Bexarotene | Side Effects, Dosage, Uses & More
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Generic Name:

bexarotene, Oral capsule

All Brands

  • Targretin
SECTION 1 of 5

Highlights for bexarotene

Oral capsule
1

Bexarotene is used to treat cutaneous T-cell lymphoma. This is a type of skin cancer. It’s given to people who haven’t responded to at least one other cancer medication.

2

This drug comes in the form of a capsule you take by mouth.

3

Bexarotene is available as a brand-name drug called Targretin. It’s also available as a generic drug.

4

The more common side effects of this drug include headache, insomnia (not being able to sleep), low energy levels caused by hypothyroidism (underactive thyroid), weakness, and a rash.

5

In some cases, bexarotene can cause serious side effects. These can include higher cholesterol and triglyceride levels, pancreatitis (swelling of your pancreas), liver problems, underactive thyroid, low white blood cell count, and cataracts.

IMPORTANT INFORMATION

FDA warning

This drug has a black box warning. This is the most serious warning from the Food and Drug Administration (FDA). A black box warning alerts doctors and patients about drug effects that may be dangerous.

Birth defects warning: You shouldn’t use this drug if you’re pregnant or plan to become pregnant. It can seriously harm or even end a pregnancy. If you get pregnant while taking this drug, call your doctor right away.   

Women of childbearing age should use two reliable forms of birth control during treatment. You should use birth control one month before you start taking this drug, while you’re taking this drug, and for one month after stopping this drug. At least one of these forms of birth control shouldn’t contain hormones. Examples of non-hormonal birth control include condoms, diaphragms, cervical caps, IUDs, or spermicides.

Men with female partners who are able to become pregnant must use a condom during treatment. They must continue using a condom for at least one month after taking their last dose of this drug.

Increase in blood fats

This drug may raise the levels of fats in your blood (triglyceride and cholesterol levels).  Your doctor will check these levels during treatment with this drug. If they get too high, your doctor may lower your dose, have you stop taking this drug, or treat you with cholesterol medication.

Underactive thyroid

This drug may cause hypothyroidism (underactive thyroid). Your doctor will do blood tests to check for this. If you develop an underactive thyroid, your doctor may give you medication to treat it.

Decrease in white blood cells

This drug may decrease the levels of white blood cells in your body. This means your body can’t fight off infections as well. Your doctor will check your white blood cell count before starting and during treatment with this drug. If your white blood cell counts are too low, your doctor may reduce your dose or have you temporarily stop treatment with this drug.

Drug features

This drug is a prescription drug. It’s available as an oral capsule.

This drug is available as a generic drug. Generic drugs usually cost less. In some cases, they may not be available in every strength or form as the brand-name version.

This drug may be used as part of a combination therapy. This means you may need to take it with other medications.

Why it's used

This drug is used to treat cutaneous T-cell lymphoma. This is a type of skin cancer. It’s given to people who haven’t responded to at least one other cancer medication.

How it works

This drug belongs to a class of drugs called retinoids. A class of drugs is a group of medications that work in a similar way.

More Details

How it works

This drug belongs to a class of drugs called retinoids. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

This drug works by stopping the growth of cancer cells.

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bexarotene Side Effects

Oral capsule

More Common Side Effects

The more common side effects of bexarotene can include:

  • high triglyceride and cholesterol levels (fats in your blood)

  • hypothyroidism (underactive thyroid)

  • headache

  • insomnia (not being able to sleep)

  • lack of energy or weakness

  • rash

  • low white blood cell count.  This may lead to an infection. Symptoms may include:

    • fever
    • chills
  • nausea

  • infection

  • edema (fluid buildup that causes swelling)

  • stomach pain

  • dry skin

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.

