Bexarotene

Bexarotene is a prescription medication used to treat cutaneous T-cell lymphoma (CTCL) in people whose disease could not be treated successfully with at least one other medication. CTCL is a type of skin cancer. Bexarotene belongs to a group of medications called retinoids. These work by stopping the growth of cancer cells.

Bexarotene comes as a capsule to take by mouth. It is usually taken once a day with food. Take bexarotene at around the same time every day.

This medication also comes as a topical gel to be applied apply to the skin. It is usually applied once every other day at first and gradually applied more frequently up to 2 to 4 times a day. Use bexarotene gel at around the same times every day.

Common side effects of bexarotene capsules include headache, weakness, rash, and nausea.

Common side effects of bexarotene gel include itching, redness, pain, and burning at site of application.

Oral/Topical:

Bexarotene is used to treat cutaneous T-cell lymphoma (CTCL, a type of skin cancer) in people whose disease could not be treated successfully with at least one other medication.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Bexarotene may be found in some form under the following brand names:

• Targretin

Oral:

Common side effects of bexarotene capsules include the following:

• decreased thyroid activity
• headache
• weakness
• rash
• low white blood cell counts
• anemia
• nausea
• infection
• swelling
• stomach pain
• dry skin

Topical:

Common side effects of bexarotene gel include the following:

• itching
• redness, burning, irritation, or scaling of the skin
• rash
• pain
• sweating
• weakness
• headache
• swelling of the arms, hands, feet, ankles, or lower legs

This is not a complete list of this medication’s side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• amiodarone (Cordarone)
• certain antifungals such as ketoconazole (Nizoral) and itraconazole (Sporanox)
• cimetidine (Tagamet)
• clarithromycin (Biaxin)
• diltiazem (Cardizem)
• erythromycin (E.E.S., E-Mycin, Erythrocin)
• fluvoxamine
• gemfibrozil (Lopid)
• HIV protease inhibitors such as indinavir (Crixivan), nelfinavir (Viracept), and ritonavir (Norvir, in Kaletra)
• insulin and oral medications for diabetes
• nefazodone
• phenobarbital
• phenytoin (Dilantin)
• rifampin (Rifadin, Rimactane)
• tamoxifen (Nolvadex)
• verapamil (Calan)
• vitamin A
• alcohol

This is not a complete list of all drug interactions. Ask your doctor or pharmacist for more information.

Do not take this medication if you are

• allergic to bexarotene or to any of its ingredients
• are pregnant

Oral:

• Your doctor will want to conduct lab tests to monitor for liver dysfunction.
• This medication may cause pancreatitis (inflammation of the pancreas).Those who have risk factors for pancreatitis (e.g., prior pancreatitis, uncontrolled hyperlipidemia, excessive alcohol consumption, uncontrolled diabetes mellitus, biliary tract disease, and medications known to increase triglyceride levels or to be associated with pancreatic toxicity) should generally not be treated with bexarotene capsules.
• Bexarotene may increase the levels of cholesterol and other fats in your blood and may stop your thyroid gland from working normally. Your doctor will monitor you carefully to see whether you are experiencing either of these side effects. If you experience either of these side effects, your doctor may prescribe another medication to control the side effect while you are taking bexarotene.

Topical:

• Because vitamin A in large doses may cause some side effects which are similar to those seen in patients applying bexarotene gel, do not take more than the recommended daily dietary allowance of vitamin A (4000 to 5000 International Units). If you take vitamins, check the label to see how much vitamin A they contain. If you are not sure, ask your doctor or pharmacist.
• Bexarotene gel should be used with caution in patients with a known hypersensitivity to other retinoids.
  • Retinoids include acitretin (Soriatane), etretinate (Tegison), isotretinoin (Accutane), tretinoin (Vesanoid) or any other medication
• Bexarotene gel is for external use only.

Grapefruit and grapefruit juice may interact with this medication and can lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Before taking bexarotene,

• tell your doctor and pharmacist if you are allergic to bexarotene or to any other retinoid, such as acitretin (Soriatane), etretinate (Tegison), isotretinoin (Accutane), tretinoin (Vesanoid) or any other medication
• tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take
• tell your doctor if you drink or have ever drunk large amounts of alcohol. Also tell your doctor if you have or have ever had pancreatitis; high levels of cholesterol and other fatty substances in the blood; diabetes; cataracts; or gall bladder, thyroid, kidney, or liver disease.
• tell your doctor if you are breastfeeding
• ask your doctor about the safe use of alcoholic beverages while you are taking bexarotene. Alcohol can make the side effects from bexarotene worse.
• plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Bexarotene may make your skin sensitive to sunlight.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category X.

