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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IGF-1 gets no respect

Monday, January 13, 2014

In describing Alex Rodriguez and the use of performance enhancing drugs, presumptive may be appropriately used, since as has been thoroughly noted by him and his spokespersons, he has never failed a drug test. Lance Armstrong also did not fail drug tests for PEDs but presumptive was removed from his status when he confessed to their use.

For Mr. Rodriguez, the battle continues but the specific types of drugs allegedly used are now public, after the Biogenesis files were made available in lawsuit documents. The culprits were testosterone, insulin growth factor 1 (IGF-1) and human growth hormone (HGH), the triumvirate of drugs that can be legally prescribed by a physician to treat a range of medical conditions. They may also be legally prescribed off-label to be used as the patient and physician see fit. The issue for Mr. Rodriguez is that these medications were neither prescribed by a physician nor allowed by his employer. While it is not illegal to have the substances in his body (though not proved by testing), Major League Baseball and its players union have agreed that performance enhancing drugs do not belong on the field of play.

The world has heard about HGH and testosterone, but IGF-1 is a silent partner in performance enhancement. The pituitary gland in the brain produces HGH and released into the blood stream, where it activates the liver to produce IGF-1. It is chemically similar to insulin but has a specific cell receptor that helps promote growth in almost all cells in the body, including muscle and cartilage. People need adequate levels of both HGH and IGF-1 to grow properly; lacking either chemical may be the cause of syndromes associated with short stature. IGF-1 levels in the body peak just after puberty allowing for the teenage growth spurt and fall off with age. HGH is useless unless the liver can produce the active ingredient IGF-1.

IGF-1 is responsible for cell growth and its presence decreases cell aging and death, which is a wonderful thing for growing healthy young people but may cause problems with cells that should die but do not. IGF-1 increases the growth of cancer cells and those who are deficient have a lower rate of cancer.

Pharmaceutical companies had high hopes for IGF-1 to help treat diabetes (it is closely related chemically to insulin), short stature like dwarfism and because of its cell growth properties, burns, Alzheimer’s disease and Lou Gehrig’s disease (ALS). Unfortunately, research results are mixed and potential side effects are real. There is no indication to treat New York Yankee third basemen.

The law allows Mr. Rodriguez to use performance enhancing medications as prescribed by a physician. Sports organizations worldwide ban their use to help maintain a level playing field and prevent one athlete from obtaining an unfair advantage over another and to prevent potentially lethal side effects. The ban of PEDs also prevents the creep of their use in younger athletes. If PEDs are required to succeed in the pros, then college athletes will use them; high school athletes will then begin abusing the drugs in their hope of getting college scholarships; middle school kids will use drugs to make high school varsity.

Lance Armstrong proved that his chemist was better than those employed by organized sport and he was able to beat the testing process. Alex Rodriguez remains an alleged used of PEDs because he too, has yet to test positive. Perhaps the time has come for pro sports to start drafting PhDs in chemistry.

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