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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HGH… be like Ryan

Monday, July 29, 2013

“I’m not a role model. I’m paid to wreak havoc on the basketball court.”  Charles Barkley

“Charles…I don’t think it’s your decision to make. We don’t choose to be role models, we are chosen. Our only choice is whether to be a good role model or a bad one.”  Karl Malone

In 1993, a controversy arose when Mr. Barkley, now a television analyst declared that his job was to play basketball, not necessarily set an example for kids and others in his fan base. His comments came in an era when Nike wanted people to “be like Mike” and buy all things Jordan. Kids tried to copy the moves of their favorite player on the court, in the batter’s box and in the end zone. Twenty years later, the sports hero worship has taken a sad turn and Ryan Braun has become the latest poster child for bad behavior. His tacit admission to abusing performance enhancing drugs and suspension from baseball involves a drug mill in Florida and the revelation that the same clinic was supplying high school kids with HGH and testosterone. Be like Ryan?

Steroid abuse to enhance athletic performance has been a cat and mouse game for decades. Backroom chemists would create a designer steroid that perhaps might not be able to be detected by available drug tests. Athletes would cycle the use of the drugs they put into their bodies, hoping to test clean when their time came to present for urine or blood tests. An industry evolved to mask the presence of an illegal substance and a Google search could find thousands of sites with purported expertise. The advent of “forever young” clinics, promising eternal youth for those who could not come to terms with aging, put anabolic steroids into the mainstream and on Main Street. How could a doctor and clinic prescribe a medication unless it was proven effective, reliable and safe? Welcome to the concept of off-label prescribing.

Human growth hormone (HGH), also known as somatotropin, is produced in the brain’s pituitary gland and is responsible for cell growth and regeneration in the body. It is an anabolic hormone, responsible for increasing height in childhood but is also a major player in muscle development, blood sugar regulation, calcium metabolism, protein production and fat breakdown. For all that it can do in the body, there are very few medical indications for it to be prescribed by a physician.

Pediatrics: Treatment of children with growth failure due to growth hormone deficiency, Prader-Willi syndrome, small for gestational age, Turner syndrome and idiopathic short stature

Adult: treatment of adults with either adult onset of childhood onset of growth hormone deficiency

That’s it. These are the only approved uses of HGH. But once a drug is on the market, a physician can choose to prescribe it off-label. Supposedly, the doctor needs to balance the benefits and risks of using a medication that has not been tested and approved for a specific condition. This is a long honored tradition in medicine and many medications have been recognized for their unintended benefit and have become routine treatments. Erythromycin, an antibiotic, seems to help patients with diabetic gastroparesis, where the stomach doesn’t empty appropriately. Reglan and Compazine, two medications used to control nausea, also seem to abort migraine headaches when injected intravenously.

Off label HGH use to improve athletic performance somehow seems different. HGH allows muscle to recover from injury and overuse, letting players train more aggressively. It can promote lipolysis, breaking down fat stores in the body and may increase lean body mass by increasing the amount of water in muscles cells, but not necessarily increasing the size or number of muscle cells in the body. This is not a wonder drug. There are significant risks that include leukemia, high blood pressure, atherosclerosis, diabetes, thyroid disease and liver and pancreas problems.

Biogenesis, the suspect Florida clinic that was the source of HGH and other hormones to pro athletes, also seemed to have a younger clientele. High school athletes are alleged to have been patients receiving performance enhancing drugs with all the attendant risks that come with taking a drug your body does not need. These were not back alley dealings but instead, parents would escort their kids to Biogenesis in hopes of them becoming the next Ryan Braun.

A year before Charles Barkley demanded that parents and other take the role model responsibility, Lyle Alzado, a Pro Bowl football player and self-admitted anabolic steroid user died of a brain tumor and his portrait on the cover of Sports Illustrated became the face of steroid abuse in the NFL.  He repented his drug abuse and urged others not to follow in his steps. We have not learned from history. The golden ring of professional athlete stardom has caused performance enhancing drugs have filtered from the pros to college to high school and slowly into middle school.

Mr. Braun’s reputation will be the most significant consequence of his drug abuse admission but he has a job playing baseball next year and $100 million awaiting him in salary. For every Ryan Braun, there are too man to count players who don’t make the major leagues or even their college team. For them, the consequences may be broken and damaged bodies that will cause them to suffer a lifetime.

Be like Ryan?

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