Bexarotene

Bexarotene is a prescription medication indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy.

• Bexarotene is available under the following different brand names: Targretin

Common side effects of Bexarotene include:

• headache
• tiredness
• fatigue
• nausea
• vomiting
• dry skin
• diarrhea
• trouble sleeping
• an increase in fat levels in the blood (blood lipids) such as cholesterol or triglycerides (blood tests will detect this)
• an underactive thyroid (blood tests will detect this)
• blood problems
• weakness or loss of strength
• swelling
• rash
• infections

Serious side effects of Bexarotene include:

• hives
• difficulty breathing
• swelling of the face, lips, tongue, or throat
• blurred vision, eye pain, or seeing halos around lights
• low blood cell counts--fever, chills, tiredness, mouth sores, skin sores, sore throat, cough, pale skin, cold hands and feet, and feeling light-headed or short of breath
• pancreatitis--severe pain in your upper stomach spreading to your back, nausea, and vomiting; or
• signs of underactive thyroid--extreme tiredness, dry skin, constipation, feeling more sensitive to cold temperatures, weight gain

Rare side effects of Bexarotene include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Capsule

• 75 mg

Gel

• 1%

Cutaneous T-cell lymphoma

Adult dosage

• 300 mg/m² orally once a day with food; titrate based on response or toxicity; may increase the dose to 400 mg/m²/day if no response after 8 weeks of therapy
• Topical: Apply to lesions every other day for 1 week initially, then increase every week up to every 6 hours
• Monitor: WBC, LFTs, lipids, thyroid function

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Bexarotene has severe interactions with the following drugs:
  • doravirine
  • lonafarnib
  • mavacamten
• Bexarotene has serious interactions with at least 38 other drugs.
• Bexarotene has moderate interactions with at least 89 other drugs.
• Bexarotene has minor interactions with the following drugs:
  • artemether/lumefantrine
  • darunavir
  • fosphenytoin
  • hydrocortisone
  • insulin aspart
  • insulin detemir
  • insulin glargine
  • insulin glulisine
  • insulin lispro
  • insulin NPH

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Hypersensitivity to retinoids
• Pregnancy (use 2 forms of contraception)

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Bexarotene?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Bexarotene?”

Cautions

• Oral
  • Suppresses TSH levels; may cause hypothyroidism; may require supplementation
  • Neutropenia and leukopenia may occur
  • May induce significant lipid abnormalities in a majority of patients
  • ALT, AST, and bilirubin elevation reported
  • Pancreatitis secondary to hypertriglyceridemia reported
  • Photosensitivity and phototoxicity may occur
  • Evaluate visual abnormalities experienced by the patient
  • Use caution in patients with diabetes mellitus and hepatic impairment
• Topical
  • Do not use occlusive dressings with gel
  • May induce significant lipid abnormalities; use caution in patients with hypertriglyceridemia
  • May cause photosensitization
  • Neutropenia and leukopenia may occur

Pregnancy and Lactation

• Do not use during pregnancy
• Lactation
  • It is not known whether bexarotene is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants from bexarotene, a decision should be made whether to discontinue nursing or to discontinue the drug, considering the importance of the drug to the mother