sarm, the new ped

Sunday, March 26, 2017

There has been an ongoing arms race in the chemistry world that pits athletes who dope and against the lab techs who test their urine samples looking for that illegal performance enhancing drug. The battle rages fiercely in the background, while the general public has become blasé about it, almost accepting the fact that many pro athletes use PEDs and when another star is suspended, the fallout is muted. The latest to do the perp walk is Joakim Noah who was suspended for 20 games, a quarter of an NBA season.

The drug in question for Noah was a selective androgen receptor modulator (SARM), LGD-4033, a substance that has been banned by the World Anti-Doping Agency since 2008. It’s an interesting drug because, while it can be easily available on the internet as a supplement (labelled not for human use), there is a good chance that perhaps this drug may actually have a significant positive use in the future. LGD-4033, tentatively named Ligandrol, was discovered by Ligand Pharmaceuticals and is now undergoing human testing by Viking therapeutics.

This class of drug, selective androgen receptor modular, are non-steroidal anti-inflammatories that are supposed to act like anabolic steroids, building up muscle and decreasing fat, but without the side effects that occur when the androgen receptors are also affected. The goal is to affect muscle and bone while leaving androgen levels (like testosterone) at normal levels. Testosterone is responsible for male sex characteristics and too much hormone may lead to high blood pressure, diabetes, acne, increased hairiness, liver disease, aggressive behavior and more. The anabolic to androgen effect ration of testosterone is 1 to 1, but some SARMs have ratios as high as 90 to 1, meaning if the correct dose can be found, the benefits would well outweigh the side effects.

The key is to get the dosing right. If the drug can be used to build muscle and prevent osteoporosis. The studies are ongoing at the present time. Phase 1 trials in 2012 in more than 70 adult males found that lean body mass could be increased and the more of the drug used, the better the outcome. Phase 2 studies began in November 2016, looking at 120 patients who were recovering from hip surgery to find out whether body mass could be maintained in people who were going to be increasingly sedentary as they recovered from surgery. This is the phase that also begins to look at side effects, safety and how the drug is metabolized (pharmacokinetics). If the drug still looks promising, then it’s off to phase 3, where thousands of patients will get the drug and their results, including side effects and complications, will be compared to a similar large group of patients who will be given placebo drugs as a control group.

For Joakim Noah, he was caught by chemists who tested his urine and found a drug that is not yet available for human consumption. For Noah, choosing this PED might have let him slip under the radar of the testing lab. The risk that was his downfall is that the characteristics of the drug in the human body aren’t yet well known. How long does it take for the body to metabolize and get rid of it? Does it interact with other medicines? Is it affected by other foods or how it’s stored? Lots of questions that will need to be answered before it is approved for human use.

The bottom line is that Noah cheated. For whatever reason, whether it was to recover from an injury or to try to escape the inevitability of age on his performance, he cheated. His inability to perform legally on the basketball court affected not only him, but also every other player on the court. Charles Barkley, Basketball Hall of Famer, said:” I’m not a role model… Just because I dunk a basketball doesn’t mean I should raise your kids.” Barkley may have been right when he talked about parenting, but was absolutely wrong with respect to PEDs. High school and college players look at Joachim Noah and wonder if they can make it to the big leagues without also having to use a performance enhancing drug. How many will choose to live better by chemistry instead of by spending hours in the gym? May be Noah can think of an answer while he serves his suspension.


Photo attribution: Getty Images

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the why of performance enhancing drugs

Monday, December 12, 2016

Every week seems to bring another player suspension by the NFL for the use of performance enhancing drugs. The frequency numbs us to the issue and unfairly, we may even suspect players who are clean and free of abuse. For that reason, the depth and breadth of the Russian doping allegations, should make us stand up and wonder what’s wrong with the state of sport. The report from the World Anti-Doping Agency provided evidence of more than a thousand international athletes who benefitted from illegal drugs or tainted testing processes as part of a governmentally run and approved program to have athletes cheat to reach the podium.

Depending upon the sport and the goal, there are a couple basic goals for doping. Anabolic steroids and human growth hormone (HGH) may allow the athlete to train harder recover more quickly, leading to muscle cell hypertrophy and increased strength. Blood doping, either by using erythropoietin (EPO) or by blood transfusion, allows increased oxygen deliver to the body prolonging the ability for muscles to work aerobically.

There is a cat and mouse chemistry battle between the athlete who dopes and the regulatory agencies that try to keep sports clean. The BALCO controversy revealed that anabolic steroid use can be successfully masked from testing but the 2002 Salt Lake Olympic testers were able to uncover the use of darbypoietin, a long acting EPO that had just been released on the market. Presumably, the athlete’s chemist may have a little time advantage initially, but the monitoring agencies catch up quickly. The question though, is why would an individual athlete want to cheat? It’s all about work ethic and philosophy.

Consider this one way of grouping athletes:

  • Group one has innate talent and work hard to maximize their potential
  • Group two does not have elite talent but does work hard to maximize potential
  • Group three has innate talent but lacks the motivation to work
  • Group four has neither talent nor motivation.

Group one athletes will generally succeed but should injury occur, fear of not returning to pre-injury levels might allow a pharmaceutical option to be a tempting proposition. Group three athletes might consider using drugs to substitute for work in the weight room to improve their performance the field.

The use of performance enhancing drugs might allow an athlete to leapfrog from one group to another. The rewards can be impressive and may mean the difference between playing varsity in high school as a showcase for getting a college scholarship. It may allow the college athlete to make a pro roster or an athlete to move from the B team to the Olympic squad. For a country to develop a system wide approach to performance enhancing drug abuse, it seems to make competition on the playing field a proxy for conflict on the battlefield. Based on the WADA report, the Russians were determined to assault the Olympic podium.

Interestingly, there are ways to artificially enhance performance that are quite legal. What is acceptable and what is cheating usually has to do with safety. Imagine a baseball player who can improve his vision by LASIK surgery to 20/15 and can then see the ball that much better than with glasses. Fans would cheer his dedication to his sport to undergo surgery to improve performance.

It gets complicated though. That same thinking to get LASIK surgery would be acceptable for an archer or a trap shooter.  If those two athletes would use a beta blocker, a common medication that blocks the effects of adrenaline in the body, slowing the heart rate and perhaps steadying a shaky hand, it would be considered doping. However, if that athlete had high blood pressure (hypertension) and was prescribed the beta blocker, a medical waiver might be issued.

It’s all about trust. Each competitor trains hard and hopes that their best is better than their opponent and as long as the playing field is level, may the better player win. It’s nice in theory but only works when everybody plays fair. One might argue that we should allow athletes to compete better by chemistry. The “only” downside are the complications of that chemistry, including but not limited to issues like cancer, stroke and death.

The next column talks about blood doping. Stay tuned.



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