Bexarotene - Uses, Dosage, Side Effects, Interactions - Rxharun

Bexarotene – Uses, Dosage, Side Effects, Interactions


  • Used orally for the treatment of skin manifestations of cutaneous T-cell lymphoma (CTCL) in patients who are refractory to at least one prior systemic therapy. Also used topically for the treatment of skin lesions in early (stage IA and IB) CTCL in patients who experience refractory or persistent disease with the use of other therapies or are intolerant of other therapies.
  • Targretin capsules are indicated for the treatment of skin manifestations of advanced-stage cutaneous T-cell lymphoma (CTCL) patients refractory to at least one systemic treatment.
  • Refractory peripheral cutaneous T-cell lymphoma
  • Bexarotene is indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in people who are refractory to at least one prior systemic therapy (oral) and for the topical treatment of cutaneous lesions in patients with CTCL who have refractory or persistent disease after other therapies or who have not tolerated other therapies (topical)

Use in Cancer

Bexarotene is approved to treat:

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


  • 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


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.


  • 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

You Might Also Read  Duvelisib - Uses, Dosage, Side Effects, Interaction
You Might Also Read  Desvenlafaxine; Uses, Dosage, Side Effects, Interactions
You Might Also Read  Clobetasol Propionate Uses - Indications, Contraindication

Pregnancy and Lactation

US FDA pregnancy category: Not Assigned


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.


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

How should this medicine be used?

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. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take bexarotene exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Swallow the capsules whole; do not chew the capsules or dissolve them in liquid or in your mouth. If you are unable to swallow the capsules whole, talk to your doctor.

Bexarotene may be harmful if it gets on the skin. Do not touch the capsules or powder from the capsules if they are broken or leaking. If the powder from a broken capsule gets on your skin, wash the area with soap and water immediately and call your doctor.

Your doctor will start you on an average dose of bexarotene and may decrease your dose if you experience side effects or increase your dose if your condition does not improve.

It may take several months or longer before you notice the full benefit of bexarotene. Do not stop taking bexarotene without talking to your doctor.

Ask your pharmacist or doctor for a copy of the manufacturer’s information for the patient.

What special precautions should I follow?

Before taking bexarotene,

  • tell your doctor and pharmacist if you are allergic to bexarotene; or any other retinoid, such as acitretin (Soriatane), etretinate (Tegison), isotretinoin (Accutane), or tretinoin (Vesanoid); or any other medications.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: 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); and vitamin A. Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with bexarotene, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
  • 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 of 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.


  8. Guide to Pharmacology Target Classification
    The data from CAS Common Chemistry is provided under a CC-BY-NC 4.0 license, unless otherwise stated.
  10. ChemIDplus Chemical Information Classification
  11. CompTox Chemicals Dashboard Chemical Lists
  12. 4-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)ethenyl]benzoic acid
    4-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)ethenyl]benzoic acid
  13. NCI Thesaurus Tree
    Data: CC-BY 4.0; Code (hosted by ECI, LCSB): Artistic-2.0
    NORMAN Suspect List Exchange Classification
    The content of the MoNA database is licensed under CC BY 4.0.
  16. PubChem
    Academic users may freely use the KEGG website. Non-academic use of KEGG generally requires a commercial license
    Therapeutic category of drugs in Japan
    Anatomical Therapeutic Chemical (ATC) classification
    Target-based classification of drugs
  18. NCBI

Consumer Information – TrustArc The Leader in Privacy Management SoftwareLooking online for info on your child's health? Here are some tipsJanja Kristan - Chief Administrative Officer - AACI | LinkedIn
Translate »
Shop From Rx Harun