Bexarotene
Trade Name:
Targretin
Type of Drug:
Bexarotene is a retinoid used in molecular targeted therapy. A retinoid is a naturally occuring substance in the body that helps to regulate, or control, the work of genes to help cells grow and divide.
How Drug Works:
Bexarotene “turns on” certain retinoid receptors on the cancer cell. The “turned on” receptor works with other substances to control cancer cell growth and division. Bexarotene capsules are used to treat skin lesions due to cutaneous T-cell lymphoma that has not responded to prior systemic treatment. The 1% topical gel is used for treatment of early stage skin lesions that no longer respond to other therapies in patients with cutaneous T-cell lymphoma.
How Drug Is Given:
Bexarotene is taken as a capsule by mouth with a meal. The dose depends on your size. To start, you will take a capsule daily until a response is seen, for up to 97 weeks. 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. Keep the medicine in a tightly closed container and out of the reach of children and pets. Also, keep the container out of heat, light, and humidity. Bexarotene can also be given as a gel on skin lesions. The dose is just enough to cover the lesion.
How Should I Take This Drug?
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.
Read the following information. If you do not understand it or if any of it causes you special concern, check with your doctor.

Before taking this drug, tell your doctor:

  • If you are trying to become pregnant, are pregnant, or breastfeeding. 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 some kind of birth control. However, do not use oral contraceptives (“the pill”) without checking with your doctor.

  • If you think you may want to have children in the future. Many chemotherapy drugs can cause sterility.

  • If you have any of the following medical problems: chickenpox or exposure to chickenpox, gout, heart disease, congestive heart failure, shingles, kidney stones, liver disease, or other forms of cancer.

  • If you are taking any other prescription or over-the-counter drugs, including vitamins and herbals.
Should I avoid any other medicines, foods, alcohol, and/or activities?
Your prescription and nonprescription medicines may interact with other drugs, causing harm. Certain foods or alcohol can also interact with drug products. Never begin taking a new medicine—prescription or nonprescription—without asking your doctor or nurse if it will interact with alcohol, food, or other medicines. Some drug products can cause drowsiness and affect activities such as driving.
Precautions:
You must AVOID direct sunlight and artificial ultraviolet (UV) light while you are taking bexarotene. UV light exposure can cause a severe sunburn.
The drug may interact with other medicines. Make sure you tell your doctor about all other medicines you are taking.
DO NOT take gemfibrozil with bexarotene as it can increase blood levels of bexarotene. Also, avoid eating grapefruit when taking the capsules.
Bexarotene may change some of your blood test results: 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. All these levels will be checked before you start bexarotene capsules.
Women of childbearing age taking the capsules should use effective contraception. Bexarotene affects the unborn fetus, and pregnancy must be avoided. Pregnancy tests should be negative before starting therapy.
Nursing mothers should not use bexarotene.
Bexarotene capsules should be used cautiously if at all in patients who have had allergic reactions to other retinoids and patients with liver problems. If you have pancreatitis (inflammation of the pancreas), or uncontrolled blood lipids or cholesterol in the blood, uncontrolled diabetes, or are taking drugs that may cause pancreatitis or increased blood lipids, you should not take this medicine. Talk with your doctor if you have any questions.
Bexarotene causes increased lipid blood levels in most patients, and this blood level needs to be monitored closely during therapy.
Bexarotene capsules may cause cataracts. Make sure that you tell your doctor right away if your vision changes during therapy.
If you are taking a vitamin A supplement, DO NOT take more than 15,000 IU/day as this will increase bexarotene (capsule) side effects.
Tell all the doctors, dentists, and pharmacists you visit that you are taking this drug.
  • Most of the following side effects probably will not occur.
  • Your doctor or nurse will want to discuss specific care instructions with you.
  • They can help you understand these side effects and help you deal with them.
Side Effects:
More Common Side Effects
  • Increased blood lipid levels (fasting triglycerides, cholesterol)
  • Headache
  • Itching (gel)
  • Decreased blood HDL level
  • Rash (gel)
  • Low thyroid function
  • Pain at application site (gel)
  • Diarrhea
Less Common Side Effects
  • Weakness or listlessness
  • Flu-like symptoms
  • Decreased white blood cells with increased risk of infection
  • Back pain
  • Rash
  • Abdominal pain
  • Peeling of skin
  • Fever and chills
  • Hair loss
  • Difficulty sleeping
  • Swelling of the ankles
Rare Side Effects
  • Increased blood level of liver function tests
  • Nausea
  • Vomiting
  • Pancreatitis
  • Loss of appetite
Side Effects / Symptoms of the Drug

You may have to take medicine to decrease your blood lipid levels. Your doctor will monitor your blood values closely. Changes in blood lipid level and thyroid function will go back to normal after the treatment is finished.

Report signs/symptoms of hypothyroidism (weight gain, tiredness, slowed thinking, skin dryness, constipation, or joint pain/stiffness).

Report fever, persistent cough, burning on urination, or other signs/symptoms of infection.

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

Report nausea, vomiting, or appetite loss.
Other side effects not listed above can also occur in some patients. Tell your doctor or nurse if you develop any problems.
FDA Approval: This drug is approved for cancer treatment.