Lives in the Balance: Why Doping Control Matters

As the Tour de France rolls onto stage 7, few in the general public know of the story of 21-year-old Linas Rumsas, but they need to consider it. Especially on this day, July 13, 2018, the 51st anniversary of cyclist Tommy Simpson’s death.

People ask us all the time why doping control matters. Some argue that it doesn’t and that we should just let folks use what they want. A doping free-for-all. Cynics might say that plenty of dopers have already escaped through the net in sports, at least for a time: Lance Armstrong, Tim Montgomery, Marion Jones, to name a few.

Linas Rumsas

Linas Rumsas was an up-and-coming cyclist whose life was cut short after he abused performance-enhancing drugs. Photo: Team Altopack-Eppela

The story of young Linas, a promising cyclist whose life was cut short after abusing performance-enhancing drugs, reminds us that doping can kill. We would be wise to remember that it has happened before. Linas’ story is one of the saddest we have come across and it powerfully demonstrates why many of us who have chosen to pursue anti-doping continue to do so. This one story illuminates in no uncertain terms the realities of what we all face with the scourge of doping, and yet outside of Italy and frequent readers of Cycling News, few sports fans have probably heard of it.

There have been others who have perished from doping. According to ProCon, which provides a comprehensive historical timeline of doping in sports, the first modern athlete chronicled to have died from doping was the Danish cyclist Knut Jensen at the Summer Olympics in Rome in 1960. Heat was the initial culprit but his autopsy found traces of Ronicol. ProCon describes Ronicol as an amphetamine, but Ronicol would be described more accurately as a vasodilator and can be used as an anti-ischemia drug. Though it is not on the 2018 WADA Prohibited List, it is similar to meldonium in many ways.

Stop to consider that the first drug to have been implicated in the death of an athlete in the Olympics in 1960 is not banned today! Ronicol, otherwise known as nicotinyl alcohol, is not prohibited as confirmed by the Global DRO. Its cousin meldonium wasn’t prohibited by WADA until 2016, when it caused hundreds of athletes to test positive. Some might like to think that doping is behind the peloton, but we fear it may still be in the middle. Just in a form we don’t currently define as doping, like Ronicol.

Fifty one years ago today on July 13, 1967, Tommy Simpson infamously died on the slopes of Mount Ventoux during Stage 13 of the Tour at the age of 29. His death was one of the central moments in anti-doping history. Shortly thereafter that same year the International Olympic Committee (IOC) created the IOC Medical Commission and the first drug testing began at the Olympics in 1968, with narcotics and stimulants making up the initial prohibited list. Steroids were not added until 1975.

There have been other examples of athlete deaths that have been seminal. MLB pitcher Steve Bechler, of the Baltimore Orioles, died during drills in 2003. Ephedrine was indicated as a contributing cause in his premature death, which played a role in the regulation of ephedrine as a dietary supplement ingredient in the United States.

Steroids have played a role in the demise of many young athletes, including Taylor Hooton, Efrain Marrero, and just two days ago, a young 18-year-old Irishman in Limerick. Numerous stories exist of athletes who went too far with blood doping, or performed transfusions the wrong way, leading to dire consequences. Many stories are out there but few are known to the broader sporting public.

Linas Rumsas’ story reminds us that the scourge of doping is still present and that it is just as deadly today as it was in 1967 when amphetamines derailed the promising life and career of Mr. Simpson.

Linas Rumsas is the son of Raimondas Rumsas, who himself was a professional cyclist and took third place in the 2002 Tour de France. After Raimondas’ wife Edita was caught with a van full of drugs on the way home from that Tour, they both received four-month suspended sentences in 2006. Raimondas later tested positive for EPO during the 2003 Giro d’Italia. Sadly, this experience did not seem to deter them from apparently assisting their two children with doping.

Linas rode for the Altopack-Eppela squad in Italy and had already been a national road race champion. But in May 2017, he died at age 21 of a heart attack. It was nearly 50 years to the day after Mr. Simpson had died.

Upon Linas’ death, police searched his family’s home and seized a number of banned substances and medications. In September 2017, his older brother Raimondas Jr. tested positive for the prohibited substance GHRP-6, a peptide that produces natural growth hormone. It seems a cocktail of banned substances and other medications were being used at the family home.

