bexarotene (Rx)

Brand and Other Names:Targretin
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 75mg

gel

  • 1%

Cutaneous T-Cell Lymphoma

300 mg/m² PO qDay with food; titrate based on response or toxicity; may increase 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 qWeek up to q6hr

Monitor: WBC, LFTs, lipids, thyroid function

Refractory Mycosis Fungoides/Sezary Syndrome (Off-label)

75-150 mg PO qDay in combination with PUVA; not to exceed 300 mg/day

Renal Impairment

Not studied; use caution

Hepatic Impairment

Not studied; use caution

Safety and efficacy not established

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Interactions

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            >10%

            Oral (CTCL trial)

            • Peripheral edema (11-13%)
            • Headache (30-42%), fever (5-17%), chills (10-13%), insomnia (5-11%)
            • Exfoliative dermatitis (10-28%), rash (16-23%), alopecia (4-12%), dry skin (10-11%)
            • Diarrhea (7-41%), nausea (8-16%), vomiting (4-13%), abdominal pain (4-11%)
            • Bacterial infection (1-13%), flu syndrome (4-13%), infections (13-23%)
            • Leukopenia (17-47%), anemia (6-25%), lactic dehydrogenase increased (7-13%), hypochromic anemia (4-13%)
            • Hyperlipidemia (78-79%), hypercholesteremia (32-62%), hypothyroidism (29-52%)
            • Back pain (2-11%)

            Topical

            • Rash (72%)
            • Pruritus (36%)
            • Pain (30%)
            • Infection (18%)
            • Contact dermatitis (14%)
            • Headache (14%)

            1-10%

            Oral

            • Hemorrhage
            • Hypertension
            • Hypothyroidism
            • