Drug intelligence / Profile preview

linzagolix + leuprorelin acetate

Development stage
Unknown
Lead developer
Kissei Pharmaceutical
Modality
Peptides, Small Molecules
Administration
Oral, Subcutaneous
01

Overview

This entry refers to the comparative clinical evaluation of **linzagolix** (KLH-2109) and **leuprorelin acetate** for the treatment of heavy menstrual bleeding (menorrhagia) associated with uterine fibroids. Linzagolix is an orally active, non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist originally developed by Kissei Pharmaceutical and licensed to JW Pharmaceutical for development in South Korea. It works by competitively binding to GnRH receptors in the pituitary gland, leading to rapid suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which subsequently reduces ovarian estradiol production. Leuprorelin acetate is a synthetic peptide GnRH receptor agonist that, upon chronic administration, causes desensitization and downregulation of GnRH receptors, resulting in a similar suppression of the hypothalamic-pituitary-gonadal axis. In the Phase 3 study conducted by JW Pharmaceutical, these two agents were evaluated as separate treatment arms (using a double-dummy design) to compare the efficacy and safety of oral linzagolix against the standard-of-care injectable leuprorelin.

Other names
linzagolix + leuprorelinKLH-2109 + leuprorelin acetate
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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