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Other drug names: A-Am An-Az B C-Ch Ci-Cz D-Dh Di-Dz E F G H I-J K-L M-Mh Mi-Mz N-Nh Ni-Nz O P-Pl Pm-Pz Q-R S-Sn So-Sz T-To Tp-Tz U-V W-Z 0-9   

Bexarotene (Systemic)

Brand Names

In the U.S.-

  • Targretin


  • Antineoplastic


Bexarotene (beks-AIR-oh-teen ) belongs to the group of medicines known as retinoids ( RET-i-noyds) . It is used to treat a certain type of cancer called cutaneous T-cell lymphoma. It works by interfering with the growth of the cancerous cells.

This medicine is available only with your doctor's prescription, in the following dosage form:

  • Capsule (U.S.)

Before Using This Medicine

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For bexarotene, the following should be considered:

Allergies- Tell your doctor if you have ever had any unusual or allergic reaction to bexarotene or other retinoid (vitamin A) preparations. Also tell your health care professional if you are allergic to any other substances, such as foods, preservatives, or dyes.

Pregnancy- Bexarotene must not be taken during pregnancy because of the possible risks to the infant. In addition, bexarotene must not be taken if there is a chance that you may become pregnant 1 month before treatment, during treatment, and within 1 month after treatment is ended. Women who are able to have children must have a pregnancy test done within 1 week before starting bexarotene, to make sure they are not pregnant. The pregnancy test must be repeated once a month during treatment. For 1 month before treatment with bexarotene, during treatment, and for 1 month after treatment is over, you must use two effective forms of birth control at the same time. Bexarotene may interfere with the effectiveness of hormonal birth control (such as the pills), so one form of birth control should be non-hormonal, such as condoms. Male patients with sexual partners who are pregnant, possibly pregnant, or who could become pregnant must use condoms during sexual intercourse while taking bexarotene and for at least 1 month after taking the last dose. Be sure you have discussed this information with your doctor.

Breast-feeding- It is not known whether this medicine passes into breast milk. However, bexarotene is not recommended during breast-feeding, because it may cause unwanted effects in nursing babies.

Children- Studies of this medicine have been done only in adult patients, and there is no specific information comparing the use of bexarotene in children with use in other age groups.

Older adults- This medicine has been tested in patients 60 years of age or older and has not been shown to cause different side effects or problems in older people than it does in younger adults. However, elderly patients may be more sensitive to the effects of bexarotene.

Other medicines- Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose or other precautions may be necessary. When you are taking bexarotene, it is especially important that your health care professional know if you are using any of the following:

