Bexarotene
Cutaneous T-Cell Lymphoma
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Drug Status
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
NO
Known Teratogen
Definite
Pharmaceutical Class
Retinoid
Controlled Drug Substance
No
Bexarotene
Summary
Bexarotene is used to treat a type of skin cancer called cutaneous T-cell lymphoma (CTCL) in patients who have not responded to other treatments.
Bexarotene works by activating retinoid X receptors. These receptors are involved in regulating gene expression that affects cell growth and differentiation. This helps to stop the growth of cancer cells.
The usual daily dose of Bexarotene for adults is 300 mg, taken orally as a single dose with a meal. The dose may be adjusted based on the patient's response and side effects.
Common side effects of Bexarotene include headache, weakness, tiredness, increased sensitivity to cold, weight gain, depression, joint or muscle pain, and dry skin. Serious adverse effects can include pancreatitis, liver toxicity, and underactive thyroid.
Bexarotene is not recommended during pregnancy due to the risk of birth defects. It is also not recommended while breastfeeding. It can interact with several medications and supplements, so it's important to inform your doctor of all medications and supplements you are taking. Bexarotene can cause dizziness and visual difficulties which can affect your ability to drive.
Indications and Purpose
How does Bexarotene work?
Bexarotene works by selectively activating retinoid X receptors (RXRs), which are involved in regulating gene expression. This activation influences cellular processes such as differentiation, proliferation, and apoptosis, helping to inhibit the growth of cancer cells in cutaneous T-cell lymphoma.
Is Bexarotene effective?
Bexarotene has been evaluated in clinical trials for the treatment of cutaneous T-cell lymphoma (CTCL). In these trials, patients with advanced and early-stage CTCL who were refractory to prior systemic therapy showed a response to Bexarotene. The medication works by activating retinoid X receptors, which regulate gene expression involved in cell growth and differentiation.
What is Bexarotene?
Bexarotene is used to treat cutaneous T-cell lymphoma (CTCL) in patients who have not responded to other treatments. It works by activating retinoid X receptors, which regulate gene expression involved in cell growth and differentiation, helping to stop the growth of cancer cells. Bexarotene is taken orally and requires careful monitoring due to potential side effects.
Directions for Use
For how long do I take Bexarotene?
Bexarotene is typically used as long as the patient is deriving benefit from the treatment. In clinical trials, it has been administered for up to 97 weeks. The duration of use will depend on the patient's response to the medication and any side effects experienced.
How do I take Bexarotene?
Bexarotene should be taken once daily with a meal to enhance absorption. Patients should avoid grapefruit and grapefruit juice, as they may increase Bexarotene levels in the blood. Regular monitoring and adherence to dietary recommendations from a healthcare provider are important for safe and effective use.
How long does it take for Bexarotene to start working?
It may take several months or longer before the full benefits of Bexarotene are noticed. Patients should continue taking the medication as prescribed and attend regular follow-up appointments to monitor progress and adjust treatment as needed.
How should I store Bexarotene?
Bexarotene should be stored at room temperature, between 20° to 25°C (68° to 77°F), and protected from light. It should be kept in its original container, tightly closed, and out of reach of children. The medication should not be stored in the bathroom to avoid exposure to moisture.
What is the usual dose of Bexarotene?
The usual daily dose of Bexarotene for adults is 300 mg/m², taken as a single oral dose with a meal. The dose may be adjusted based on the patient's response and side effects. Bexarotene is not recommended for use in children, as its safety and effectiveness have not been established in this population.
Warnings and Precautions
Can Bexarotene be taken safely while breastfeeding?
Bexarotene is not recommended for use while breastfeeding, as it is unknown whether the drug passes into breast milk. Due to the potential for serious adverse reactions in nursing infants, breastfeeding should be discontinued during treatment with Bexarotene.
Can Bexarotene be taken safely while pregnant?
Bexarotene is contraindicated during pregnancy due to the risk of birth defects. It is a retinoid, a class of drugs known to cause fetal harm. Women of childbearing potential must use effective contraception for one month before, during, and one month after treatment. Monthly pregnancy tests are recommended to ensure safety.
Can I take Bexarotene with other prescription drugs?
Bexarotene can interact with several medications, including gemfibrozil, which increases Bexarotene levels, and tamoxifen, which may have reduced effectiveness. It may also affect the metabolism of drugs processed by CYP3A4 enzymes, such as certain contraceptives, potentially reducing their effectiveness. Patients should inform their doctor of all medications they are taking to avoid interactions.
Is Bexarotene safe for the elderly?
In clinical trials, 64% of patients with CTCL were 60 years or older, and 33% were 70 years or older. No overall differences in safety were observed between older and younger patients, but greater sensitivity in some older individuals cannot be ruled out. Elderly patients should be monitored closely for side effects and may require dose adjustments.
Is it safe to drink alcohol while taking Bexarotene?
Drinking alcohol can worsen the side effects of Bexarotene, particularly those related to liver function and triglyceride levels. Patients are advised to discuss alcohol consumption with their doctor to understand the potential risks and to ensure safe use of the medication.
Who should avoid taking Bexarotene?
Bexarotene is contraindicated in pregnant women due to the risk of birth defects. It can cause hyperlipidemia, pancreatitis, hepatotoxicity, hypothyroidism, and neutropenia. Patients should avoid alcohol and sun exposure. Regular monitoring of blood lipids, liver function, and thyroid function is necessary. Patients with a history of pancreatitis or uncontrolled lipid levels should use Bexarotene with caution.
