Linzagolix for treating symptoms of endometriosis

Linzagolix is an oral GnRH receptor antagonist drug with low pharmacokinetic/pharmacodynamic (PK/PD) variability (1)

• works by binding to and blocking the GnRH receptor in the pituitary gland, which causes a dose-dependent decline in the production of LH and FSH
  • this fall in LH and FSH levels then results in a dose-dependent downturn in oestrogen concentrations

NICE has stated that (2):

• Linzagolix with hormonal add-back therapy can be used within its marketing authorisation as an option to treat symptoms of endometriosis in adults of reproductive age who have had medical or surgical treatment for their endometriosis
• the NICE committee states that "...clinical trial evidence shows that linzagolix with hormonal add-back therapy reduces dysmenorrhoea (painful periods) and non-menstrual pelvic pain compared with placebo. Indirect comparisons suggest that linzagolix with hormonal add-back therapy gives similar pain relief to leuprorelin acetate and relugolix combination therapy..."

Reference:

1. Donez J et al. Profile of Linzagolix in the Management of Endometriosis, Including Design, Development and Potential Place in Therapy: A Narrative Review. Drug Des Devel Ther. 2023 Feb 8;17:369-380.
2. NICE (June 2025). Linzagolix for treating symptoms of endometriosis