  • Acyclovir (e.g., Zovirax) or
  • Anticonvulsants (seizure medicine) or
  • Antidiabetics, oral (diabetes medicine taken by mouth) or
  • Anti-infectives by mouth or by injection (medicine for infection) or
  • Antipsychotics (medicine for mental illness) or
  • Captopril (e.g., Capoten) or
  • Enalapril (e.g., Vasotec) or
  • Flecainide (e.g., Tambocor) or
  • Gold salts (medicine for arthritis) or
  • Imipenem or
  • Inflammation or pain medicine, except narcotics or
  • Lisinopril (e.g., Prinivil, Zestril) or
  • Maprotiline (e.g., Ludiomil) or
  • Penicillamine (e.g., Cuprimine) or
  • Pimozide (e.g., Orap) or
  • Procainamide (e.g., Pronestyl) or
  • Promethazine (e.g., Phenergan) or
  • Ramipril (e.g., Altace) or
  • Sulfasalazine (e.g., Azulfidine) or
  • Tiopronin (e.g., Thiola) or
  • Tocainide (e.g., Tonocard) or
  • Tricyclic antidepressants (medicine for depression) or
  • Trimeprazine (e.g., Temaril)-Concurrent use of these agents with bexarotene may cause blood disorders
  • Alpha interferons (e.g., Intron A, Roferon-A) or
  • Amphotericin B by injection (e.g., Fungizone) or
  • Antineoplastics, other (cancer medicine) or
  • Antithyroid agents (medicine for overactive thyroid) or
  • Azathioprine (e.g., Imuran) or
  • Chloramphenicol (e.g., Chloromycetin) or
  • Colchicine or
  • Cyclophosphamide (e.g., Cytoxan) or
  • Flucytosine (e.g., Ancobon) or
  • Ganciclovir (e.g., Cytovene) or
  • Zidovudine (e.g., AZT, Retrovir)-Concurrent use of these agents with bexarotene increases the risk of infection
  • If you have ever been treated with radiation or cancer medicines-Bexarotene may increase the effects that these medicines or radiation therapy may have on the blood
  • Phenobarbital or
  • Phenytoin (e.g., Dilantin) or
  • Rifampin (e.g., Rifadin, Rimactane) or
  • Erythromycin (e.g., E-Mycin, Ery-Tab, Ilotycin) or
  • Grapefruit juice or
  • Itraconazole (e.g., Sporanox) or
  • Ketoconazole (e.g., Nizoral)-These medicines may increase or decrease the metabolism (breakdown) of bexarotene, leading to higher-than-usual or lower-than-usual amounts of bexarotene in the body
  • Gemfibrozil (e.g., Lopid)-This medicine may lead to higher-than-usual amounts of bexarotene in the body
  • Insulin (e.g., Humulin, Novolin) or
  • Medications that make your body more sensitive to insulin, such as:
    • Pioglitazone (e.g., Actos) or
    • Rosiglitazone (e.g., Avandia)
  • Medications that help your body to secrete more insulin, such as:
    • Acetohexamide (e.g., Dymelor) or
    • Chlorpropamide (e.g., Diabinese) or
    • Glimepiride (e.g., Amaryl) or
    • Glipizide (e.g., Glucotrol) or
    • Glyburide (e.g., DiaBeta) or
    • Tolazamide (e.g., Tolinase) or
    • Tolbutamide (e.g., Orinase)-Use of bexarotene may increase the effects of these medicines, which may cause low blood sugar (hypoglycemia)
  • Tamoxifen (e.g., Nolvadex)-Bexarotene may lead to lower-than-usual amounts of tamoxifen in the body
  • Vitamin A supplements (e.g., Aquasol A)-May increase the chance of side effects

Other medical problems- The presence of other medical problems may affect the use of bexarotene. Make sure to tell your doctor if you have any other medical problems, especially
  • Bone marrow depression, existing or
  • Infection-There may be an increased risk of infections or worsening of infections because of the body's reduced ability to fight them
  • Cataracts-May cause new cataracts or worsen previous cataracts
  • Chickenpox (including recent exposure) or
  • Herpes zoster (shingles)-Risk of severe disease affecting other parts of the body
  • Diabetes mellitus-May be more likely to experience low blood sugar (hypoglycemia).
  • High cholesterol-Bexarotene can cause an increase in cholesterol levels.
  • Kidney disease-May increase the chance of side effects
  • Liver disease-Effects of bexarotene may be increased because of slower removal from the body.
  • Pancreatitis or
  • Risk factors for pancreatitis, such as:
    • Drinking large quantities of alcohol or
    • Problems with your gallbladder or biliary tract or
    • Diabetes mellitus (sugar diabetes) that is not well-controlled or
    • High cholesterol that is not well-controlled or
    • Taking medicines that cause high levels of triglycerides (fat-like substances) or
    • Taking medicines that are toxic to the pancreas or
    • Prior pancreatitis-Bexarotene can cause an increase in triglyceride levels which can cause inflammation of the pancreas.
  • Photosensitivity-Bexarotene may cause increased sensitivity of the skin to sunlight

Proper Use of This Medicine

Use this medicine exactly as directed by your doctor . Do not use more or less of it, and do not use it more often than your doctor ordered. The exact amount of medicine you need has been carefully worked out. Using too much will increase the risk of side effects, while using too little may not improve your condition.