Serious Side Effects

Call your doctor right away if you have serious side effects. Call 9-1-1 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

  • High triglyceride and cholesterol levels (fats in your blood)

  • Pancreatitis (swelling of your pancreas). Symptoms can include:

    • upper stomach pain
    • stomach pain that spreads to your back
    • stomach pain that’s worse after eating
    • nausea and vomiting
    • stomach tenderness
    • unexplained weight loss
    • smelly, oily stools
  • Liver problems, including liver failure. Symptoms can include:

    • yellowing of your skin and the whites of your eyes
    • stomach swelling and pain
    • bruising more easily than normal
    • swelling in your ankles and legs
    • feeling tired all of the time
    • pale, black, or bloody stools
    • vomiting and nausea
    • itchy skin
    • dark-colored urine
    • loss of appetite
  • Hypothyroidism (underactive thyroid). Symptoms can include:

    • tiredness and weakness
    • constipation
    • dry skin
    • increased sensitivity to cold
    • unexplained weight gain
    • depression
    • trouble remembering things
    • irregular or heavier than normal menstrual periods
    • hair thinning
  • Low white blood cell count. Symptoms can include:

    • fatigue
    • infections
    • fever
  • Cataracts. Symptoms can include:

    • clouded or blurred vision
    • trouble seeing at night
    • eye sensitivity to glare and light
Pharmacist's Advice
Healthline Pharmacist Editorial Team

This drug doesn’t cause drowsiness.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.
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bexarotene May Interact with Other Medications

Oral capsule

Bexarotene can interact with other medications, vitamins, or herbs you may be taking. An interaction is when a substance changes the way a drug works. This can be harmful or prevent the drug from working well.

To help avoid interactions, your doctor should manage all of your medications carefully. Be sure to tell your doctor about all medications, vitamins, or herbs you’re taking. To find out how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.

Food interactions

Grapefruit juice increases the levels of bexarotene in your blood. This may raise your risk of side effects from bexarotene.

Alcohol interaction

The excessive use of drinks that contain alcohol can increase your risk pancreatitis (swelling of your pancreas) from bexarotene. If you drink alcohol, talk to your doctor. You may need to be monitored for signs of pancreatitis.

Medications that might interact with this drug

Drugs that should not be used with this drug

Do not take these drugs with bexarotene. When used with bexarotene, these drugs can cause dangerous effects in the body. Examples of these drugs include:

  • Vitamin A. Taking bexarotene with Vitamin A can increase your risk of vitamin A toxicity. This can cause nausea, vomiting, headache, dizziness, and blurred vision. You shouldn’t take these drugs together.
  • Gemfibrozil. This drug increases the levels of bexarotene in your blood. This may raise your risk of side effects from bexarotene.

Interactions that increase your risk of side effects
  • Side effects from bexarotene: Taking bexarotene with certain medications raises your risk of side effects from bexarotene. This is because the amount of bexarotene in your body is increased. Examples of these drugs include:
    • Antibiotics, such as erythromycin
    • Antifungals, such as ketoconazole and itraconazole
  • Side effects from other drugs: Taking bexarotene with certain medications raises your risk of side effects from these drugs. Examples of these drugs include:
    • Diabetes drugs, such as insulin, glipizide, pioglitazone, or repaglinide. Taking these drugs with bexarotene can raise your risk of hypoglycemia (low blood sugar).

Interactions that can make your drugs less effective
  • When bexarotene is less effective: When bexarotene is used with certain drugs, it may not work as well to treat your condition. This is because the amount of bexarotene in your body may be decreased. Examples of these drugs include:
    • Tuberculosis drugs, such as rifampin and rifabutin
    • Seizure drugs, such as phenytoin and phenobarbital
  • When other drugs are less effective: When certain drugs are used with bexarotene, they may not work as well. This is because the amount of these drugs in your body may be decreased. Examples of these drugs include:
    • Oral contraceptives or other hormonal contraceptives. Your doctor will recommend that you also use a non-hormonal form of birth control. These include condoms, diaphragms, cervical caps, IUDs, or spermicides.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs interact differently in each person, we cannot guarantee that this information includes all possible interactions. This information is not a substitute for medical advice. Always speak with your healthcare provider about possible interactions with all prescription drugs, vitamins, herbs and supplements, and over-the-counter drugs that you are taking.

People with a history of pancreas problems

This drug can raise your risk of pancreatitis (swelling of your pancreas). Your risk may be higher if you have or previously had pancreas problems, including pancreatitis.

People with a history of gallbladder problems

This drug can raise your risk of pancreatitis (swelling of your pancreas). Your risk may be higher if you have or previously had gallbladder problems.

People with diabetes

If you have diabetes that isn’t controlled well, this drug can increase your risk for pancreatitis (swelling of your pancreas).

