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An 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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Tagged: Biomedicine, doping, WADA

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