The result of all this has been one family torn apart, again, from doping. Perhaps doping didn’t matter to the Rumsas family either until their son died. But Linas didn’t just die, if the allegations in this case hold true. He died as a result of family support and encouragement to dope.

It gets worse. In the course of the investigation, six people have been arrested in an apparent team-sponsored doping program including the team owner, directeur sportif, pharmacist, and trainer, who stand accused of providing drugs to riders. Seventeen other people are being investigated. Sadly, however, it is too late for Linas.

Unfortunately, the recent decision to allow Chris Froome to ride again with no sanctions after testing positive for elevated levels of salbutamol has called into question the validity and utility of the anti-doping system, again, at least in some people’s eyes. WADA has tried to explain the reasoning now, including clarifying the levels (1,428 ng/ml of urine, when adjusted for specific gravity, which is above the decision limit of 1,200 ng/ml). The reasons may not satisfy everyone, or anyone, but Froome’s case is certainly not a reason to give up on anti-doping.

Linas’ story personifies why giving up on anti-doping is simply not an option and should remind us all that doping is a significant matter. In fact, it is all the more reason to recognize that the failures of the anti-doping system are largely due to a lack of resources and money. For that to change, more people will need to truly understand what is at stake when athletes dope and to demonstrate the will to do more to combat the problem.

– Oliver Catlin

Banned Sports Doping Agents and Illegal Drugs Marketed as Dietary Supplements on Amazon.com

Designer steroids and prohormones, Selective Androgen Receptor Modulators (SARMs), growth hormone secretagogues, and new blood doping agents like FG-4592 all available to athletes and consumers through the online retailer, often under the guise of dietary supplements

The media has been swarming over possible concerns about Amazon’s poor treatment of its employees. Apparently there is less scrutiny on the products the retpillsailer has available for sale. Those interested in anti-doping and drugs in sport wonder how athletes manage to get their hands on banned doping agents to enhance their performance. One simple answer, products masquerading as dietary supplements on Amazon.com.

For years we have marveled at the easy access to steroids and other drugs via Amazon.com, and have written blog posts about it in 2010, 2011, 2013 and assisted with a Slate article in May 2014. Anabolic steroids like methasterone, new drugs like the SARM Ostarine, prescription drugs, and more have all been available. Ever since we realized the prevalence of doping agents on the site, some of which were on the list of DEA Controlled Substances, we have tracked the issue further.

We recently circled back again to see how Amazon has responded, especially after the passage of the new Designer Anabolic Steroid Control Act in December 2014 (DASCA). We applaud our friends at the United Natural Products Alliance (UNPA) for promoting this bill and the government for finally enacting stronger regulations in this arena.

So what is still available at Amazon.com in the way of sports doping agents, or designer drugs? Plenty. This week, a search for prohormones brings up 94 items. When we were here a week ago there were 96, and it went up to 97 while we were exploring, so the list is constantly in flux. Having reviewed the offerings before, and being reasonably familiar with the products, we focused our review on a few items of interest. It is good that we are familiar, because for some of these potentially dangerous products, which presume to be dietary supplements, no information is provided about the ingredients.

Real problems remain. Take Blackstone Labs Alpha-1 Max, the product description on Amazon merely says, “Great product.” Visiting Strong Supplement Shop online, you find the product, label information and the ingredient, 20mg of Methyl-1-Etiocholenolol-Epietiocholanolone. This drug is otherwise known in the vernacular as Alpha One, Methyl-1-AD, or Methyl-1-Alpha. PubChem lists it as Epietiocholanolone with 43 depositor-supplied-synonyms, so the naming conventions are broad for this one compound, which is part of the challenge in tracking it and others like it.

If you Google the drug name, many links come up. Just pick one and an explanation like the following appears: “Methyl-1-Etiocholenolol-Epietiocholanolone, aka Methyl 1-AD, M1A, or Alpha One is one of the strongest designer steroid/prohormone compounds on the market.” Alpha-1 Max is not alone, Xtreme Alpha-1 contains the same drug, according to the Amazon product description.