The dose of bexarotene will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of bexarotene. If your dose is different, do not change it unless your doctor tells you to do so.

  • For oral dosage form (capsule):
    • For cutaneous T-cell lymphoma:
      • Adults-Dose is based on body size and must be determined by your doctor. The usual dose is 300 milligrams (mg) for each square meter of body surface area taken once a day with a meal. Your dose may then be adjusted by your doctor.
      • Children-Use and dose must be determined by your doctor.

Missed dose-

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.


To store this medicine:

  • Keep out of the reach of children.
  • Do not store in the bathroom, near the kitchen sink, or in other damp places. Heat or moisture may cause the medicine to break down.
  • Do not keep outdated medicine or medicine no longer needed. Ask your health care professional how you should dispose of any medicine you do not use. Be sure that any discarded medicine is out of the reach of children.

Precautions While Using This Medicine

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly and to check for unwanted effects.

While you are being treated with bexarotene, and after you stop treatment with it, do not have any immunizations (vaccinations) without your doctor's approval . Bexarotene may lower your body's resistance, and there is a chance you might get the infection that the immunization is meant to prevent. In addition, other persons living in your household should not take oral polio vaccine, since there is a chance they could pass the polio virus on to you. Also, avoid persons who have taken oral polio vaccine within the last several months. Do not get close to them, and do not stay in the room with them for very long. If you cannot take these precautions, you should consider wearing a protective face mask that covers the nose and mouth.

Bexarotene can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. It can also lower the number of platelets, which are necessary for proper blood clotting. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection or bleeding:

  • If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.
  • Check with your doctor immediately if you notice any unusual bleeding or bruising; black, tarry stools; blood in urine or stools; or pinpoint red spots on your skin.
  • Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.
  • Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
  • Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.
  • Avoid contact sports or other situations where bruising or injury could occur.

Bexarotene may cause your skin to be more sensitive to sunlight than it is normally. Exposure to sunlight, even for brief periods of time, may cause a skin rash, itching, redness or other discoloration of the skin, or a severe sunburn. When you begin taking this medicine:

  • Stay out of direct sunlight, especially between the hours of 10:00 a.m. and 3:00 p.m., if possible.
  • Wear protective clothing, including a hat. Also, wear sunglasses.
  • Apply a sun block product that has a skin protection factor (SPF) of at least 15. Some patients may require a product with a higher SPF number, especially if they have a fair complexion. If you have any questions about this, check with your health care professional.
  • Apply a sun block lipstick that has an SPF of at least 15 to protect your lips.
  • Do not use a sunlamp or tanning bed or booth.

Side Effects of This Medicine

Side Effects of This Medicine

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Since this medication is given in varying doses, the actual frequency of side effects may vary. In general, side effects are less common with lower doses than with higher doses.

Check with your doctor as soon as possible if any of the following side effects occur:

  • More common
    • Unusual tiredness or weakness;  skin rash or other skin and mucous membrane lesions;  fever;  increase in lipid or cholesterol levels;  coldness, dry, puffy skin or weight gain;  chills, cough, hoarseness, lower back or side pain or painful or difficult urination;  swelling of the arms, feet, hands, or legs 

  • Less Common
    • Severe stomach pain with nausea or vomiting;  shortness of breath;  yellow eyes or skin  

Other side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. However, check with your doctor if any of the following side effects continue or are bothersome:

  • More common
    • Abdominal pain;  hair loss;  loss of appetite;  loss of strength or energy, tiredness or weakness;  back pain;  diarrhea;  dry skin;  general feeling of discomfort or illness;  trouble in sleeping;  headache;  nausea or vomiting  

Other side effects not listed above may also occur in some patients. If you notice any other effects, check with your doctor.

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Last updated: Tue, 06 Jan 2009 00:20:03 GMT