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Retinoid X receptor agonist (specialist)

Bexarotene

Brand names: Targretin

Adult dose

Dose: 300mg/m² PO OD with food
Route: Oral
Frequency: OD

Clinical pearls

  • NICE TA177: cutaneous T-cell lymphoma
  • BAD CTCL guidance; ESMO
  • Pregnancy Prevention Programme — contraception 1 month before, throughout, 1 month after

Contraindications

  • Pregnancy (highly teratogenic — Pregnancy Prevention Programme)
  • Severe hepatic impairment
  • Pancreatitis history
  • Hypersensitivity

Side effects

  • Hyperlipidaemia (very common)
  • Hypothyroidism
  • Hepatotoxicity
  • Photosensitivity
  • Pancreatitis
  • Cataracts
  • Cytopenias
  • Teratogenicity

Interactions

  • Strong CYP3A4 inhibitors
  • Vitamin A
  • Gemfibrozil (avoid)
  • Grapefruit juice

Monitoring

  • Lipids weekly initially
  • TFTs
  • LFTs
  • FBC
  • Pregnancy testing (PPP)

Reference: BNF; NICE TA177; BAD CTCL; ESMO; SmPC; https://bnf.nice.org.uk/drugs/bexarotene-specialist-drug/. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.