LG121071 (or LGD-121071) is a selective androgen receptor modulator (SARM) developed by Ligand Pharmaceuticals that was first described in 1999 and was the first orally active nonsteroidal androgen to be discovered.[1][2] It is a tricyclic quinolone derivative, structurally distinct from other nonsteroidal AR agonists like andarine and enobosarm (ostarine).[2] The drug acts as a high-affinity full agonist of the androgen receptor (AR) (Ki = 17 nM),[2] with a potency and efficacy that is said to be equivalent to that of dihydrotestosterone (DHT).[3] Unlike testosterone, but similarly to DHT, LG121071 and other nonsteroidal androgens cannot be potentiated by 5α-reductase in androgenic tissues (nor aromatized into estrogenic metabolites), and for this reason, show tissue-selective androgenic effects.[4] In accordance, they are said to possess full anabolic activity with reduced androgenic activity, similarly to anabolic-androgenic steroids.[5]
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| Other names | LG-121071; LGD-121071 |
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| Formula | C15H15F3N2O |
| Molar mass | 296.293 g·mol−1 |
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The in vitro metabolism of LG121071 has been characterized in anticipation of its possible use as a doping agent.[5][6]