Wednesday 26 February 2014

CJC-1295 and sports doping – an update


This was one of the peptides used by some Australian sports players (see my previous blog Australians doping with designer peptides: do they work as sports drugs?) and also this article. As I explained in my blog it is designed to be a growth hormone releasing compound, enhancing the natural production of the hormone. Hence the interest as an agent that could theoretically increase muscle mass.

But why were these kind of compounds developed in the first place when human growth hormone (and human growth hormone releasing factor or GHRH) are themselves easy to obtain? As is usual the economic driver is medicine not sports performance.

CJC-1295 was made by a Canadian biotechnology company called ConjuChem (hence the acronym CJC). It was engineered to be longer lasting in the bloodstream, making it more effective than authentic GHRH. GHRH is a peptide (or small protein). We learn in school biology that proteins cannot be absorbed in the diet in their native state and so have to be broken down into smaller parts (peptides and then amino acids) by enzymes. That is why you need to inject a peptide drug, rather than swallow a pill, if you want it to have any effect in the body. However, enzymes that can digest peptides are not restricted to the gut. There are some in the blood and these naturally break down GHRH. So injected GHRH does not last long in the body. CJC-1295 is a form of GHRH, modified so it can bind to serum albumin – a very abundant protein in the plasma. Here it “hides” from the enzymes that are trying to degrade it. This makes CJC-1295 a potentially more effective drug than GHRH in treating growth hormone efficiency.

The modifcations that have been engineerd into CJC-1295 are a bit of a double edged sword for dopers. So, yes the drug could be more effective, but it is also easier to test for because it is: (a) completely artificial so cannot be confused with a “natural” version already in the body; (b) lasts longer in the blood stream so there is a longer “window of opportunity” for testers to act. In 2010 a US group gave 0 CJC-1295 to healthy individuals to try and develop an indirect test as part of a biological passport [1]; in 2010 the Norwegian anti doping lab was able to detect it in a formulation used by bodybuilders [2].  

So what became of ConjuChem and did they make their millions from CJC-1295? Sadly for their investors the answer is no. CJC-1295 never did make it as a clinical product. ConjuChem ran out of money in 2010. All is not lost for the CJC name however. Its assets were bought by US investors, and it moved from Montreal to warmer climes in Los Angeles. Its main product is now CJC-1134-PC, a molecule designed to enhance insulin action in Type II diabetes. Again it hides from destruction by binding to albumin. Although some athletes dope with insulin, a quick trawl of the Internet revealed no one seems to be selling this particular peptide on the black market. Give it time I guess ....


[1]        Henninge, J., Pepaj, M., Hullstein, I., and Hemmersbach, P. (2010) Identification of CJC-1295, a growth-hormone-releasing peptide, in an unknown pharmaceutical preparation. Drug testing and analysis 2, 647-650.

[2[        Sackmann-Sala, L., Ding, J., Frohman, L. A., and Kopchick, J. J. (2009) Activation of the GH/IGF-1 axis by CJC-1295, a long-acting GHRH analog, results in serum protein profile changes in normal adult subjects. Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society 19, 471-477.

2 comments:

  1. As someone who competes in athletics, it's discouraging to read about all of these new drugs. Hopefully with the long half life, it can be detectable in urine for a long time. Has WADA developed a urine test for this or the other GH peptides yet?

    ReplyDelete
  2. There is a blood test for growth hormone. The urine test would probably be included as part of some from of "hormone biological passport" but this is not available yet. I know of no validated test for CJC-1295, but I am sure it is being looked at. Like all such compounds, the utility of a direct detection test depends on how long it lasts in the circulation. However, as it is an artificial compound the detection limit could be set very low i.e. anything in the blood would be considered doping, whereas,for GH you also need to conform that it is from an unnatural source.

    ReplyDelete