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Bexarotene

(bex-air-uh-teen)

Trade/other name(s): Targretin

Why would this drug be used?

Bexarotene capsules are used to treat skin lesions caused by cutaneous T-cell lymphoma that did not respond to prior systemic treatment.

The 1% topical gel (for use on the skin) is used to treat early stage skin lesions of cutaneous T-cell lymphoma that no longer respond to other treatments.

How does this drug work?

Bexarotene is a retinoid used as targeted therapy. Retinoids are compounds related to vitamin A that help to regulate the gene functions that allow cells to grow and divide. Bexarotene "activates" certain retinoid receptors on the cancer cell. The "turned on" receptor works with other substances to control cancer cell growth and division.
Note that most of the drug interactions and other statements listed below are for the capsules. The sections that pertain to the gel specify that the statement applies to the gel, or to both the gel and capsule.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods. (This applies to both the gel and the capsule.)
  • If you have any medical conditions such as liver disease (including hepatitis), kidney disease, or diabetes. These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you have ever had pancreatitis or gallbladder disease. Bexarotene can cause these problems or make them worse.
  • If you have high triglycerides or cholesterol (lipids or fats) in the blood. This drug can raise these levels higher.
  • If you drink a lot of alcohol. You are more likely to have problems with your liver or pancreas while on this drug.
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. This drug may cause birth defects if either the male or female is taking it at the time of conception or during pregnancy. Men and women who are taking this drug need to use 2 kinds of birth control during treatment and for a month after treatment is done. It is important to check with your doctor about what kinds of birth control can be used with this medicine. (This applies to the gel form of this drug as well as to the pill form.)
  • If you are breast-feeding. The drug may pass into breast milk and harm the baby. Breast feeding is not recommended while you are taking bexarotene capsules or using the gel.
  • About any other prescription or over-the-counter medicines you are taking, including vitamins and herbs. In fact, keeping a written list of each of these medicines (including the doses of each and when you take them) with you in case of emergency may help prevent complications if you get sick.

Interactions with other drugs

Vitamin A supplements from animal sources (such as fish liver oil) can cause toxic levels of Vitamin A in the body when taken during treatment with bexarotene. Do not take more than 15,000 IU of Vitamin A per day while on bexarotene. This applies to the gel as well as the pill form of bexarotene. Vitamin A precursors from vegetable sources (such as beta carotene) are not a problem.

Bexarotene gel can cause large amounts of DEET (from insect repellant) to be absorbed through the skin and get into your blood, raising the risk of toxic side effects. (This applies only to the gel, and not to the capsule form of the drug.)

If gemfibrozil is taken with bexarotene, it can increase blood levels of bexarotene and raise the risk of side effects. Using these 2 drugs at the same time is not recommended.

Bexarotene can increase the risk of low blood sugar if you are taking medicine for diabetes, such as insulin, pioglitazone (Actos), rosiglitazone (Avandia), acetohexamide (Dymelor), chlorpropamide (Diabinese), glimepiride (Amaryl), glipizide (Glucotrol), glyburide (DiaBeta), tolazamide (Tolinase), or tolbutamide (Orinase).

This drug can interact with a number of drugs and supplements. Some cause the drug to build up in your blood, and can worsen side effects and other problems:

  • anti-depressant drugs nefazodone (Serzone), fluvoxamine (Luvox), fluoxetine (Prozac, Serafem)
  • antibiotics erythromycin, clarithromycin, telithromycin, and similar drugs
  • anti-fungal antibiotics such as ketoconazole, itraconazole, and voriconazole
  • the anti-nausea drug aprepitant
  • certain blood pressure medicines such as diltiazem and verapamil
  • HIV drugs such as indinavir, ritonavir, amprenavir, fosamprenavir, nelfinavir, and others
  • St. John's wort (an herbal dietary supplement)
  • Other drugs may lessen the actions of bexarotene so that it doesn't work as well:
  • anti-seizure drugs carbamazepine, phenobarbital, and phenytoin
  • rifampin and rifabutin (TB drugs)
  • steroid drugs such as dexamethasone

Don't start or stop taking any drugs while you are taking bexarotene capsules without talking with your doctor first. Your dose of bexarotene may need to be adjusted before or after the change.

Baroxetene can affect the breakdown of the drug tamoxifen (used for breast cancer) and make it less effective. It may also affect other hormones, including contraceptives.

Certain medicines that are used for infection, pain, inflammation, high blood pressure, and mental illness may increase the risk of blood problems if taken with bexarotene.

Check with your doctor, nurse, or pharmacist about the other medicines, vitamins, herbs, and supplements you are taking.

Interactions with foods

Grapefruit or grapefruit juice can raise the level of this drug in your body. This can worsen any bad effects the drug may have on you and may increase its action in a harmful way.

Check with your doctor, nurse, or pharmacist about whether other foods may be a problem.

Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.

How is this drug taken or given?

Bexarotene is taken as a capsule by mouth with food. The dose of bexarotene depends on your size. To start, you will take the drug every day until a response is seen. Sometimes the bexarotene dose needs to be lowered if you have a lot of side effects. If the side effects go away on a lowered dose, then your doctor may try to slowly increase the dose again. The drug is given as long as it keeps helping you.