• For female patients:
  • If you can become pregnant, you will need to avoid becoming pregnant during your treatment with bexarotene. You must use two acceptable forms of birth control for 1 month before you begin to take bexarotene, at all times during your treatment, and for 1 month after your treatment. Your doctor will tell you which forms of birth control are acceptable. Bexarotene may decrease the effectiveness of hormonal contraceptives (birth control pills, patches, rings, implants, and injections), so it is especially important to use a second form of birth control along with this type of contraceptive.
  • You will begin to take bexarotene on the second or third day of your menstrual period. You must have a negative pregnancy test within 1 week of the start of your treatment and every month during your treatment. After each negative pregnancy test, you will be given only 1 month's supply of bexarotene.
  • Stop taking bexarotene and call your doctor right away if you think you are pregnant, you miss a menstrual period, or you have sex without using two forms of birth control.
• For male patients:
  • You must use a condom every time you have sexual contact with a female who is pregnant or able to become pregnant while you are taking bexarotene and for 1 month after your treatment. Call your doctor if your partner becomes pregnant during this time.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if bexarotene crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using this medication.

Take this medication exactly as prescribed.

Oral:

• Bexarotene comes as a capsule to take by mouth. It is usually taken once a day with food. Take bexarotene at around the same time every day.

Topical:

• Do NOT apply the gel on or near mucosal surfaces of the body such as eyes, nostrils, mouth, lips, vagina, tip of the penis, rectum, or anus.
• Do NOT use insect repellents containing DEET (N,N-diethyl-m-toluamide) or other products containing DEET while using bexarotene gel.
• How to Apply
  • Apply bexarotene gel to your CTCL lesions using a clean washed finger. Place a generous coating of gel over the entire surface of each lesion. You should not apply gel to the healthy skin around the lesion. The extra effort you take in carefully applying the gel only to the area of the CTCL lesion will help to lessen any irritation or redness that may occur. Proper application should leave some gel visible on the surface of the lesion when you are finished with the application.
  • Immediately following application, wipe the finger(s) you have used to apply the gel with a disposable tissue and wash your hands using soap and water.
  • Allow five (5) to ten (10) minutes for the gel to dry before covering a treated area with clothing.
  • A mild non-deodorant soap is recommended when bathing or showering. If you apply bexarotene gel after your shower or bath, you should wait 20 minutes before application.
• When to Apply
  • Bexarotene gel should be applied at an initial frequency of once every other day for the first week. The frequency of application should then be increased as tolerated at weekly intervals to once daily, then twice daily, then three times daily, and finally four times daily. Your health care provider may instruct you to apply bexarotene gel at a different frequency.
• What shoud I avoid?
  • You should avoid applying bexarotene gel to areas of healthy skin around a CTCL lesion. Exposure of healthy skin to bexarotene gel may cause unnecessary irritation or redness.
  • You should avoid showering, bathing, or swimming until at least three (3) hours after any application, if possible.
  • You should avoid covering the CTCL lesions treated with bexarotene gel with any bandage or material other than loose clothing.
  • You should avoid prolonged exposure of the treated area to sunlight or other ultraviolet (UV) light (such as tanning lamps).
  • You should avoid the use of other topical products on your treated CTCL lesions.
  • You should avoid scratching the treated areas.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.
The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication
• your weight
• your height
• your age
• your gender

Oral:

• The recommended dose range is 100 to 400 mg/m²/day. Bexarotene capsules should be taken as a single daily dose with a meal.

Topical:

• Bexarotene gel should be initially applied once every other day for the first week.
• The application frequency should be increased at weekly intervals to once daily, then twice daily, then three times daily and finally four times daily according to tolerance.
• Sufficient gel should be applied to cover the lesion with a generous coating.

If you take too much this medication, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If this medication is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

Oral:

• Store capsules at room temperature.
• Avoid exposing capsules to high temperatures and humidity after the bottle is opened.
• Protect capsules from light.
• Keep this and all medications out of the reach of children.

Topical:

• This product contains alcohol an should be kept away from open flame.
• Bexarotene gel takes time to work. In clinical trials, some patients began to respond as early as 4 weeks, but most patients did not experience their best response until 48 to 62 weeks of treatment. Do not stop treatment at the first sign of improvement. Continue to use bexarotene gel as instructed by your health care provider.
• The opening of the bexarotene gel tube is covered by a metal safety seal. If this seal has been punctured or is not visible when you first open the package, DO NOT USE this tube and promptly return the product to your pharmacy or place of purchase.
• To open, use the pointed portion of the cap to puncture the metal safety seal.
• Always use the cap to close the tube tightly after each use.
• Store at room temperature. Keep away from heat or flame.
• The gel should not be used after the expiration date printed on the tube.
• Keep this and all medications out of the reach of children.

Oral:

Bexarotene capsules are a member of the retinoid class of drugs that is associated with birth defects in humans. Bexarotene capsules also caused birth defects when administered orally to pregnant rats. Bexarotene capsules must not be administered to a pregnant woman.