People with high cholesterol or triglycerides

If you have high levels of fats (cholesterol or triglycerides) in your blood that aren’t controlled well, this drug can increase your risk for pancreatitis. This drug may also further raise your triglycerides and cholesterol. Your doctor will check these levels during treatment with this drug. If they become too high, your doctor may lower your dose, have you stop taking this drug, or treat you with cholesterol medications called statins.

People with a history of liver problems

If you have liver problems or a history of liver disease, you may not be able to clear this drug from your body well. This may increase the levels of this drug in your body. This can cause more side effects. This medication may also make your liver disease worse. This can lead to liver failure and death. Your doctor will monitor your liver function while you’re taking this drug.

People with thyroid problems

This drug may cause you to develop an underactive thyroid. This may affect your thyroid treatment. Your doctor will check your thyroid function with blood tests while you’re taking this drug. Your doctor may adjust your thyroid medication.

People with a history of cataracts

This drug may make your cataracts worse or cause new cataracts to form. If you have any changes in vision, tell your doctor. You may need to have an eye exam.

People with a low white blood cell count

This drug may further decrease your white blood cell count. This means your body can’t fight off infections as well. Your doctor will check your white blood cell count before starting and during treatment with this drug.

People with a history of ovarian cancer

Tell your doctor if you have or previously had ovarian cancer before starting this drug. This drug may increase the protein CA125 in your blood. This protein may be used to check for ovarian cancer during and after treatment. It can detect early ovarian cancer in people with a very high risk for the disease.

Pregnant women

This drug is a category X pregnancy drug. That means two things:

Category X drugs should never be used during pregnancy.

Women of childbearing age should use two reliable forms of birth control during treatment. You should use birth control one month before you start taking this drug, while you’re taking it, and one month after stopping this drug. At least one form of birth control shouldn’t contain hormones. Examples of non-hormonal birth control include condoms, diaphragms, cervical caps, IUDs, or spermicides.

Men with female partners who are able to become pregnant must use a condom during treatment. They must continue using a condom for at least one month after taking their last dose of this drug.

Women who are breast-feeding

This drug may pass into breast milk and may cause side effects in a child who is breast-fed.

Talk to your doctor if you breast-feed your child. You may need to decide whether to stop breast-feeding or stop taking this medication.

For children

This drug hasn’t been studied in children. It shouldn’t be used in people younger than 18 years.

When to call the doctor

Call your doctor right away if you become pregnant while taking this drug or one month after you stop taking it.

Allergies

This drug can cause a severe allergic reaction. Symptoms can include:

  • trouble breathing
  • swelling of your throat or tongue

If you have an allergic reaction, call your doctor or local poison control center right away. If your symptoms are severe, call 9-1-1 or go to the nearest emergency room.

Don’t take this drug again if you’ve ever had an allergic reaction to it. Taking it again could be fatal (cause death).

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How to Take bexarotene (Dosage)

Oral capsule

All possible dosages and drug forms may not be included here. Your dosage, drug form, and how often you take the drug will depend on:

  • your age
  • the condition being treated
  • how severe your condition is
  • other medical conditions you have
  • how you react to the first dose

What are you taking this medication for?

Cutaneous T-cell lymphoma

Generic: bexarotene

Form: Oral capsule
Strengths: 75 mg

Brand: Targretin

Form: Oral capsule
Strengths: 75 mg
Adult dosage (ages 18 years and older)

Your doctor will decide your dose using your body surface area (BSA). This is calculated from your height and weight. It’s measured in squared meters (m2). 

  • Typical starting dose: 300 mg/m2 taken once per day with a meal
  • Dose increases: If you have side effects from this drug, your doctor may decrease your dose to 200 mg/m2 per day and then to 100 mg/m2 per day. Or they may have you temporarily stop taking bexarotene. If your tumor doesn’t respond after 8 weeks of treatment and you’re able to tolerate the 300 mg/m2 dose, your doctor may increase your dose to 400 mg/m2 per day. They’ll monitor you closely.
  • Maximum dose: 400 mg/m2 per day
Child dosage (ages 0–17 years)

This drug hasn’t been studied in children. It shouldn’t be used in people younger than 18 years.

