Bexarotene (Oral)

Bexarotene is a prescription medication used to treat cutaneous T-cell lymphoma.


Bexarotene is a prescription medication used to treat cutaneous T-cell lymphoma by interfering with the growth of cancerous cells. Also known by its brand name, Targretin, bexarotene is an anti-cancer drug classified as a retinoid. Retinoids are relative of vitamin A and help to control normal cell growth, cell death during embryonic development and certain tissues later in life, and cell differentiation (the typical process of making cells different from one another).

A somewhat new cancer drug class, retinoids have been used either alone or in combination with other medications to treat a variety of cancers, such as lung cancer, skin cancers, kidney cancer, acute promyelocytic leukemia, cutaneous T-cell lymphoma, bladder cancer, ovarian cancer, and head and neck cancers.

Condition(s) Treated

  • Cutaneous T-cell lymphoma (mycosis fungoides)

Type of Medicine

  • Retinoid

Side Effects

Some medications deliver treatment as well as unwanted side effects. Though many of these side effects will not occur in most patients, if they do occur, they might require medical attention. Since the dosage varies from patient to patient, the frequency of side effects generally varies. Generally, side effects occur less often in patients prescribed lower doses of this medication. Contact your doctor if you begin experiencing some of the more common side effects listed below:

  • Fever
  • Unusual weakness or tiredness
  • Puffy, dry, or cold skin or weight gain
  • Swelling of the feet, arms, legs, or hands
  • Hoarseness, cough, chills, side or lower back pain or difficult or painful urination
  • Increase in cholesterol or lipid levels
  • Skin rash or other skin and mucous membrane lesions

Some side effects that occur do not require medical attention, as they tend to go away on their own during the course of treatment as your body adjusts to the medication. Your doctor may be able to help you figure out ways to reduce or prevent some of the side effects you do experience. The more common side effects of this nature include:

  • Nausea or vomiting
  • Abdominal pain
  • Headache
  • Hair loss
  • Trouble sleeping
  • Loss of appetite
  • General feeling of illness or discomfort
  • Loss of tiredness, energy, or weakness
  • Diarrhea
  • Back pain

Some side effects you experience may not be listed. If you experience any side effects not on this list, contact your doctor right away. He or she may be able to help you report your side effects to the FDA (Food and Drug Administration).


The dosage of this medication varies from patient to patient. Follow the directions on the label or your doctor's orders. This information is the general dosage information for bexarotene. It is not intended to replace the advice of a licensed health care provider. Avoid changing your dosage unless your physician tells you to. The strength of the medication will vary as well as the amount you take. The length of time you take this medication, the time between each dose and the amount of doses per day will depend on what medical condition you're treating.

To treat cutaneous T-cell lymphoma, adults typically take around 300 milligrams for each square meter of body surface. Your dosage will be determined by your physician and will be based on your body size. This medication is to be taken once per day with a meal. After you begin taking it, your doctor might adjust your dosage as necessary. Children must have their dosages determined by their healthcare providers.

If you miss a dose of bexarotene, take the missed dose as soon as you realise - unless it's close to the time for your next dose. If that's the case, skip the dose you have missed and revert to your usual dosing schedule. Never double up on doses to make up for a dose you miss.


Generally, medications should not be combined at all, however, in some special cases, two different medications might be used in conjunction despite a potential interaction. In the case of a major, moderate, or minor drug interaction, seek medical attention. Your doctor might decide to change the dosage if this happens, or other necessary precautions may be taken. Let your physician know immediately if you're taking any of the following medications.

  • Chlortetracycline
  • Minocycline
  • Gemfibrozil
  • Demeclocycline
  • Oxytetracycline
  • Lymecycline
  • Paclitaxel
  • Doxycycline
  • Meclocycline
  • Rolitetracycline
  • Tetracylcline
  • Efavirenz
  • Methacycline

The following list contains medications that can cause an increased risk of some side effects. However, using both medications could be the best treatment for you as determined by your doctor. If your doctor does determine that you need both simultaneously, he or she may prescribe one in a lower dosage, or he or she may change how frequently you take one or both medications.

