Retinoid X receptor agonist (specialist) Pregnancy: Contraindicated in pregnancy and breastfeeding, and in women of child-bearing potential without effective birth-control measures. No adequate human data; animal studies show reproductive toxicity and a margin of safety for human teratogenicity has not been demonstrated. Obtain a negative sensitive pregnancy test (e.g. serum beta-hCG) within one week before starting; effective contraception must be used from the negative test through initiation, during therapy and for at least one month after discontinuation, with two reliable forms used simultaneously where contraception is required and a non-hormonal method included. Male patients with partners who are or may become pregnant must use condoms during treatment and for at least one month after the last dose. Bexarotene should not be used in breastfeeding mothers.

Bexarotene

Brand names: Targretin

Bexarotene is a retinoid (rexinoid) used in the treatment of skin manifestations of advanced cutaneous T-cell lymphoma in patients refractory to at least one prior systemic therapy.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 300 mg/m²/day (recommended initial dose), given as whole 75 mg capsules per body surface area: BSA 0.88–1.12 m² = 300 mg/day (4 capsules); 1.13–1.37 m² = 375 mg (5); 1.38–1.62 m² = 450 mg (6); 1.63–1.87 m² = 525 mg (7); 1.88–2.12 m² = 600 mg (8); 2.13–2.37 m² = 675 mg (9); 2.38–2.62 m² = 750 mg (10)

Route: Oral — taken as a single daily dose with a meal; the capsule must be swallowed intact and not chewed (it contains butylated hydroxyanisole, which may irritate mucous membranes)

Frequency: Once daily — treatment should be continued as long as the patient is deriving benefit (bexarotene was given for up to 118 weeks in clinical trials)

Max: Doses greater than 650 mg/m²/day have not been evaluated in patients with CTCL

Source: UK SPC (eMC) §4.2 for Bexarotene 75 mg soft capsules (https://www.medicines.org.uk/emc/product/15579/smpc). VERBATIM: 'The recommended initial dose is 300 mg/m2/day.' INDICATION: cutaneous T-cell lymphoma (CTCL); therapy should only be initiated and maintained by physicians experienced in treating CTCL. DOSE MODIFICATION: the 300 mg/m²/day level may be reduced to 200 mg/m²/day, then to 100 mg/m²/day, or temporarily suspended, if necessitated by toxicity; when toxicity is controlled doses may be carefully readjusted upward. With appropriate clinical monitoring, individual patients may benefit from doses above 300 mg/m²/day. LIPID MONITORING AND MANAGEMENT: measure fasting triglycerides and cholesterol before starting, then weekly until the lipid response is established (usually 2–4 weeks) and at least monthly thereafter; fasting triglycerides should be normal or normalised before starting, and every attempt should be made to keep triglycerides below 4.52 mmol/L; if triglycerides are or become elevated, start antilipaemic therapy and if necessary reduce the dose (300 → 200 → 100 mg/m²/day) or discontinue. LIVER MONITORING: baseline LFTs, then weekly for the first month and monthly thereafter; consider suspension or discontinuation if AST, ALT or bilirubin exceed three times the upper limit of normal. OTHER: patients receiving bexarotene should not donate blood; use with caution in known retinoid hypersensitivity. ELDERLY: use the standard dose. PAEDIATRIC: safety and efficacy in children under 18 years have not been established; no data are available. CROSS-CHECK (US labelling, openFDA/DailyMed, Targretin, Bausch Health US, label date 2020-04-30): same 300 mg/m²/day initial dose and the same BSA table, and additionally states that if there is no tumour response after 8 weeks and the 300 mg/m²/day dose is well tolerated, the dose may be escalated to 400 mg/m²/day with careful monitoring — that escalation step is NOT in the UK SPC text fetched. The eMC §4.4 and §4.8 text was truncated at the source-fetch limit.

Dose adjustments

Renal

No formal studies have been conducted in renal insufficiency. Urinary elimination is a minor excretory pathway (estimated renal clearance was less than 1 mL/min in all evaluated patients). In view of the limited data, patients with renal insufficiency should be monitored carefully while on bexarotene therapy — no numeric dose adjustment is stated.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or to any of the excipients
Pregnancy and lactation
Women of child-bearing potential without effective birth-control measures
History of pancreatitis
Uncontrolled hypercholesterolaemia
Uncontrolled hypertriglyceridaemia
Hypervitaminosis A
Uncontrolled thyroid disease
Hepatic insufficiency
Ongoing systemic infection

Side effects

Hyperlipaemia, primarily elevated triglycerides (74%) and hypercholesterolaemia (28%) — acute pancreatitis associated with elevated fasting triglycerides has been reported
Hypothyroidism (29%)
Headache (27%)
Leucopenia (20%)
Pruritus (20%), rash (16%) and exfoliative dermatitis (15%)
Asthenia (19%) and pain (12%); liver function test abnormalities

Interactions

Gemfibrozil — substantially increases plasma bexarotene concentrations; concomitant administration is NOT recommended (eMC §4.4)
Atorvastatin — bexarotene concentrations were not affected by concomitant atorvastatin in clinical studies (eMC §4.4)
Oestroprogestative / hormonal contraceptives — bexarotene can potentially induce metabolic enzymes (CYP3A4) and theoretically reduce contraceptive efficacy; a reliable non-hormonal contraceptive method is also recommended (eMC §4.6; US label §7). Full eMC §4.5 was not included in the fetched bundle.
Laboratory test interference — CA125 assay values in patients with ovarian cancer may be increased by bexarotene therapy (US label §7)

Clinical monograph

How it works

It selectively binds and activates retinoid X receptors, modulating gene transcription to influence cellular differentiation and apoptosis of malignant lymphocytes.

Prescribing in practice

It commonly causes marked hyperlipidaemia and central hypothyroidism, which require baseline and ongoing monitoring and management.
It is a specialist oral retinoid used only under supervision of clinicians experienced in cutaneous T-cell lymphoma.
It is teratogenic and strictly contraindicated in pregnancy; concurrent vitamin A supplements and photosensitivity also warrant caution.

Monitoring

Monitor fasting lipids, thyroid function, full blood count and liver function before and regularly during treatment.

Counselling the patient

Pregnancy must be avoided; use reliable contraception during and for a period after treatment.
Avoid additional vitamin A supplements and limit sun exposure.
Attend regular blood tests to check cholesterol and thyroid function.

Evidence & guidelines

Its activity in cutaneous T-cell lymphoma is supported by registration studies and reflected in its licensed indication and the SPC.

Reference: NICE TA177; BAD CTCL; ESMO; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Myasthenia Gravis Activities of Daily Living (MG-ADL) Scale · Neuromuscular

Pathways