Australia is no stranger to sporting scandals. Cricket’s “John the bookmaker” affair, horse racing’s “Fine Cotton” scandal and any number of player salary cap breaches (to name but a few).  However, 2013 has marked what is perhaps the biggest scandal in Australia’s sporting history – the use of peptides in Australia’s biggest sporting code, Australian Rules Football (AFL).  In this post, we take a look at the patent behind the peptides.

Over the last few months, it has been widely reported that Essendon Football club players were prescribed the anti-obesity drug AOD-9604 in the 2012 AFL season.  This drug is the subject of an Australian patent. Below, we take a look at the patent behind the drug that has become a high profile exotic peptide, but first a history lesson:

The Essendon Bombers

For those readers not familiar with the AFL, it is the most widely followed Australian sporting code.  The Essendon football club is a founding member of the AFL and the club was formed sometime between 1871 and 1873.

Those all too familiar with the “Dons” (as they are also known) would be aware of the 16 premiership titles and/or the premiership drought persisting since 2000.

At the time of writing (14 May 2013), Essendon are currently in second position on the AFL ladder.

So, what exactly is AOD-9604?

AOD-9604 is a small peptide derived from the fat metabolizing region of human growth hormone (hGH). For science trainspotters like us, it is a 15 amino acid region (amino acids 177-191 of hGH) to which a tyrosine was added to help make the molecule as stable as Gary Moorcroft’s mark of the century off Brad Johnsons shoulders:

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AOD-9604 was invented around 1997 in the laboratory of Professor Frank Ng, a biochemist at Monash University who had been studying human growth hormone since the 1960s. In vitro and in vivo tests on AOD-9604 showed that the drug retained all of the fat metabolic properties of growth hormone, without any of the hormone’s undesirable effects.  A patent application for AOD-9604 was filed in 1997:

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A patent was subsequently granted in 2003 and includes a claim to the peptide itself:

  1. A peptide which comprises an analogue of the carboxyl-terminal sequence of a growth hormone, said analogue comprising the amino acid sequence Tyr-Leu-Arg-lle-Val-Gln-Cys-Arg-Ser-Val-Glu-Gly-Ser-Cys-Gly-Phe, or an organic or inorganic acid addition salt thereof.

AOD-9604 was initially intended as a potential treatment for obesity. Australian company Metabolic Pharmaceuticals (the patentee of the above patent), had previously conducted six human clinical studies involving 925 patients. While the trials proved that AOD-9604 was profoundly safe, they did not show a clinically meaningful weight loss outcome across the total trial population. As a result, the obesity program was terminated in February 2007.

More recently, Metabolic Pharmaceuticals demonstrated AOD-9604 may have potential to be used as a treatment for the repair of cartilage, muscle and joint disorders such as Osteoarthritis.  In April of this year, Adelaide University Chair of Medicine Professor Gary Wittert said there was no clinical evidence that it helped with tissue repair or had any other benefit in people. “However, when we gave it intravenously, we noticed that 60 per cent of people felt a euphoric effect, so (the company) and I patented it as an anti-depressant.”.

AOD-9604 & Anti Doping in Sport

AOD-9604 has been classified a prohibited substance by the World Anti-Doping Authority (WADA). It has been alleged that AOD-9604 was injected into AFL and National Rugby League (NRL) players by sports scientist Steven Dank.  Mr Dank told the media in April that he used AOD-9604 on Essendon players in the 2012 season during the club’s controversial supplements program.

In a statement dated 22 April 2013, WADA advised that AOD-9604 falls into the S0 – Non-approved substances category of the 2013 Prohibited Substances and Methods Lists.

AOD-9604 has not been granted approval by Australia’s Therapeutic Goods Administration or any other government health authority in the world to be marketed as a pharmaceutical product in Australia.

AOD-9604 & Cellulite?

As well as providing a euphoric effect, it turns out that AOD-9604 is a key component of an anti-cellulite cream.  So for those who are interested in the euphoric effect or just to do WHATEVER IT TAKES (Essendon’s unfortunate and ill-timed 2013 season tagline) to get rid of cellulite, Australian company Phosphagenics “Elixia BodyShaper Cellulite Contour Crème” is available online.