  • Atorvastatin
  • Medroxyprogesterone Acetate
  • Estradiol Valerate
  • Desogestrel
  • Tamoxifen
  • Norgestimate
  • Ethinyl Estradiol
  • Dienogest
  • Norgestrel
  • Fosphenytoin
  • Phenobarbital
  • Ethynodiol Diacetate
  • Levonorgestrel
  • Drospirenone
  • Vitamin A
  • Erythromycin
  • Mestranol
  • Estradiol Cypionate
  • Phenytoin
  • Norelgestromin
  • Etonogestrel
  • Rifampin
  • Norethindrone
  • Ketoconazole

Along with certain medications, some foods can cause interactions as well. Using alcohol or tobacco with some medications can also cause interactions. Grapefruit juice is one food that may cause an interaction, so it's best to avoid it. There are certain medical conditions that may exacerbate your condition if you take this medication while taking bexarotene. These conditions include:

Risk factors for pancreatitis can also interact with bexarotene. Those factors include:

  • Prior pancreatitis - Bexarotene can cause increased triglyceride levels, which can lead to inflammation of the pancreas
  • Drinking large quantities of alcohol
  • Taking medications that are toxic to the pancreas
  • Problems with your biliary tract or gallbladder
  • Taking medications causing high levels of triglycerides
  • High cholesterol that's not well controlled
  • Type 2 diabetes mellitus (also not well controlled)

Patients with diabetes mellitus are more likely to experience low blood sugar (hypoglycemia). Bexarotene can increase the chances of side effects in patients with kidney disease and cause patients with cataracts to develop new cataracts or their previous condition to worsen. Patients have an increased risk of infections worsening or new ones developing because of the body's decreased ability to fight off infections. Patients with herpes zoster (shingles) have a risk of this disease affecting other parts of the body. Patients with liver disease taking this medication could cause the medication to be removed more slowly from the body.


Before taking bexarotene, you and your doctor must decide if it's right for you. You must determine if the good it will do outweighs the potential risks. Consider the following information before taking bexarotene.

Talk to your doctor if you have any allergies to this medication, or any other medications. Also, inform your doctor if you have any other types of allergies, such as to food, animals, dyes, or preservatives. Read any nonprescription medication labels or packaging to determine whether you might be allergic to any of the ingredients.

You may be required to have your doctor check your progress regularly through office visits to make sure the medication is properly working and to make sure there aren't any unwanted effects.

Taking this medication means you're at a higher risk of infection. Avoiding crowds or people with colds is recommended. Be sure to report any signs of infection (including fever) to your health care provider.

Avoid getting any immunizations while you're taking bexarotene and after you stop taking it without first talking to your doctor. This medication has the ability to lower your body's resistance, meaning a higher chance you'll get the infection that the immunization is supposed to prevent. That means other people living with you should not receive the oral polio vaccine, as there's a chance that person could pass the virus on to you. You should also avoid people who've had the polio vaccine within the past several months. Avoid getting too close or staying in the same room too long with them. If you can't avoid these things, it's best you consider wearing a protective mask for your face that covers your mouth and nose.

Bexarotene also has the potential to momentarily lower your white blood cell count, which increases your chances of getting an infection. This medication has also been known to decrease platelet counts - something necessary for proper blood clotting. There are measures you can take if this occurs to reduce your risk of bleeding or infection, including:

  • Avoiding infected people. Talk to your doctor right away if you believe you're seeing signs of an infection, such as chills or fever, side or lower back pain, hoarseness or cough, or difficult or painful urination.
  • Avoiding any contact sports or other circumstances where injury or bruising might occur.
  • Avoiding touching the inside of your nose or your eyes before washing your hands. Avoid touching these parts of your body with unclean hands.
  • Talking to your doctor right away if you start to experience any unusual bruising or bleeding, pinpoint red spots on your skin, blood in the urine or stools, or black, tarry stools.
  • Using caution when using sharp objects - such as a knife or razor - to avoid cutting yourself.
  • Using caution when brushing your teeth with a normal toothbrush, or using dental floss or a toothpick. Your dentist, doctor, or nurse might recommend alternative ways to clean your gums and teeth. Consult your doctor before having any dental surgery done.

