Linzagolix at a glance
Medicine class
Non-peptide gonadotropin-releasing hormone receptor antagonist
Licensed uses
Uterine fibroid symptoms and previously treated endometriosis
Administration
Film-coated oral tablet that may be taken with or without food
Contraception
Does not provide contraception; effective non-hormonal contraception is required when pregnancy is possible
Additional monitoring
Carries the black-triangle symbol for enhanced safety reporting
What is Linzagolix used for?
UK-licensed uses in adults of reproductive age are:
Treatment of moderate to severe symptoms caused by uterine fibroids.
Symptomatic treatment of endometriosis after previous medical or surgical treatment for endometriosis.
How does Linzagolix work?
Linzagolix blocks pituitary GnRH receptors, reducing signals that stimulate ovarian oestrogen and progesterone production. Lower hormone exposure can reduce menstrual bleeding, pelvic discomfort and pain associated with fibroids or endometriosis.
Linzagolix preparations and strengths
Tablet
Route: Oral
Strengths: 100 mg, 200 mg
How to take Linzagolix
Follow the specialist’s prescription and take any separately prescribed hormonal add-back therapy exactly as directed.
Swallow the film-coated tablet with water.
It may be taken with or without food.
Do not rely on linzagolix as contraception.
Do not stop prescribed hormonal add-back therapy independently.
Linzagolix side effects
Common or expected effects
- Hot flushes and increased sweating
- Headache
- Mood changes, including anxiety, irritability or depressed mood
- Nausea, vomiting, constipation or upper abdominal pain
- Changes in menstrual or vaginal bleeding
- Pelvic or joint pain
- Vaginal dryness or reduced libido
- Reduced bone mineral density
- Raised liver enzymes
Get urgent medical advice
- Symptoms suggesting liver injury, particularly jaundice or dark urine
- Severe or substantially worsening depression or suicidal thoughts
- Clinically important bone loss identified during monitoring
Linzagolix in pregnancy
Linzagolix is contraindicated during pregnancy, and pregnancy should be excluded before treatment. It may reduce or stop menstrual bleeding, making pregnancy harder to recognise. Use effective non-hormonal contraception and perform a pregnancy test if pregnancy is possible. Stop treatment and contact the prescriber promptly if pregnancy is confirmed.
Linzagolix while breastfeeding
Linzagolix is contraindicated while breastfeeding. It is unknown whether it enters human milk, and a risk to a breastfed infant cannot be excluded.
Linzagolix interactions
The prescriber and pharmacist should review all medicines, including contraception and separately prescribed add-back therapy.
Repaglinide
Linzagolix may increase exposure and adverse effects; concomitant use should be avoided.
Paclitaxel or sorafenib
These narrow-therapeutic-index CYP2C8 substrates may reach higher concentrations; concomitant use should be avoided.
Other CYP2C8 substrates
Monitor for increased medicine-specific adverse effects.
Medicines that prolong the QT interval
Combined use requires caution, particularly with cardiovascular disease, hypokalaemia or a family history of QT prolongation.
Common questions about Linzagolix
Answers are fully visible for fast scanning and source review.
Is linzagolix a hormonal medicine?
No. It directly blocks GnRH receptors, but this lowers the body’s production of oestrogen and progesterone.
Can linzagolix cure endometriosis?
No cure is established. Linzagolix is used to reduce symptoms after previous medical or surgical treatment.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.