Around this time of year there starts to be a rush of articles in magazines and newspaper supplements on ‘getting skinny for summer’ – this one is a tip that wont appear on those articles – the experimental drug GW1516. This experimental compound now appears to be the drug of choice for cyclists with several positive tests in the past few days.
The background
In 2009 the World Anti Doping Agency (WADA) placed the compound GW1516 (also known as GW501516) on the list of compounds prohibited for use in sport. The compound was developed by GlaxoSmithKline (GSK) for use as a peroxisome-proliferator-activated receptor (PPAR)-delta agonist. In lay terms PPAR agonists are compounds that have potential for use in treatment of cardiovascular and metabolism disorders. For example one compound is being investigated to raise the HDL (‘good cholesterol’) and lower clogging of arteries. For sports people the main advantage is helping the body burn more fat, thereby getting the athlete very lean, whilst potentially increasing muscular strength. There were rumours around the use of these substances a few years ago when several cyclists were extremely thin without having lost the muscles required to climb hills quickly. The use of GW1516 with another banned compound AICAR is reported widely in sports circles as being particularly good at promoting fat loss whilst giving endurance gains. That sounds perfect for endurance cyclists (and to be fair other endurance sports such as athletics or cross country skiing). The potential for abuse of this was mentioned in a New Scientist article in 2004, whilst the drug was still under investigation by GSK. The report mentioned that the pill could provide all of the positive muscular effects of exercise without having to get sweaty!
So far so good – but here is the catch. The trials of GW1516 by GSK were stopped. According to their own data (found in abstract 895) the use of GW501516 was seen to promote many different cancer types in various rats cells. The compound was not developed further for human use. Even so, you can buy Gw1516 on the internet. A quick search found various sources of the ‘research chemical’ at costs a professional sports person should be able to afford. AICAR was also readily available. Both are marked as ‘not for human consumption’.
Test methods
The published method for testing urine sample for the metabolites of compound GW1516 uses LC-MS. The metabolites are as the compound to the right but oxygenated on the central sulphur (S) (either one or two O atoms bonded to the S). The method published by Thevis et al (Anal Bioanal Chem (2010) 396:2479–2491) described the use of LC-MS following enzymic hydrolysis, a method routinely available to the anti doping labs. The paper suggested that there was a likely four day window of detection of the drug after it had last been used. This is a very good detection window as several drugs of abuse are only detectable for hours after their last use.
Positive tests
Last week it was announced that a Russian cyclist Valerie Kaykov had failed a test for the compound GW1516 – the first time this has been reported. This was days after WADA had warned athletes of the dangers of using GW1516. The report mentions the metabolite GW1516 sulfone – this is where the body has added two oxygen atoms to the S atom in the middle (both with double bonds). Also this week the world cycling governing body UCI announced that four Costa Rican cyclists had tested positive in an event in December (three from the same team). So has the introduction of the test for this caught out the athletes in question? Most probably. This is seen from time to time when a new test is introduced (eg in 2008 several cyclist failed tests for CERA).
There have been several studies over the years that have shown that elite athletes are prepared to gamble with their health by using drugs if they have an increased chance of winning. This compound does seem to be a huge gamble on their future health. Obviously I hope that nothing ill comes of any of them but they have taken a big risk. Cycling is also once again dragged into doping stories which it really needed to avoid in the after mark of the Armstrong and the ongoing Puerto cases. Let’s hope the rest of the season is quiet and we can see some great victories from true champions!
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