elacestrant dihydrochloride: clinical use

Prescribing considerations

• Confirm an activating ESR1 mutation in plasma using an appropriately marked diagnostic or another validated test.
• Treatment should be initiated by a clinician experienced in anticancer therapy.
• Review hepatic function, thromboembolic risk, comorbidities and interacting medicines.
• Exposure rises substantially with hepatic impairment; use cautiously and follow product-specific adjustment guidance.
• Evidence is limited in people aged 75 years or older, and gastrointestinal adverse effects were more frequent in this group.
• Safety and efficacy have not been established in children or adolescents.

Contraindications and cautions

• Hypersensitivity to elacestrant or any excipient.
• Do not use during pregnancy or where effective contraception is not being used by a person who could become pregnant.

Monitoring

• Clinical benefit and treatment toxicity.
• Liver function, particularly with pre-existing hepatic impairment or symptoms of liver injury.
• Full blood count, lipids, creatinine and electrolytes where clinically appropriate.
• Nausea, vomiting, diarrhoea, appetite and hydration.
• Symptoms or signs of venous thromboembolism.
• Effects and concentrations of clinically sensitive P-glycoprotein or BCRP substrates where relevant.

Clinical pharmacology

Elacestrant is an orally active ER-alpha antagonist and degrader. It is primarily metabolised by CYP3A4, is a substrate of OATP2B1 and P-glycoprotein, and inhibits P-glycoprotein and BCRP. It is highly protein-bound and is eliminated mainly through oxidative metabolism and faecal excretion.

Formulation and product differences

• The selected presentation is a blue to light-blue, round film-coated tablet marked “ME”.
• A larger oval film-coated tablet presentation is also available; tablet presentations must not be split, crushed or chewed.

Tablet

Route: Oral

Strengths: 86 mg, 345 mg