Linzagolix

Linzagolix is a non-peptide, selective antagonist of the gonadotropin-releasing hormone (GnRH) receptor. It has been studied for the treatment of estrogen-dependent conditions including uterine fibroids and endometriosis. It is similar to other GnRH receptor antagonists like [cetrorelix], [relugolix], and [elagolix]. Uterine fibroids occur in >70% of women of reproductive age, and when symptomatic are associated with heavy menstrual bleeding, anemia, abdominal pain and pressure, bloating, increased urinary frequency, and reproductive dysfunction. As these fibroids are essentially estrogen-dependent phenomena, hormone therapies which suppress estrogen activity – including GnRH receptor antagonists like linzagolix – are thought to be beneficial by preventing intramyometrial growths in the endometrial glands. Linzagolix was approved for use in the European Union in June 2022 for the management of symptoms caused by uterine fibroids. Linzagolix is an orally bioavailable gonadotropin-releasing hormone (GnRH or LHRH) receptor antagonist, with potential hormone production inhibitory activity. Upon oral administration of linzagolix, this agent competes with GnRH for receptor binding and inhibits GnRH receptor signaling in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with hormonally dependent disease states including hormone-dependent prostate cancer. In women, this prevents the production of estrogen by the ovaries and may relieve symptoms from sex-hormone dependent diseases, including pain associated with endometriosis, heavy menstrual bleeding or uterine fibroids. It is grouped under the following drug class(es): LHRH analogues. The directory classifies it as a commercial API with a synthetic source/manufacturing origin. Other names for this substance include OBE-2109 and OBE2109. Its PubChem CID is 16656889.