Linzagolix is an orally administered, selective, non-peptide small molecule gonadotrophin-releasing hormone (GnRH) receptor antagonist.
Linzagolix binds to and blocks the GnRH receptor in the pituitary gland, modulating the hypothalamic-pituitary-gonadal axis, resulting in a dose-dependent reduction of serum luteinising hormone (LH) and follicle-stimulating hormone (FSH) production and a subsequent dose-dependent reduction of serum estradiol and progesterone (1):
- estradiol levels of 20–50 pg/mL (the low-normal range resulting from partial suppression) are the optimal range for improving symptoms associated with endometriosis or uterine fibroids
- full suppression of the hypothalamic-pituitary-gonadal axis results in estradiol levels < 20 pg/mL and is associated with an increased incidence of hot flushes
NICE states (2):
- Linzagolix is recommended as an option for treating moderate to severe symptoms of uterine fibroids in adults of reproductive age only if:
- it is intended to be used for longer-term treatment (normally for more than 6 months and not for people who need short-term treatment, for example, before planned surgery)
- the following dosage is used:
- with hormonal add-back therapy (ABT): 200 mg once daily
- without hormonal ABT: 200 mg once daily for 6 months, then 100 mg once daily
Reference:
- Keam SJ. Linzagolix: First Approval. Drugs. 2022 Aug;82(12):1317-1325. doi: 10.1007/s40265-022-01753-9.
- NICE (August 2024). Linzagolix for treating moderate to severe symptoms of uterine fibroids