Avoid prolonged exposure to the sun, as this can cause a skin rash, redness, itching, or other discoloration of the skin, as well as severe sunburn. If you do have to go out, make sure to wear plenty of SPF 15 or higher sunscreen or sunblock, as well as protective clothing (such as a hat and sunglasses) to prevent any adverse side effects of this medication. Some patients may require a product with a higher SPF number, especially patients with a fairer complexion. You should also be sure to protect your lips with an SPF of at least 15. It's best to avoid direct sunlight between the hours of 10am and 3pm, if you can. Avoiding the use of tanning beds and sunlamps is recommended.

Maintain good nutrition and get plenty of rest while taking this medication. Many chemotherapy drugs can cause weakness or tiredness. Avoid drinking grapefruit juice, as it can increase your risk of adverse effects.

Patients who are pregnant cannot take bexarotene. A negative pregnancy test is required prior to starting this medication. This medication may harm your unborn baby, therefore, if you're pregnant or planning on becoming pregnant, you should not take bexarotene. There is an extremely heightened risk of infant deformities in patients who are or who become pregnant while taking this medication. It's best to use an effective form of birth control while taking bexarotene. Two methods are currently recommended for women of childbearing years - unless the woman chooses to abstain from sexual intercourse during treatment. Talk to your doctor about which birth control methods are best for you. Also, avoid breastfeeding while taking this medicine.

Female patients usually start bexarotene on the second or third day of their menstrual period. After a negative pregnancy test, patients are given just a one-month supply of this medication. If you become pregnant despite using birth control, stop taking this medication and call your doctor immediately.

Male patients must use condoms each time they have sexual intercourse with a pregnant female patient, or a female who is able to get pregnant while they're taking bexarotene - and for up to one month after treatment. Call your doctor if your partner gets pregnant during your course of treatment.

While taking bexarotene, drinking about two to three quarts of fluid every 24 hours is recommended, unless your doctor instructs you otherwise. Bexarotene should be taken at the same time every day along with meals containing fatty foods. If you're taking vitamin A supplements, it is recommended that you limit your intake while on bexarotene to less than 15,000IU/day. But be sure to discuss taking any vitamins or supplements with your doctor first.

Bexarotene, a retinoid, has been known to be associated with certain side effects, such as reversible elevation in liver enzymes, headaches, low thyroid levels, temporary abnormal lipid levels, and skin problems (sun sensitivity, dryness, itching, and peeling). Vitamin A supplements can increase these side effects and should be discussed with your healthcare provider before taking them.

Avoid drinking alcoholic beverages, or keep your consumption to a minimum. Discuss your alcohol intake with your doctor if you consume alcohol on a regular basis. It may interfere with your treatment.


Bexarotene should be stored in a tightly closed container and kept at room temperature. Keep it away from direct light, heat, and moisture. Do not freeze this medication and keep it out of sight and reach of children and pets.

Do not store unused or expired medication. Be sure to dispose of it properly. Avoid throwing it in the trash or flushing it down the toilet. Instead, ask your doctor or pharmacist how best to dispose of your unused medication. They may be able to suggest community medicine take-back programs that take unused medication.


Bexarotene is a great drug for patients suffering from cutaneous T-cell lymphoma. However, it can pose serious risks to patients who don't fully communicate with their physicians. As a treatment designed to stop the growth of cancerous cells, bexarotene controls normal cell growth and cell death during embryonic development. In a class of drugs called retinoids - a fairly new type of anti-cancer drug - bexarotene can cause potential side effects when combined with certain medications. Medications such as tetracycline and doxycycline can cause side effects like abdominal pain, hair loss, and dry skin.

When taken correctly, bexarotene can provide great benefits to patients with certain types of cancers, sometimes to the point of reducing certain side effects associated with their condition. You and your physician will need to work together to find the right dosage of this medication to treat your condition. This means communicating any side effects - whether listed or not - to your doctor immediately and following any instructions given carefully.

Last Reviewed:
December 23, 2017
Last Updated:
April 02, 2018