Bexarotene

Topical bexarotene is a gel used to treat a type of cancer known as cutaneous T-cell lymphoma.

Overview

Bexarotene belongs to family of chemicals known as retinoids. These are chemically related to vitamin A and are used by the body in a range of functions.

One of the many functions of retinoids is to activate a gene contained in every cell called the 'anti-oncogene', more commonly known as the 'tumor suppressor gene'. When this gene is activated, it helps prevent healthy cells from turning into cancerous cells. By delivering retinoids to areas containing certain types of tumor, it may be possible to prevent or limit the growth of the tumor to some degree.

Bexarotene is not generally offered as a first line treatment, but is usually tried when a patient with cutaneous T-cell lymphoma has not responded to other oral or topical drugs.

Pregnant women should not use this drug under any circumstances, as it can pass to the unborn child and cause severe birth defects.

Conditions treated

  • Cutaneous T-cell lymphoma

Type of medicine

  • Retinoid (third generation)
  • Antineoplastic

Side effects

You may experience some mild discomfort, dryness or irritation in the area you applied the medication. Consult your doctor if this becomes painful or bothersome.

Bexarotene may cause photosensitivity, which means that your skin may become more sensitive to sunlight. If you are exposed to direct sunlight while taking this medication, even if for only a short period or when it does not feel very warm outside, you may experience sunburn, itching, redness or pain in the skin. If you are exposed to the sun for long periods, you may become severely sunburned.

Take the following precautions when using bexarotene to avoid or minimize side effects: avoid direct sunlight, especially in the late morning and afternoon; wear clothing, including a hat and sunglasses, that covers your skin if you do need to go outdoors; use sunscreen on any area of your skin that is exposed (your doctor or pharmacist will advise you on the strength of sunscreen you should use - normally SPF 15 as a minimum is recommended, but you may need a higher strength if you have light skin) and avoid tanning beds and sun lamps.

Other side effects

Bexarotene may cause other side effects. Consult your doctor immediately if you experience any of the following while taking this medication:

  • Bloating or swelling
  • Bruising easily
  • Coughing
  • Decreased production of urine
  • Fatigue, tiredness or weakness
  • Fever or chills
  • Headaches
  • Muscle pain the lower back or the sides
  • Pain or difficulty when urinating
  • Scaly or thick-feeling skin
  • Sore throat
  • Sticky sensation to the skin
  • Sweating
  • Swelling in the glands in the neck, groin or armpit

This is not a complete list and you may experience other side effects that are not mentioned here. Some side effects may dissipate over time as your body becomes accustomed to the presence of the drug in your body, but others may persist or require medical attention. Pay attention to how the medication is affecting your body, and, if you notice anything unusual or concerning, consult your doctor promptly.

Allergic reactions

Serious allergic reactions to bexarotene are rare. However, they can occur in some people. If you experience any of the following symptoms, seek emergency medical assistance immediately:

  • Any issues with your breathing, such as wheezing
  • Breakouts of a rash or hives
  • Loss of coordination, drowsiness, dizziness, fainting
  • Swelling in the area of the face, throat or tongue.

Dosage

Every patient will receive a different dose of bexarotene, according to factors like their age and the severity of their symptoms. Always use this medication exactly as prescribed by your doctor. If you use more, you increase the risk that you will experience unpleasant side effects. If you use less than prescribed, you may not receive enough of the drug to combat your symptoms.

Bexarotene gel is usually administered with a strength of 1%, although you may be prescribed a preparation of a different strength if this is appropriate for you. You will typically start by applying the gel less than once per day, and increase the frequency of application gradually over several weeks. The following dosing schedule is typical for adults:

Week 1 - One application every second day

Week 2 - One application every day

Week 3 - Two applications every day

Week 4 - Three applications every day

Week 5 and beyond - Four applications every day

When you are applying the medication several times a day, try to apply it at around the same time each day, and make sure the doses are evenly spaced from each other. This will help ensure that the drug is continuously in your system and working to relieve your symptoms throughout the whole day.

People over the age of 65 may be more sensitive to the effects of bexarotene, and, therefore, may require a lower dose. Your doctor will advise you on the correct dosage if you are over 65.

Ensure that you completely cover the area you are treating with the gel, and try to avoid getting the gel onto the skin surrounding the affected area. This will ensure that you are making the best use of the medication.

Do not bathe or shower for at least three hours after you have applied the gel and wait for around 20 minutes after you have bathed to apply it, so that the skin is completely dry. This will ensure that you receive the correct amount of the medication.

If you miss a dose, apply the gel as soon as you remember. The only exception to this is if it is almost time to apply your next dose. In this case, just skip the missed dose and continue the schedule as normal. Do not apply a larger amount of the gel when you miss a dose as this may make side effects more likely to occur.

Interactions

Some drugs may interact with bexarotene in ways that produce unwanted or dangerous side effects. Always tell your doctor about any prescription or over the counter medications you are taking, as well as any vitamins, nutritional products or herbal supplements. The following drugs are of particular concern:

Any topical medication - discuss with your doctor any topical medication or products you currently use.

