GW501516
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| Formula | C21H18F3NO3S2 |
| Molar mass | 453.498 g/mol |
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GW501516 (also known as GW-501,516, GW1516, GSK-516 and on the black market as Endurobol) is a PPARδ receptor agonist that was invented in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s, was entered into clinical development as a drug candidate for metabolic diseases and cardiovascular diseases, and was abandoned in 2007 because animal testing showed that the drug caused cancer to develop rapidly in several organs.
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.
GW501516 was initially discovered during a research collaboration between GSK and Ligand Pharmaceuticals that began in 1992. The discovery of the compound was published in a 2001 issue of PNAS. Oliver et al. reported that they used "combinatorial chemistry and structure-based drug design" to develop it. One of the authors was the son of Leo Sternbach who discovered benzodiazepines in the 1960s.
R & D Focus Drug News reported that GSK began phase I trials of the compound for the treatment of hyperlipidemia in 2000 followed by phase I/II in 2002. In 2003, Ligand Pharmaceuticals earned a $1 million payment as a result of GSK continuing phase I development.
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