Linzagolix
Linzagolix, sold under the brand name Yselty, is a medication used in the treatment of uterine fibroids and endometriosis. Linzagolix is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist developed by Kissei Pharmaceutical and ObsEva.
In June 2022, it was approved for medical use in the European Union and in the United Kingdom.
Medical uses
Linzagolix is indicated for treatment of moderate to severe symptoms of uterine fibroids in adult women of reproductive age and for treatment of intractable endometriosis.Available forms
Linzagolix is available as linzagolix choline, the choline salt of linzagolix, in the form of 100 and 200mg film-coated oral tablets.Pharmacology
Pharmacodynamics
Linzagolix acts as a selective antagonist of the GnRH receptor, the biological target of GnRH. By blocking this receptor, linzagolix prevents GnRH-mediated secretion of the gonadotropins, luteinizing hormone and follicle-stimulating hormone, and prevents them from signaling the gonads to produce sex hormones including estrogens, progesterone, and androgens.In clinical studies, linzagolix fully suppressed estradiol levels in women at a dosage of 200mg/day, whereas partial suppression of estradiol levels occurred at a dosage 100mg/day. Progesterone levels were also variably suppressed with these dosages.