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Linzagolix choline (KLH-2109 choline) is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. Linzagolix choline inhibits the release of endogenous gonadotropins such as luteinizing hormone LH and follicle-stimulating hormone FSH by binding to the GnRH receptor within the pituitary gland. This inhibition results in a reduction in the production of sex hormones such as estrogen and progesterone, which in turn affects the course of sex hormone-dependent diseases. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids[1].

[1] Kobayashi K, et al. Non-clinical studies indicating lack of interactions between iron/calcium ions and linzagolix, an orally available GnRH antagonist[J]. Xenobiotica, 2022, 52(5): 488-497. DOI:10.1080/00498254.2022.2109076