Warnings

For females who can become pregnant: You should start taking your first dose of this drug on the second or third day of a normal menstrual cycle, as instructed by your doctor.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always to speak with your doctor or pharmacist about dosages that are right for you.
Pharmacist's Advice
Healthline Pharmacist Editorial Team

This drug comes with serious risks if you don’t take it as prescribed.

If you stop taking the drug suddenly or don’t take it at all

If you don’t take this drug, your cancer won’t be treated and will get worse.

If you miss doses or don’t take the drug on schedule

Your medication may not work as well or may stop working completely. Your cancer may get worse. For this drug to work well, a certain amount needs to be in your body at all times.

What to do if you miss a dose

Take your dose as soon as you remember. But if you remember just a few hours before your next scheduled dose, take only one dose. Never try to catch up by taking two doses at once. This could result in dangerous side effects.

If you take too much

You could have dangerous levels of the drug in your body. Symptoms of an overdose of this drug can include:

  • neutropenia (low white blood cell levels)
  • lack of energy
  • rash
  • nausea
  • swelling in your legs or arms
  • infection
  • abdominal pain
  • dry skin
  • headache
  • hypothyroidism (low thyroid levels)
  • increase in cholesterol

If you think you’ve taken too much of this drug, call your doctor or local poison control center. If your symptoms are severe, call 9-1-1 or go to the nearest emergency room right away. 

How to tell if the drug is working

Your skin lesions may improve or go away. Your doctor will also do blood tests to check if this drug is working.

This drug is used for long-term treatment.

Important considerations for taking this drug
Take this drug with food Take this drug with food
timing Take this drug at the time(s) recommended by your doctor
storage Store this drug carefully See Details
drug is refillable A prescription for this drug is refillable See Details
Travel Travel See Details
Clinical monitoring Clinical monitoring See Details
Sun sensitivity Sun sensitivity See Details
not usually stocked Not every pharmacy stocks this drug. When filling your prescription, be sure to call ahead
prior authorization required Insurance See Details

Store this drug carefully

  • Store this drug between 36°F and 77°F (2°C and 25°C). Keep it away from light.

A prescription for this drug is refillable

Only one month’s supply should be given to female patients who can become pregnant. This allows for pregnancy testing before the next refill.

Travel

When traveling with your medication:

  • Always carry your medication with you. When flying, never put it into a checked bag. Keep it in your carry-on bag.
  • Don’t worry about airport x-ray machines. They can’t hurt your medication.
  • You may need to show airport staff the pharmacy label for your medication. Always carry the original prescription-labeled box with you.
  • Don’t put this medication in your car’s glove compartment or leave it in the car. Be sure to avoid doing this when the weather is very hot or very cold.

Clinical monitoring

You and your doctor should monitor certain health issues. This can help make sure you stay safe while you take this drug. These issues include:

  • White blood cell count. Your doctor will check your white blood cell count before and during treatment with this drug.
  • Blood fats (cholesterol and triglycerides). Your doctor should check your cholesterol and triglycerides before treatment, at weeks two, three, and four of treatment, and at other times during treatment with this drug.
  • Liver function tests. Your doctor should check your liver function before treatment, at weeks two, three, and four of treatment, and at other times during treatment with this drug.
  • Thyroid function tests. Your doctor should check your thyroid function before starting and during treatment with this drug.
  • Pregnancy tests. If you can become pregnant, your healthcare provider will do a pregnancy test within one week before you start this drug and every month during treatment. This is done to make sure you’re not pregnant.

Sun sensitivity

This drug can make your skin more sensitive to the sun. This increases your risk of sunburn. Stay out of the sun if you can. If you must be in the sun, wear protective clothing and sunscreen.

Insurance

Many insurance companies require a prior authorization for this drug. This means your doctor will need to get approval from your insurance company before your insurance company will pay for the prescription.

Are there any alternatives?

There are other drugs available to treat your condition. Some may be better suited for you than others. Talk to your doctor about other drug options that may work for you.

What does the pill look like?

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How Much Does bexarotene Cost?

Oral capsule

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Content developed in collaboration with University of Illinois-Chicago, Drug Information Group

Medically reviewed by Creighton University, Center for Drug Information and Evidence-Based Practice on December 11, 2015

Disclaimer: Healthline has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.
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