bexarotene: clinical use

Prescribing considerations

• Initiation and maintenance require a clinician experienced in treating cutaneous T-cell lymphoma.
• Normalise uncontrolled triglycerides or cholesterol before treatment and assess pancreatitis risk factors.
• Review pregnancy risk, contraception, interacting medicines, vitamin A supplementation, mental-health history and photosensitivity precautions.
• Use caution in renal impairment because clinical data are limited, despite renal elimination being minor.

Contraindications and cautions

• Hypersensitivity to bexarotene or an excipient
• Pregnancy or breastfeeding
• Pregnancy potential without effective contraception
• History of pancreatitis
• Uncontrolled hypercholesterolaemia or hypertriglyceridaemia
• Hypervitaminosis A
• Uncontrolled thyroid disease
• Hepatic insufficiency
• Ongoing systemic infection

Monitoring

• Check fasting lipids before treatment, frequently until the response is established, and regularly thereafter.
• Check liver function, haemoglobin and differential white-cell count at baseline and closely during early treatment, then regularly.
• Check thyroid function at baseline and regularly; central hypothyroidism is common and may require replacement therapy.
• Monitor mood and behaviour, especially with a history of depression.
• Arrange ophthalmological assessment if visual difficulties develop.

Clinical pharmacology

A synthetic RXR-alpha, RXR-beta and RXR-gamma agonist. Bexarotene is highly protein-bound, undergoes mainly CYP3A4-mediated oxidative metabolism and has negligible renal excretion.

Formulation and product differences

• The oral soft capsule contains a liquid suspension and must be swallowed intact.
• The capsule contains sorbitol and butylated hydroxyanisole, which may be relevant in fructose intolerance or mucosal irritation.
• Because of cytotoxic handler risk, it is not considered suitable for multi-compartment compliance aids.

Capsule

Route: Oral

Strengths: 75 mg