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