501516 given to mice dramatically improved their physical performance; the work was widely discussed in popular media, and led to a black market for the drug candidate and to its abuse by athletes as a doping agent.

The World Anti-Doping Agency (WADA) developed a test for GW501516 and other related chemicals and added them to the prohibited list in 2009; it has issued additional warnings to athletes that GW501516 is not safe.

[15] The work was published in 2007 in Cell and was widely reported in the popular press including The New York Times and The Wall Street Journal.

[17] Concerns were raised prior to the 2008 Beijing Olympics that GW501516 could be used by athletes as a performance-enhancing drug that was not currently controlled by regulations or detected by standard tests.

One of the main researchers from the study on enhanced endurance consequently developed a urine test to detect the drug, and made it available to the International Olympic Committee.

[32] In July 2022, the 2012 800 m Olympic silver medalist from Botswana, Nijel Amos tested positive for GW501516 and was provisionally suspended just days before the 2022 World Athletics Championships.

[33] Surinam's Issam Asinga, who set the under-20 world track record in the men's 100 meters, was informed on Aug. 9, 2023 by the Athletics Integrity Unit that his July 18 drug test the prior month detected trace amounts of GW501516.

[36] Furthermore, in rats treated with GW501516, increased fatty acid metabolism in skeletal muscle and protection against diet-induced obesity and type II diabetes was observed.