tcsc0003317 Elagolix sodium

Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC₅₀ and K_i of 0.25 and 3.7 nM, respectively.

IC50 & Target: IC50: 0.25 nM (GnRHR)^[1]


Ki: 3.7 nM (GnRHR)^[2]

In Vitro: Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC₅₀ of 0.25 nM in Kinase assay. Elagolix sodium has advanced to phase 3 trials for the treatment of endometriosis and uterine fibroids. Elagolix sodium also shows NFAT inhibition with an IC₅₀ of 5.4 nM and effectively blocks Ca²⁺ flux with an IC₅₀ of 0.86 nM^[1]. Kinase assay also demonstrates that Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with a K_i value of 3.7 nM^[2].