Linzagolix: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
Linzagolix: clinical details
Prescribing considerations
- Specialist initiation and supervision are required.
- Exclude pregnancy and review medical and family history, blood pressure, bone-health risks, mood history, cardiovascular risks and concurrent medicines.
- Consider all contraindications and precautions belonging to separately prescribed hormonal add-back therapy.
- Use caution with abnormal liver history, mild renal impairment, cardiovascular disease, QT-risk factors, depression or suicidal ideation, elevated lipids and medicines associated with bone loss.
Contraindications and cautions
- Hypersensitivity to linzagolix or an excipient
- Pregnancy or breastfeeding
- Known osteoporosis
- Genital bleeding of unexplained cause
- Any applicable contraindication to concomitant hormonal add-back therapy
Monitoring
- Assess bone mineral density before treatment when osteoporosis or bone-loss risks are present, after the first year for all patients, and subsequently according to risk and treatment context.
- Monitor adverse reactions in mild renal impairment; avoid use in moderate or severe renal impairment or end-stage renal disease.
- Obtain baseline and regular liver tests when there is a history of abnormal hepatic function; discontinue if jaundice develops.
- Monitor mood carefully in those with current or previous depression or suicidal ideation.
- Monitor lipids when elevated before treatment.
- Continue periodic clinical review, including blood pressure and treatment benefit-risk.
Clinical pharmacology
Linzagolix is a non-peptide GnRH receptor antagonist. It is rapidly absorbed, highly protein-bound, has an approximate elimination half-life of 15 hours and is eliminated mainly in urine, with about one-third through faeces.
Formulation and product differences
- The selected product is a pale-yellow, round film-coated tablet containing lactose and is essentially sodium-free.
- Linzagolix tablets do not contain hormonal add-back therapy; when required, this is prescribed separately.
- Patients with galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this formulation.
Linzagolix preparations and strengths
Tablet
Route: Oral
Strengths: 100 mg, 200 mg
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.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.