SARMs

Selective Androgen Receptor Modulators (SARMs) are therapeutic agents with anabolic activity and are typically classified based on core chemical structures into 1: Arylpropionamides; 2: Bicyclic hyantoins; 3: Quinolines; and 4: Tetrahydoquinolines. From a therapeutic perspective SARM-like compounds hold advantages over existing steroids used for the treatment of human conditions as they demonstrate full anabolic activity in target tissues such as bone and muscle but reduced androgenic activity on other organs such as liver, prostate and cardiovascular tissue thereby eliminating undesirable effects typically associated with anabolic androgenic compounds. This difference in activity profile is mainly due to androgen receptor activation by SARMs which significantly are not substrates for 5a-reductase and aromatases thus removing the amplified androgenic/estrogenic actions associated with anabolic androgenic steroids. Whilst much interest in the development of these agents has focused on their use as human therapeutic interventions, their increasing availability has led to attention being drawn to their application as illegal anabolic agents in animals and consequently these compounds now appear on the current World Anti-Doping Agency (WADA) list of prohibited substances.

SARM compounds of interest to the MET-A-FOR project

The favourable oral bioavailability and short half-life properties of SARM compounds which originally helped forge interest in their use as human therapeutics and sparked expansion of research and development for clinical use, are also properties which make them suitable as anabolic agents for use in animals– potentially illegally in either performance sports or food producing animals. Oral bioavailability facilitates ease of administration to animals whilst their short half-lives and rapid metabolism necessitates daily dosing regimens – this latter property is important from an illegal use perspective as parent compounds are eliminated from the body quickly making detection based on targeted compound analysis extremely challenging. More recently the use of SARM-like agents as growth promoting agents in food producing animals has been suggested and significantly in 2011 the first patent (WO2011119544)citing the commercial use of SARMs to increase meat production in cattle or swine animals through actions increasing the lean mass, reducing the fat mass and improving feed efficiencywas filed.

MET-A-FOR research will focus on the development of techniques to monitor for and detect the use of designer anabolic compounds such as SARMs in animals associated with food production and performance sports.