SARMs (S-4) discovered on the black market by scientists: Welcome to 2007
As usual, the scientific and medical community is at least a couple of years behind knowing what everybody in the underground already knew. A group of scientists found a supply of S-4, ordered some, and found out that it was legit. Too bad it’s been available for at least two years now…I’m personally on my fifth or sixth bottle. I could have told them this kind of thing ages ago… my supplier, the original SARM company on the internet, has been around for a pretty long time, and they’re the only guys I trust…but these scientists did confirm in a published scientific journal that legitimate S-4 is indeed currently available on the black market…something I could have told them two years ago if they weren’t busy being scientists. Here are some of the articles written about their “discovery” -
Unapproved SARM turns up on black market
A failed drug candidate for muscle wasting in cancer patients appears to be making a comeback as a black-market product for bodybuilders and fitness enthusiasts.
Antidoping researchers led by Mario Thevis, PhD, of German Sport University Cologne in Cologne, Germany, have confirmed that a substance sold over the Internet — labeled as face moisturizer and green tea extract — is actually S-4, a selective androgen receptor modulator (SARM) originally developed by GTx of Memphis, Tenn.
GTx is a legitimate development firm attempting to commercialize SARMs for medical conditions including cancer cachexia, sarcopenia, and osteoporosis. It also is working on other classes of sex hormone receptor modulators.S-4 is a nonsteroidal, arylpropionamide compound that activates certain androgen receptors, while having no effects or acting as an antagonist at others. GTx conducted a Phase I trial of S-4 about five years ago, but later dropped the compound in favor of a second-generation agent with the trade name Ostarine, which has completed Phase II trials in cancer cachexia and chronic sarcopenia.
In a report that appears in the December issue of Drug Testing and Analysis, Thevis and colleagues said they bought two 15-mL bottles of a substance described as S-4 on an Internet Web site for $100. The bottles came with no ingredient list, instructions for use, or other documentation, they said.
Thevis told MedPage Today that the site was not easy to find and did not suggest any uses for the drug. But, he said, “once you know the ‘correct’ search terms, you will end up at various Internet sites offering S-4.” He declined to identify the site that supplied the substance.
The researchers noted that products sold as performance-enhancing drugs are frequently counterfeit, so they used liquid chromatography and tandem mass spectrometry to identify the contents.
Thevis and colleagues found the bottles contained about 4.5 grams of a compound that exactly matched the published specifications of S-4. They also found a significant quantity of another organic compound, which they said was probably a byproduct of the method used to produce S-4.
Thevis and colleagues offered no explanation or speculation on where the drug originated. GTx did not respond to a request for comment.
“This product with considerable anabolic properties is readily available without sufficient research on its undesirable effects; this is especially significant where uncontrolled dosing is applied and drug impurities with unknown effects are present in considerable amounts as observed in the studied material,” Thevis said in a statement.
The hope has been that SARMs would have the desirable effects of anabolic steroids and hormones such as testosterone, but with fewer unwanted side effects.
That same hope has energized blogs and other Internet forums for bodybuilders for the past several years, as S-4 and other SARMs have gone into clinical development for legitimate medical purposes.
Earlier this year, a series of posts on a site called Mind and Muscle Forums described one member’s experiment with a drug he believed was S-4.
“So far this stuff seems pretty damn good. Strength is slightly up, pumps are great, muscles are full and hard and I’m leaning out a little bit,” the poster wrote on March 6.
Ten days later, he posted an update: “Yesterday was the start of week four. So far strength is up, pumps are ridiculous, fat loss is great, putting on a little bit of muscle, libido is through the roof.”
He did not say where he bought the drug.
In anticipation of such agents leaking out of pharma company research labs and into athletes’ hands, the World Anti-Doping Agency in 2008 put SARMs on its list of substances prohibited in sports.
At a recent international meeting, the WADA’s president, John Fahey, said government action was needed to control trafficking in illegal performance-enhancing substances.
Promising Pharmaceutical Agents Emerge as Sports Doping Products
Researchers from the German Sport University Cologne in Germany found that non-steroidal and tissue-selective anabolic agents such as Selective Androgen Receptor Modulators (SARMs) are being sold on the black market for their performance enhancing qualities. The availability of authentic SARMs was recently demonstrated for the first time by the detection of the drug candidate Andarine in a product sold via the Internet. Full findings of the study appear in the latest issue of Drug Testing and Analysis published by Wiley-Blackwell.
SARMs represent a promising class of therapeutics for the treatment of various diseases such as sarcopenia, osteoporosis, benign prostatic hyperplasia (BPH), and cancer cachexia. While none of these agents have yet been approved for therapeutic use, SARMs are gaining popularity in the sports doping community because they are believed to provide the benefits of traditional anabolic/androgenic steroids such as testosterone with fewer unwanted side effects.
In 2008, the World Anti-Doping Agency (WADA) prohibited the use of SARMs in sports due to their potential for misuse. WADA closely cooperates with pharmaceutical and biotechnological companies, as well as medicine agencies and drug evaluation bodies on the issue of therapeutics being misused in sports. WADA’s preventive approach was validated with the recent finding of a commercially available, non-approved arylpropionamide-derived SARM termed Andarine. This product, declared as green tea extracts and face moisturizer to pass customs, was available on the Internet at a discount price of $100 USD.
