A new class of yet-to-be approved drugs in development to treat a variety of diseases are being used by athletes to enhance their performance, according to researchers at the German Sport University Cologne in Germany. They found that non-steroidal and tissue-selective anabolic agents such as Selective Androgen Receptor Modulators or SARMs are being sold on the black market. The availability of authentic SARMs was recently demonstrated for the first time by the detection of the drug candidate Andarine in a product sold over the Internet, according to the study published in the journal Drug Testing and Analysis.

SARMs represent a promising class of therapeutics for the treatment of various diseases such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and cancer cachexia. The researchers say while no SARMs have yet been approved for therapeutic use, these drugs 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 or WADA prohibited the use of SARMs in sports due to their potential for misuse. WADA works closely with pharmaceutical and biotech 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 customs, was available on the Internet at a discount price of $100.

 

To prove that SARMs lacking clinical approval are distributed and potentially misused in sports, researchers analyzed the advertised substance using state-of-the-art mass spectrometric approaches with high resolution/high accuracy mass spectrometry. One unit 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. Analysis of this solution revealed the presence of SARM. Besides the detection of the active ingredient S-4, a significant amount of byproduct was observed.

 

“Major concerns result from these findings,” says researcher Mario 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 at the end of October at the United Nations Educational, Scientific and Cultural Organization's 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,” says Thevis, “demonstrates once more that the misuse of therapeutics without clinical approval by athletes cannot be dismissed.”