Bexarotene, Targretin

  • Indications
  • Mechanism
  1. Synthetic Retinoid (Retinoic Acid analog) with antineoplastic activity, used in T-Cell Lymphoma
  2. Bexarotene binds Retinoid X receptors (RXRs include RXR-a, RXR-b, RXR-y)
    1. Bound receptors act as transcription factors that alter gene expression
    2. Receptor binding promotes increased cell differentiation and decreased cell proliferation
    3. Induces apoptosis and Cutaneous T-Cell Lymphoma tumor regression
  • Medications
  1. Bexarotene oral capsules: 75 mg
  2. Bexarotene gel 1%
    1. Avoid applying gel under Occlusive Dressings
    2. Avoid use in combination with DEET
  • Dosing
  1. See other references for disease specific dosing protocols
  • Adverse Effects
  • Capsules (Systemic)
  • Safety
  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Systemic Retinoids are associated with severe birth defects
    2. Use reliable Contraception, with at least one form that is a non-hormonal (see Drug Interactions below)
  3. Monitoring (systemic capsules)
    1. Complete Blood Count
    2. Lipid profile
    3. Liver Function Tests
    4. Thyroid Function Tests
  • Drug Interactions
  • Capsules (Systemic)
  1. Other agents that increase Bexarotene levels
    1. Gemfibrozil
  2. CYP3A4 Inducer
    1. May decrease activity of drugs metabolized by CYP3A4 including Oral Contraceptives