LG121071

LG121071 is a selective androgen receptor modulator developed by Ligand Pharmaceuticals that was first described in 1999 and was the first orally active nonsteroidal androgen to be discovered. It is a tricyclic quinolone derivative, structurally distinct from other nonsteroidal AR agonists like andarine and enobosarm. The drug acts as a high-affinity full agonist of the androgen receptor , with a potency and efficacy that is said to be equivalent to that of dihydrotestosterone. Unlike testosterone, but similarly to DHT, LG121071 and other nonsteroidal androgens cannot be potentiated by 5α-reductase in androgenic tissues, and for this reason, show tissue-selective androgenic effects. In accordance, they are said to possess full anabolic activity with reduced androgenic activity, similarly to anabolic-androgenic steroids.
The in vitro metabolism of LG121071 has been characterized in anticipation of its possible use as a doping agent.