Bexarotene – Uses, Dosage, Side Effects, Interactions

Use in Cancer

Bexarotene is approved to treat:

• Skin problems caused by cutaneous T-cell lymphoma that cannot be treated or that did not respond to other treatments.

Bexarotene is also being studied in the treatment of other types of cancer.

Contraindications

• Hypersensitivity to the active substance or to any of the excipients in the preparation(s).
• Pregnancy and lactation
• Women of child-bearing potential without effective birth-control? measures
• History of pancreatitis?
• Uncontrolled hypercholesterolemia
• Uncontrolled hypertriglyceridemia
• Hypervitaminosis A
• Uncontrolled thyroid disease
• Hepatic insufficiency
• Ongoing systemic infection?
• a condition with low thyroid hormone levels
• poor control of diabetes?
• high amount of triglyceride in the blood
• low levels of white blood cells
• alcoholism
• clouding of the lens of the eye called cataracts
• biliary and gallbladder? problem
• acute inflammation? of the pancreas?
• abnormal liver function tests
• pregnancy
• a patient who is producing milk and breastfeeding

Dosage?

Strengths: 75 mg

Cutaneous T-cell Lymphoma

• 300 mg/m2/day orally once a day with a meal
• Duration of Therapy: This drug should be continued as long as the patient is a deriving benefits. In clinical trials with CTCL patients, this drug was administered for up to 118 weeks.
• If there is no tumor response after 8 weeks of treatment and the initial dose was well-tolerated, the dose may be escalated to 400 mg/m2/day with careful monitoring?.

Dose Adjustments

If Toxicity Occurs:

• Reduce the dose to 200 mg/m2/day than to 100 mg/m2/day, or temporarily suspend treatment.
• Carefully readjust the dose upward when toxicity is controlled.

If Fasting Triglycerides are Elevated or Become Elevated During Treatment:

• Institute antilipemic therapy.
• If necessary, reduce the dose to 200 mg/m2/day then to 100 mg/m2/day, or discontinue treatment.

Side Effects

The Most Common

• headache?
• weakness?
• tiredness
• increased sensitivity to cold
• increase in weight
• depression
• joint or muscle pain?
• thin, brittle hair or fingernails
• constipation?
• rash?
• dry skin
• redness, scaling, or itching? of the skin
• hair loss
• swelling? of ankles, feet, and legs
• difficulty falling asleep or staying asleep
• nausea?
• vomiting?
• diarrhea
• sudden or ongoing back or stomach pain
• severe and ongoing nausea and vomiting
• fever, sore throat, chills, or other signs of infection
• changes in vision

More Common

• skin reactions (mostly itchiness and rashes),
• leucopenia,
• headache,
• weakness,
• thyroid anomalies (which seem to be mediated by RXR-mediated downregulation of thyroid stimulating hormone) and
• blood lipid anomalies such as hypercholesterolemia (high blood cholesterol) and
• hyperlipidemia,
• hypothyroidism.

Rare

• 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, 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.
• low blood cell counts;
• headache, weakness
• nausea, stomach pain;
• rash, dry skin; or
• swelling in your hands or feet.

Drug Interactions

Pregnancy and Lactation

US FDA pregnancy category: Not Assigned

Pregnancy

The US FDA has amended the pregnancy labeling rule for prescription drug products to require labeling that includes a summary of risk, a discussion of the data supporting that summary, and relevant information to help healthcare providers make prescribing decisions and counsel women about the use of drugs during pregnancy. Pregnancy categories A, B, C, D, and X are being phased out.

Lactation

Breastfeeding should be discontinued during treatment. Excreted into human milk: Unknown
Excreted into animal milk: Data not available

References