XtremeShedThe list of steroidal products available on Amazon continues with Xtreme Shed. Strong Supplement Shop has a version of the same product which is no longer available due to the prohormone ban in 2014. According to the Amazon product description Xtreme Shed includes: “(3,3-azo-17a-methyl-5a-androstan-17b-ol) 20mg (6a-Chloro-androst-4-en-17b-ol-3-one) 30mg”. The first ingredient is known as methyldiazirinol, the second hexadrone. Both are prohormones or designer steroids. The StrongSupplementShop listing for Xtreme Shed says the product contained 4-chloro-17a-methyl-androst-4-en-17b-ol3-one, otherwise known as methylclostebol.

Methylclostebol is a steroid that was added to the DEA Controlled Substances list under the DASCA legislation, probably why Xtreme Shed was discontinued at Strong Supplement Shop. The two compounds in Xtreme Shed on Amazon are not listed by name in the DASCA language. Perhaps the one on Amazon is a new version with the ingredients adjusted in hopes of getting around the DASCA legislation? If you thought the prohormone and designer steroid era was over, think again.

It doesn’t stop there. SARMs, a new category of developing drugs that aim to mimic the effects of anabolic steroids, remain available on Amazon.com in offerings like EPG OstaLean, or Osta, or Osta Laxogen. The names and product information suggest they contain the drug Ostarine, which appears on the WADA Prohibited List. Its scientific name is Enobosarm with a long name, (2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(Trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide). In the case of Osta and Osta Laxogen, the Amazon product descriptions include the long name, the same way it is written in an FDA warning letter from December 11, 2014 addressing the sale of the SARM by another company.

Interestingly, if you purchase Osta the order is fulfilled by Amazon. What does it mean to be fulfilled by Amazon? According to the site, “Fulfillment by Amazon (FBA) is a service we offer sellers that lets them store their products in Amazon’s fulfillment centers, and we directly pack, ship, and provide customer service for these products. Something we hope you’ll especially enjoy.” So, in the case of Osta, fulfilled by Amazon apparently means that the product is currently inventoried in an Amazon warehouse, with Amazon shipping and providing customer service, all for a product described to contain a drug that the FDA has issued a warning letter against previously.

The FDA wrote the following in its warning letter, “androgenic modulator products are unapproved new drugs sold in violation of sections 505(a) and 301(d) of the Federal Food, Drug, and Cosmetic Act (FDCA) [21 U.S.C. §§ 355(a) and 331(d)] and are misbranded drugs sold in violation of sections 502 and 301(a) [21 U.S.C. §§ 352 and 331(a)] of the FDCA”. It goes on to say that SARMs, “are not dietary supplements.”

A Maxim magazine article focused on the popularity of SARMs, secretagogues and other unapproved drugs sold as supplements earlier this year. The DEA’s position on SARMs after the passage of DASCA is represented as follows in the article: “The way the statute is written, we have to be able to demonstrate a substance is chemically and pharmaceutically similar to testosterone,” says DEA spokesman Joseph Moses. “That makes them incapable of being controlled under the term anabolic steroid.” Nonetheless, SARMs certainly don’t qualify as legal dietary supplement ingredients, hence the FDA’s warning letter.

Unfortunately, the list of doping agents available at Amazon.com does not stop with steroids and SARMs. Blackstone Labs MK Ultra contains the drug Ibutamoren, also known as MK-677, according to the label and product information found elsewherefg-4592. Ibutamoren is in development for the treatment of growth disorders; in the doping realm it is known as a growth hormone secretagogue. Growth hormone secretagogues are listed generally on the WADA Prohibited List, but this specific drug does not appear yet by name. Even the new blood doping agent FG-4592 can be found on Amazon.com, although it is not currently available from the listed supplier nor is it clear if it is offered as a dietary supplement.

Athletes don’t need any kind of clandestine network to get sports doping agents; all they need is Amazon. The reality is banned and unapproved new drugs are at our finger tips often pretending to be dietary supplements. If you don’t believe this is a problem, picture a 16-year-old kid unknowingly buying a potent anabolic steroid on Amazon that can cause serious health issues, like Alpha-1 Max, and it might change your thinking. From the anti-doping perspective, we have a tough fight ahead if new doping drugs appear as supplements on Amazon.com as quickly as we can create the tests to detect them.

