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Bexarotene

Bexarotene is an oral retinoid primarily used to treat cutaneous T-cell lymphoma (CTCL), a rare form of cancer that affects the skin. It belongs to a class of drugs called retinoid X receptor (RXR) agonists, which are synthetic forms of vitamin A. Bexarotene works by regulating cell growth and differentiation, helping to control the abnormal growth of T-cells in the skin. It is available in both oral capsule and topical gel formulations.



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Frequently Asked Questions

How long does it take for bexarotene to show results?
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It may take several weeks to months before improvements are seen. Continuous treatment is necessary for optimal benefits.

Can bexarotene cause weight gain?
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Weight gain can occur, primarily due to fluid retention and hypothyroidism, which may develop during treatment. Regular thyroid monitoring can help manage this.

Is it safe to use bexarotene during pregnancy?
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No, bexarotene is highly teratogenic and should not be used during pregnancy. Effective contraception is mandatory for both men and women during treatment and for at least one month after stopping the medication.

Can bexarotene be used long-term?
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Yes, bexarotene can be used long-term in patients with CTCL, provided that regular monitoring of lipid levels, thyroid function, and liver enzymes is maintained.

What should I do if I miss a dose of bexarotene?
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If you miss a dose, take it as soon as you remember unless it is close to the time of your next scheduled dose. Do not double the dose to catch up.

Comprehensive Drug Guide

How Does Bexarotene Work?

Bexarotene works by selectively binding to retinoid X receptors (RXRs) in the nucleus of cells. This binding influences the transcription of genes responsible for cell growth, differentiation, and apoptosis (programmed cell death). By affecting these processes, bexarotene helps control the overgrowth of T-cells in the skin associated with cutaneous T-cell lymphoma.



Common Dosages

  • Oral capsules: 75 mg
  • Topical gel: 1% concentration

Typical Dosing

  • Oral formulation: The typical starting dose for CTCL is 300 mg/m²/day, adjusted based on body surface area. Dose adjustments may be needed based on response and tolerability.
  • Topical formulation: Apply a thin layer to the affected skin areas once or twice daily, as directed by your healthcare provider.


Typical Dosing

FDA Approved Indications

  • Cutaneous T-cell lymphoma (CTCL) in patients who are refractory to at least one prior systemic therapy.


Who Shouldn't Take Bexarotene?

  • Hypersensitivity to bexarotene or any of its components
  • Pregnancy, due to the risk of severe birth defects. Effective contraception is required during treatment and for one month after discontinuation.
  • Patients with severe hyperlipidemia or uncontrolled thyroid disorders should use caution, as bexarotene can exacerbate these conditions.


Advice From The Pharmacist

  • Bexarotene should be taken with food to improve absorption.
  • Women of childbearing potential must use effective contraception during and for at least one month after treatment, as the drug is highly teratogenic.
  • Regular monitoring of lipid levels, thyroid function, and liver enzymes is essential during treatment, as bexarotene can cause abnormalities in these areas.
  • Avoid prolonged exposure to sunlight or tanning beds, as bexarotene may increase your skin’s sensitivity to the sun.


Side Effects of Bexarotene

Common Side Effects

  • Hyperlipidemia (high cholesterol or triglycerides)
  • Hypothyroidism (low thyroid hormone levels)
  • Headache
  • Nausea
  • Skin rash
  • Fatigue


Uncommon/Severe Side Effects

  • Pancreatitis
  • Severe liver toxicity
  • Thyroid dysfunction
  • Leukopenia (low white blood cell count)


Risks and Warnings of Bexarotene

  • Teratogenicity: Bexarotene can cause severe birth defects, so it is contraindicated in pregnancy. Women of childbearing age must use effective contraception, and men must use condoms to avoid exposing pregnant partners.
  • Hyperlipidemia: Bexarotene can cause significant increases in cholesterol and triglycerides, requiring regular monitoring and possibly lipid-lowering medications.
  • Thyroid function: Bexarotene commonly induces hypothyroidism, which requires monitoring and treatment with thyroid hormone replacement if necessary.


Interactions with Bexarotene

Common Drug Interactions

  • Lipid-lowering agents: Bexarotene may require the use of statins or fibrates to control elevated lipid levels.
  • Thyroid hormone replacement: Patients with bexarotene-induced hypothyroidism may need levothyroxine or other thyroid hormones.
  • CYP3A4 inhibitors (such as ketoconazole, clarithromycin) may increase bexarotene levels and the risk of toxicity.


Alternatives to Bexarotene

  • Vorinostat: Another medication used for the treatment of cutaneous T-cell lymphoma, particularly in cases resistant to other therapies.
  • Romidepsin: A histone deacetylase inhibitor used to treat CTCL.
  • Methotrexate: An immunosuppressant sometimes used for treating various forms of cancer, including T-cell lymphomas.