Posted on April 28th, 2009 by

Class: Chemotherapy

Generic Name: Bexarotene (becks-AIR-oh-teen)
Trade Name: Targretin®

For which conditions is this drug approved? Bexarotene is FDA approved for the treatment of cutaneous T-cell lymphoma that has not responded to prior therapies.  It is important for patients to remember that physicians have the ability to prescribe medication for conditions other than those for which the drug has been approved by the FDA. Patients who have received a prescription of this drug for a condition other than which it is approved may wish to discuss this issue with their physician.

What is the mechanism of action? Bexarotene belongs to a class of agents called retinoids. Retinoids are a form of vitamin A and are involved in cellular growth and maturation. Bexarotene produces its anticancer effects by binding to retinoid receptors within a cell and disrupting the differentiation and excessive replication of cancer cells. This action inhibits the growth and proliferation of the cancer.

How is bexarotene typically given (administered)? Bexarotene is given by mouth, in capsule form, or as a gel that is administered directly onto the skin. If taken orally, bexarotene should be taken with a meal and the dose depends on several factors, including the condition being treated, the size of the patient, the particular regimen being used and the overall health of the patient.

How are patients typically monitored? Patients will usually have scheduled meetings with their healthcare provider while they are being treated with bexarotene.  Typically, blood will be drawn to check levels of blood cells and to monitor functions of some organ systems, such as the kidneys or liver.  Patients may also undergo physical examinations, scans or other measures to assess side effects and response to therapy.  In addition, patients will have their blood cholesterol, triglyceride, and glucose levels measured, as bexarotene may affect these levels.  Patients may also have their thyroid hormone levels measured.

What are the common (occur in 30% or more of patients) side effects of treatment with bexarotene?

• Skin irritation or abnormalities at the site of gel application
• Abnormalities in blood cholesterol or triglyceride levels
• Headache
• Abnormal levels of thyroid hormone
• Weakness
• Low white blood cell levels – increases risk of infection

What are the less common (occur in 10% to 29% of patients) side effects of treatment with bexarotene?

• Swelling of the hands or feet
• Nausea and vomiting
• Lack of appetite
• Abdominal pain
• Chills
• Infection
• Eye abnormalities (cataracts), visual field effects, dry eyes
• Sensitivity to sunlight
• Diarrhea
• Low red blood cell levels – increased risk of anemia
• Dry skin, rash, itchiness

This is not a complete list of side effects. Some patients may experience other side effects that are not listed here. Patients may wish to discuss with their physician the other less common side effects of this drug, some of which may be serious.

Some side effects may require medical attention. Other side effects do not require medical attention and may go away during treatment. Patients should check with their physician about any side effects that continue or are bothersome.

What can patients do to help alleviate or prevent discomfort and side effects?

• Patients often develop sensitivity to sunlight while being treated with bexarotene, and precautions against sunburn should be taken. Light clothing, hats, sunglasses and suntan lotion should all be used when going outdoors.
• Patients taking the oral form of bexarotene should take the medication with a meal containing some fat.
• Patients should not take the oral form of bexarotene with grapefruit juice.
• Avoid vitamin A supplements due to potential vitamin A toxicity (dry skin, abdominal pain, liver changes)
• Pay careful attention to the physician’s instructions and inform the physician of any side effects.
• Maintain adequate rest and nutrition.
• Drink plenty of fluids. (Patients should ask their physician about the amount of liquid to consume during a day.)
• If possible, avoid large crowds or people who are sick or not feeling well, as this drug may leave some patients susceptible to infection.
• Wash hands often to reduce the risk of infection.
• Eat small meals frequently to help alleviate nausea.

Are there any special precautions patients should be aware of before starting treatment?

• Retinoids are known to significantly increase the risk of birth defects. Women should use two types of contraception if engaged in sexual activity, or completely abstain from sexual intercourse during treatment and for at least 1 month after treatment .  Women of childbearing age are required to take a pregnancy test prior to treatment with bexarotene, and at pre-planned intervals during treatment with bexarotene.
• It is important that patients inform their physician of any pre-existing conditions (chicken pox, heart disease, kidney disease, liver disease, lung disease, etc.) as they may worsen with this drug.
• Patients should inform their physicians if they have cataracts or high cholelesterol.
• Patients should inform their physician of any other medication they are taking (whether prescription or over-the-counter, including vitamins, herbs, etc.) as they may interfere with treatment.
• Patients should check with their physician before starting any new drug or nutritional supplement.
• Patients should inform their physician of any known drug or food allergies or any reactions to medications they have experienced in the past.
• If an oral dose is missed, do not double up on doses.  Patients should contact their physician in this event.
• Keep capsules out of reach of children and return to the pharmacy for safe disposal if treatment is terminated.

When should patients notify their physician?

• Yellowing of skin or eyes
• Severe or persistent headache
• Severe abdominal pain or back pain
• Persistent nausea or vomiting
• Sudden increase in abdominal size
• Persistent or severe weakness, fatigue
• Severe or persistent diarrhea
• Changes in vision
• Swelling of feet or hands
• Fever, chills, sore throat, cough, flu or cold-like symptoms
• Signs of infection – redness, swelling, pus, tenderness
• Irregular heartbeat
• Shortness of breath

What is a package insert?

A package insert is required by the FDA and contains a summary of the essential scientific information needed for the safe and effective use of the drug for healthcare providers and consumers.  A package insert typically includes information regarding specific indications, administration schedules, dosing, side effects, contraindications, results from some clinical trials, chemical structure, pharmacokinetics and metabolism of the specific drug. By carefully reviewing the package insert, you will get the most complete and current information about how to safely use this drug. If you do not have the package insert for the drug you are using, your pharmacist or physician may be able to provide you with a copy.

Copyright © 2016 CancerConnect Last updated 07/10.

Important Limitations of Use

The information provided above on the drug you have selected is provided for your information only and is not a substitute for consultation with an appropriate medical doctor. We are providing this information solely as a courtesy and, as such, it is in no way a recommendation as to the safety, efficacy or appropriateness of any particular drug, regimen, dosing schedule for any particular cancer, condition or patient nor is it in any way to be considered medical advice. Patients should discuss the appropriateness of a particular drug or chemotherapy regimen with their physician.

As with any printed reference, the use of particular drugs, regimens and drug dosages may become out-of-date over time, since new information may have been published and become generally accepted after the latest update to this printed information. Please keep in mind that health care professionals are fully responsible for practicing within current standards, avoiding use of outdated regimens, employing good clinical judgment in selecting drugs and/or regimens, in calculating doses for individual patients, and verifying all dosage calculations.



The prescribing physician is solely responsible for making all decisions relating to appropriate patient care including, but not limited to, drugs, regimens, dose, schedule, and any supportive care.

Tags: Chemotherapy, Drug Dictionary, T

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