Elagolix
GnRH analogues (agonists and antagonists)
GnRH analogues (agonists and antagonists)Pregnancy: contraindicated
Contraindicated: pregnancy is excluded before starting, and a reliable non-hormonal method is used because elagolix may weaken hormonal contraceptives.
Oral non-peptide GnRH antagonist for endometriosis pain. It lowers oestrogen, so it causes hot flushes, raised lipids and bone loss.
Quick facts
- Group
- GnRH analogues (agonists and antagonists)
- Target
- Gonadotropin-releasing hormone receptor (GnRH-R) on pituitary gonadotroph cells
- Key effects
- Hot flushes and night sweats · Headache
- Monitor
- Pregnancy test before starting · Bone health
- ATC
- H01CC03
No doses: the clinician sets them by the current guideline.
Mechanism of action
The crystal shows elagolix bound to the human GnRH receptor; part of an intracellular loop was replaced by a helper protein to allow crystallisation.
Elagolix is an oral, non-peptide GnRH receptor antagonist. Blocking the pituitary receptor lowers LH and FSH, so the ovaries make less oestrogen; endometriosis lesions, which depend on oestrogen, cause less pain. The same low oestrogen explains its hot flushes, raised lipids and loss of bone density.
- Elagolix blocks pituitary GnRH receptors
- LH and FSH fall; the ovaries make less oestrogen
- Endometriosis pain eases; low oestrogen causes side effects
Indications
- Moderate to severe pain from endometriosis. Endometriosis →
Adverse effects
Common
- Hot flushes and night sweats
- Headache, nausea, insomnia
- Changes in menstrual bleeding (irregular, less or none)
- Raised blood lipids; joint pain; weight gain; mood changes
Contraindications
- Pregnancy
- Osteoporosis or liver disease (it may be ruled out)
- Use with cyclosporine or gemfibrozil
Key interactions
- Cyclosporine and gemfibrozil
- Not combined with elagolix.
- Hormonal contraceptives
- Elagolix may make some of them less effective; a reliable non-hormonal method is used.
What is monitored
- Pregnancy test before starting, or start within days of a period
- Bone health: fracture history, calcium and vitamin D
- Mood and suicidal thoughts
- Liver tests and blood lipids
Administration and safety
- Oral tablet once or twice a day at about the same times; the course is time-limited.
- Calcium and vitamin D may be recommended during treatment.
- All other medicines are checked with the pharmacist before starting.
Pregnancy and breastfeeding
Contraindicated: pregnancy is excluded before starting, and a reliable non-hormonal method is used because elagolix may weaken hormonal contraceptives.
Nursing care
- Confirm that pregnancy is excluded and teach a non-hormonal contraceptive method.
- Ask about osteoporosis, fractures, liver disease, depression and suicidal thoughts before starting.
- Teach the patient and family to report new or worse mood changes at once.
Pharmacokinetics
- Absorption
- Oral tablet, once or twice a day, with or without food; the length of treatment is limited.
Test yourself
Think of the answer, then tap the question to see it.
Why does elagolix cause bone loss?
It lowers oestrogen, which normally protects bone density.
Which contraceptive advice is given with elagolix?
Use a reliable non-hormonal method, because elagolix may make hormonal contraceptives less effective.
Which two drugs must not be combined with elagolix?
Cyclosporine and gemfibrozil.
Connections
← Back to the class: GnRH analogues (agonists and antagonists)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Elagolix: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2018); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); Crystal structure of the protein 1 (RCSB Protein Data Bank, 2020).
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Representative model, for educational purposes only.