To prove that SARMs lacking clinical approval are distributed and potentially misused in sports, Mario Thevis, Ph.D., and colleagues, analyzed the advertised substance using state-of-the-art mass spectrometric approaches with high resolution/high accuracy (tandem) mass spectrometry. “One unit (30 mL) was purchased online and delivered in a box labeled to contain face moisturizer and green tea extract. The sealed bottle did not declare any content and no further documents accompanied package,” said Dr. Thevis. He went on to explain that LC-MS(/MS) analysis of this solution revealed the presence of S-4 at approximately 150 mg/mL with equal amounts in each container, yielding a total of 4.5 g of the SARM. The active ingredient was identified and characterized by a) its elemental composition (as determined by high resolution/high accuracy mass spectrometry, b) comparison to synthesized reference material regarding retention time and product ion mass spectrum, and c) elucidation of its mass spectrometric behavior. Besides the detection of the active ingredient S-4, a significant amount of byproduct was observed.
“Major concerns result from these findings,” explained Dr. Thevis. “This product with considerable anabolic properties is readily available without sufficient research on its undesirable effects; this is especially significant where uncontrolled dosing is applied and drug impurities with unknown effects are present in considerable amounts as observed in the studied material.”
The issue was recently addressed at the Conference of Parties to the International Convention against Doping in Sport, held October 26-28, 2009 at the United Nations Educational, Scientific and Cultural Organization’s (UNESCO) headquarters in Paris. WADA President John Fahey said that government agencies will need to adopt laws and regulations to combat the trafficking and supply of illegal substances in order to rid sport of doping.
The ease of purchasing SARMs as a performance-enhancing drug supports the need to make early implementation of screening for emerging therapeutic compounds a routine part of sports drug testing. “Our study demonstrates once more that the misuse of therapeutics without clinical approval by athletes cannot be dismissed,” Dr. Thevis concludes.
Full Citation: “Detection of the arylpropionamide-derived selective androgen receptor modulator (SARM) S-4 (Andarine) in a black-market product.” Mario Thevis, Matthias Kamber, and Wilhelm Schanzer. Drug Testing and Analysis; Published Online: November 19, 2009 (DOI: 10.1002/dta.91:).
Thursday, November 19, 2009
Sports Doping Drugs Available Online
Drugs not yet approved for medical use are easily accessible online to cheating athletes.By Emily SingerAn experimental drug that mimics the effect of steroids, such as testosterone, without many of the harmful side effects is freely available online, according to new research. A group from the German Sport University Cologne in Germany detected the compound in a product called Andarine, available online for $100 and labeled as green tea extracts and face moisturizer. The research appears in the current issue of the journal Drug Testing and Analysis.
Known as selective androgen receptor modulators, or SARMs, the drugs are being developed for diseases such as muscle-wasting and osteoporosis. The World Anti-Doping Agency, an international, independent organization based in Lausanne, Switzerland, that coordinates anti-doping regulations across sports, banned the drugs last year, before any of them were approved for medical use, in recognition of the molecules’ potential allure to sports dopers, and athletes’ willingness to take even experimental compounds. Since then, the agency has quietly been working with scientists across the globe to develop new tests to detect illegal use of the compounds.
According to a previous TR article on sports doping,
These drugs represent “a whole new horizon for anabolic therapies, and the potential for abuse will be exceedingly high,” says William Evans, director of the Nutrition, Metabolism, and Exercise Laboratory at the University of Arkansas for Medical Sciences.
SARMs work similarly to testosterone but in a more targeted way. “They are effective by binding to the steroid receptor in only specific tissue, like muscle,” says Evans, who is also a scientific advisor to GTx, a company developing the drugs. “They are not steroid drugs, but they produce the anabolic effect of the steroids.” GTx, based in Memphis, TN, has shown in a clinical trial that one compound being developed for muscle wasting and bone loss can significantly boost lean muscle mass in older people.
According to a press release from the journal,
Mario Thevis, Ph.D., and colleagues, analyzed the advertised substance using state-of-the-art mass spectrometric approaches with high resolution/high accuracy (tandem) mass spectrometry. “One unit (30 mL) was purchased online and delivered in a box labeled to contain face moisturizer and green tea extract. The sealed bottle did not declare any content and no further documents accompanied package,” said Dr. Thevis. He went on to explain that LC-MS(/MS) analysis of this solution revealed the presence of S-4 at approximately 150 mg/mL with equal amounts in each container, yielding a total of 4.5 g of the SARM. The active ingredient was identified and characterized by a) its elemental composition (as determined by high resolution/high accuracy mass spectrometry, b) comparison to synthesized reference material regarding retention time and product ion mass spectrum, and c) elucidation of its mass spectrometric behavior. Besides the detection of the active ingredient S-4, a significant amount of byproduct was observed.
“Major concerns result from these findings,” explained Dr. Thevis. “This product with considerable anabolic properties is readily available without sufficient research on its undesirable effects; this is especially significant where uncontrolled dosing is applied and drug impurities with unknown effects are present in considerable amounts as observed in the studied material.”
The issue was recently addressed at the Conference of Parties to the International Convention against Doping in Sport, held October 26-28, 2009 at the United Nations Educational, Scientific and Cultural Organization’s (UNESCO) headquarters in Paris. WADA President John Fahey said that government agencies will need to adopt laws and regulations to combat the trafficking and supply of illegal substances in order to rid sport of doping.
The ease of purchasing SARMs as a performance-enhancing drug supports the need to make early implementation of screening for emerging therapeutic compounds a routine part of sports drug testing. “Our study demonstrates once more that the misuse of therapeutics without clinical approval by athletes cannot be dismissed,” Dr. Thevis concludes.
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