Do not break, chew, or dissolve capsules, and do not handle any that have been broken. If you get any of the capsule's contents on your skin, wash it off with soap and water and call your doctor or pharmacist for further instructions.

Bexarotene also comes in the form of a gel that can be used on skin lesions. Usually, it is applied every other day for the first week, once a day the next week, then increased each week until it is being used 4 times a day. Apply just enough to cover the lesion. You can spread the gel with a cotton swab or your fingers. If you use your fingers, wash your hands thoroughly afterward so that none of the medicine gets into your eyes, nose, or mouth. Never use the gel near mucous membranes (the moist pink tissues of the eyes, nose, mouth, rectal area, penis, or vagina). Wait until the gel completely dries before covering it with clothing. Do not bandage the area where the gel is applied unless your doctor tells you to do so.

Take this drug exactly as directed by your doctor. If you do not understand the instructions, ask your doctor or nurse to explain them to you.

Keep the medicine in a tightly closed container out of heat, light, and humidity, and out of the reach of children and pets.

Precautions

Sunlight, sun lamps, and tanning beds can cause severe sunburn while you are using bexarotene. Cover your skin and use sunscreen when outside during daylight hours. (This is a precaution for the gel form and the pill form of the drug.)

Bexarotene capsules may cause cataracts in your eyes. Make sure that you tell your doctor right away if your vision changes during treatment.

Your doctor will likely test your blood throughout your treatment, looking for possible effects of the drug on blood counts or on other body organs, such as increased triglycerides and total cholesterol, decreased HDL, increased blood levels of liver function, decreased blood levels of thyroid function, increased LDH, and decreased white blood cells.. Based on the test results, you may be given medicines to help treat any effects. Your doctor may also need to reduce or delay your next dose of this drug, or even stop it altogether. Keep all your appointments for lab tests and doctor visits.

Report signs of low thyroid function, such as weight gain, tiredness, slowed thinking, skin dryness, constipation, feeling cold all the time, low energy, or joint pain or stiffness.

You may have to take medicine to lower your blood lipid levels or to get your thyroid hormone levels back to normal while you are taking bexarotene. Usually your doctor monitors these blood values closely. Changes in blood lipid level and thyroid function generally go back to normal after the treatment is finished.

This drug can increase your chance of getting an infection. Be sure to let your doctor or nurse know right away if you have any signs of infection, such as fever (100.5° or higher), shaking chills, pain when passing urine, a new cough, or bringing up sputum.

This drug may increase your risk of bleeding. Speak with your doctor before taking any drugs or supplements that might affect your body's ability to stop bleeding, such as aspirin or aspirin-containing medicines, warfarin (Coumadin), or vitamin E. Tell your doctor right away if you have unusual bruising, or bleeding such as nosebleeds, bleeding gums when you brush your teeth, or black, tarry stools.

Do not get any immunizations (vaccines), either during or after treatment with this drug, without your doctor's OK. Bexarotene may affect your immune system. This could make vaccinations ineffective, or even lead to serious infections if you take a live virus vaccine during or soon after treatment. Try to avoid contact with people who have recently received a live virus vaccine, such as the oral polio vaccine or smallpox vaccine. Check with your doctor about this.

Call your doctor if you have nausea, vomiting, pain in your back or abdomen, or appetite loss. These can be signs of pancreatitis, a dangerous complication.

Report rash, severe pain at application site (gel), or peeling of skin right away.

Men and women should avoid conceiving a baby while on this drug and for at least a month afterward. If there is any chance of pregnancy, your doctor may have you use 2 forms of birth control, and get frequent pregnancy tests for women who are taking bexarotene. The drug can cause birth defects and otherwise harm the fetus. (This applies to both the gel and capsule forms of the drug.)

Possible side effects

You will probably not have most of the following side effects, but if you have any talk to your doctor or nurse. They can help you understand the side effects and cope with them.

Common

  • increased blood lipid levels (fasting triglycerides, cholesterol)*
  • decreased blood HDL cholesterol ("good cholesterol") level*
  • low thyroid function, which may require treatment*
  • headache
  • diarrhea
  • itching (gel)
  • rash (gel)*
  • pain where the gel is applied*

Less common

  • weakness or listlessness
  • flu-like symptoms
  • low white blood cell counts with increased risk of infection*
  • back pain*
  • rash
  • abdominal pain*
  • peeling of skin*
  • fever and chills*
  • hair loss
  • difficulty sleeping
  • swelling of the hands, feet or ankles

Rare

  • increased blood level of liver function tests, possible liver damage*
  • nausea*
  • vomiting*
  • pancreatitis*
  • loss of appetite*
  • bleeding*
  • cataracts*
  • allergic reaction, with trouble breathing, skin welts, itching, dizziness, or swelling of the face, mouth, or throat
  • gallbladder disease
  • birth defects if taken during pregnancy, or if pregnancy occurs up to a month after taking the drug*
  • death due to pancreatitis, liver failure, or other cause

*See "Precautions" section for more detailed information

There are other side effects not listed above that can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.

FDA approval

Yes – first approved in 1999

Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.

Last Medical Review: 02/22/2010
Last Revised: 02/22/2010