AICAR – the get fit without exercise drug

Part three of the new doping mini series – this time AICAR.

A drug to help lose weight, gain muscle and get fit even without exercise?  This week I will take a look at AICAR…

AICAR – full name  aminoimidazole carboxamide riboside (also with the drug name acadesine) is a drug under development and in clinical trials for various treatments.  The drug is a target for use in various metabolic disorders, obesity and possibly for use in heart operations to prevent damage to tissues.  During animal testing AICAR was evaluated for effects on endurance in mice.  The results showed an improvement of up to 44% in treadmill tests after 4 weeks using the drug without training!  Another study looked at whether GW1516 and AICAR combined was as effective at getting fit compared with GW1516 plus exercise.  The effects were very similar.  This means that gains can be made in fitness using GW1516 and AICAR without training!  This was dubbed ‘exercise in a bottle’ in the media a few years ago. The conclusion is that AICAR makes the body think it has exercised.  This trick is classed as ‘gene doping’ by WADA and AICAR is prohibited in all sports at all times.  This was added to the prohibited list in 2009.

In 2009 the British Medical Journal reported that anti doping authorities in France had analysed contents of cyclists bins and found evidence of the use of AICAR, even though unlicensed (along with another unlicensed product and new variants of EPO).   The head of the French testing authority said he was convinced it was being used.  I have looked on the internet and as with SARMS and GW1516 there are sites that offer it for sale in the UK, but I haven’t tried to order any.

Although there are tests available for AICAR in urine samples – published several years ago – it appears that no athletes have yet been caught using the drug.  The method may not be in routine use as yet due to various difficulties in interpretation.  The drug is naturally present in urine, excreted by the kidneys, even if you have not used the drug.  A paper by Thevis et al (An and Bioan Chem, 2010) looked at the levels found in elite sports persons and suggested a threshold value.  There are various difficulties with this approach such as: the need to have a statistically significant sample for baseline evaluation; to ensure that there are not people who are naturally going to have very high levels (and be tested ‘positive’); to determine whether any illness or disease would increase the urinary excretion; to ensure those using the drug will be tested positive; and hopefully develop a second confirmatory method.  A perfect candidate for this method would be isotope ratio mass spectrometry, which allows differentiation of naturally occurring compounds and pharmaceutical preparations and is currently used to detect testosterone administration.

Long term the effects are not clear, as with GW1516 and SARMS these have not been around long.  For a professional athlete the benefits are clear – improvements in endurance and other fitness measures without increased training.  The ‘coach potato’ may see this as an advantage also.  Exercise does however have a much more beneficial effect on many body organs though.

Thanks for reading – I have one more post on gene doping that will be up next week.  I’ll keep an eye out for other interesting  forensic science stories in the meantime.