New Sports Doping Agent FG-4592 Not the Only HIF Drug Available to Athletes

fg-4592 What drugs are athletes using to dope? This is one of the most commonly asked questions in the realm of sports anti-doping. Recently the answer has been provided in glaring form. During the week of July 29, Dr. Don Catlin, BSCG’s chief science officer and former longtime director of the UCLA Olympic Analytical Laboratory, was interviewed by the New York Times regarding a new drug called FG-4592, which was detected in tests of at least two elite cyclists.

AstraZeneca, one of the drugs’ developers, summarizes FG-4592 as “a small molecule inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase. HIF is a protein that responds to oxygen changes in the cellular environment and meets the body’s demands for oxygen by inducing erythropoiesis, the process by which red blood cells are produced.”

FG-4592 is available in pill form and is orally active, unlike its cousin, recombinant erythropoietin, or EPO, which must be injected. Some have dubbed FG-4592 as oxygen in pill form. This new drug is a breakthrough for anemia treatment and other similar blood ailments.  doping-271623_640Unfortunately, an effective blood boosting drug in pill form is also the Holy Grail for endurance dopers. Though FG-4592 remains in third-stage clinical trials around the world, it is widely available as a research chemical on the Internet. Its apparent arrival in elite sport is troubling, yet predictable.

Similar to EPO, HIF drugs like FG-4592 help increase oxygen carrying capacity by spurring the production of red blood cells. Some researchers believe HIF stabilizers might be even more effective than EPO as they can help stimulate iron absorption and suppress the inflammation of cytokines.[1] FG-4592 was recently added to the WADA (World Anti-Doping Agency) Prohibited List for 2015, as have cobalt and other HIF stabilizers and activators in general.  No other HIF drugs are named though they would be prohibited if they are detected.

According to PubChem’s listing of Chemical Vendors, there are 18 suppliers of FG-4592 worldwide . One of the vendors, the Houston-based company APExBIO, has eight HIF-related biochemicals available on its website including BAY 87-2243, 2-Methoxyestradiol, PX 12, ML 228, KC7F2, Chetomin, DMOG, and its top seller, IOX2 (Glycine). On PubChem, there are 251 Related Compounds with Annotation to explore.

Recent positive drug tests of two elite cyclists suggest athletes have managed to obtain FG-4592 for use as a performance-enhancer. Though the chemical vendors listed on PubMed are not marketing the drug to athletes, another site does not seem as scrupulous, as it sells research peptides like FG-4592 alongside an array of “performance enhancers.”  Some research peptides at www.superhumanstore.com overlap the list of performance enhancers. Numerous drugs on the WADA Prohibited List are available on this site including Aicar, CJC-1295 (a growth hormone secretagogue), Erythropoietin-mimetic peptide 17 (EMP17), GHRP-2, Sermorelin, Thymosin Beta- 4 and more. Similar drugs are available that are not included on the WADA Prohibited List by name, like BAY 87-2243 and Follistatin 344 (a myostatin inhibitor).

The average cyclists pictureprofessional cyclist in the UCI Tour makes $142,000, according to Ernst & Young.  Top riders can earn up to $5 million. Currently, the average dose of FG-4592 is recommended at 1-2mg/kg, 3 times a week, so $780 for 500mg will buy a two- week’s supply. An athlete could buy a year’s supply for around $20,280. This is a relatively affordable rate, even to an average Tour rider. With the difference between the average salary and the top salaries in elite cycling so significant, the financial incentives to use this new drug, or its cousins, remains high.

The good news is FG-4592 is detectable with drug tests. Similar developing drugs will undoubtedly be pursued and tried by athletes in the not-too-distant future. Whether these other options, particularly those not specified on the WADA Prohibited List, are detectable only time will tell. One thing history has proven, these will not be the last athletes to test positive for a new sports doping agent.

By Oliver Catlin and Joe Taylor

[1] Medscape  (http://www.medscape.org/viewarticle/548667)