Antifungals - the following examples of antifungal drugs may enhance the effect of bexarotene: erythromycin (E.E.S., E-Mycin, Erythrocin), itraconazole (brand name: Sporanox), gemfibrozil (brand name: Lopid), and ketoconazole (brand name: Nizoral).

Vitamin A - because topical bexarotene is chemically related to vitamin A, it is not recommended that you take any vitamin A supplements while you are using it. You should check the label of any other dietary or nutritional supplements you take to ensure they do not contain vitamin A.

Diethyltoluamide (DEET) - an insect repellant most commonly used to repel mosquitos, this chemical has a mild toxic effect, which can be enhanced to dangerous levels if used at the same time as topical bexarotene. You will probably be advised not to use insect repellants containing DEET while you are using this medication.

Warnings

Some people are allergic to bexarotene. If you are allergic to this medication, or any other retinol medication, inform your doctor before you take bexarotene. Other retinol drugs include:

  • Acitretin (Soriatane)
  • Etretinate (Tegison)
  • Isotretinoin (Accutane)
  • Tretinoin (Vesanoid)

Topical bexarotene should not be used by women who are pregnant. This medication can be extremely harmful to the unborn baby and may produce severe birth defects. If you are a woman and you are prescribed topical bexarotene, you may be asked to take several precautions while taking the medication, such as starting your use of the medication on the second or third day of your menstrual cycle. You may also be required to take a pregnancy test to confirm you are not pregnant both before you start taking the drug and after you stop using it, as well as being asked to submit a negative pregnancy test every month in order to receive your medication, and you may have to use two forms of birth control for the duration of the time you are taking the drug. If you do become pregnant while using topical bexarotene, consult your doctor immediately.

Researchers have not determined whether topical bexarotene can pass into the breast milk. As a precaution, you are not advised to breastfeed while you are using topical bexarotene.

If you are man and you have a partner who is pregnant, or who can become pregnant, you should discuss the situation with your doctor. You may need to take additional precautions to ensure that your partner does not become pregnant, and that the medication does not transfer to your partner through contact with your skin.

Grapefruit and grapefruit juice may enhance the effect of bexarotene and should be avoided while you are taking the medication.

People who have certain medical conditions are at a greater risk of experiencing side effects and other problems if they take bexarotene. Talk through your medical history with your doctor, as they may want to adjust your dose of bexarotene or monitor you more closely if you have certain medical conditions. Of particular concern are the following conditions:

  • Kidney disease - if you have kidney disease, you may be more likely to experience side effects as a result of taking bexarotene.
  • Liver disease - if you have liver disease, your body may not remove the bexarotene from your system as quickly as it otherwise would. Therefore, you may experience a stronger effect from the drug.
  • Photosensitivity conditions - bexarotene may make this condition worse, increasing your sensitivity to sunlight. Your doctor will advise you about any other precautions that you need to take while taking bexarotene.

Your doctor will likely want to see you frequently after you start taking this medication. This is to ensure that the medicine is working, and to check whether you are experiencing any undesired side effects. Make sure that you attend all of these appointments.

Wash your hands thoroughly after you have applied the medication to avoid transferring it to another part of your body, or to other people. Do not allow the medication to come into contact with your genitals, rectum, eyes, nose or mouth, as this can cause irritation.

Bexarotene gel is flammable. You should not smoke while applying it, and avoid open flames and sources of heat.

Storage

Store this medication in a dry location at room temperature, well away from sources of heat, such as heaters, radiators, direct sunlight, open flames and cooking devices. The glove compartment of your vehicle is usually too warm to store medication.

Do not store the medication in the freezer or refrigerator, as this may cause it to become damaged. Do not store the medication in your bathroom, as this is usually too hot and humid to serve as a suitable place to store your medicines.

Look for signs of damage before you take the medication. If you notice a change in the color or odor of the medication, do not use it, as it may be damaged. Talk to your pharmacist for further advice.

This medication can be harmful if used by children. Keep your topical bexarotene in a child-safe container, in a location that is too high for children to reach, and well out of their line of sight.

When you have finished your course of treatment, do not throw any remaining medication into the trash, and do not pour it down the drain or into the toilet. Take the medication to your pharmacist who may be able to dispose of it for you, or they may direct you to a 'take-back' program for medications operating in your area.

Summary

Bexarotene belongs to a class of drugs called retinoids. These are chemically related to vitamin A, and are used to suppress the growth of tumors in people with a type of cancer called cutaneous T-cell lymphoma.

Topical bexarotene products come as a gel which is applied directly to lesions caused by cutaneous T-cell lymphoma. Patients usually start by applying the gel every other day, and build up the frequency over a period of weeks, until they reach four applications per day.

Topical bexarotene can cause unwanted side effects in the people who use it. These can include sensitivity to sunlight - sometimes to the extent that sun exposure should be limited - and skin irritation.

This medication should not be taken by pregnant women, because it can pass to the unborn baby and cause serious birth defects. Women taking the drug are usually required to submit a negative pregnancy test before they are prescribed the medication.

Resources
Last Reviewed:
December 23, 2017
Last Updated:
December 22, 2017
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