Orteronel (racemate)

Orteronel racemate is a highly selective 17,20-lyase inhibitor with IC₅₀ of 38 and 54 nM for human and rat 17, 20-Lyase, respectively. Orteronel racemate shows less active than Orteronel (IC₅₀, 19 and 48 nM for human and rat 17, 20-Lyase, respectively). IC50 & Target: IC50: 38 nM (Human 17, 20-Lyase), 54 nM (Rat 17, 20-Lyase)^[1] In Vitro: Orteronel racemate demonstrates both promising inhibitory activity against human 17,20-lyase with IC₅₀ value of 38 nM and selectivity between human 17,20-lyase and the other CYPs (vs 11-hydroxylase and CYP3A4).Both hydroxyl group and fused ring structure of Orteronel racemate may have the responsibility for its selectivity between 17,20-lyase and CYP3A4 (IC₅₀>10,000)^[1].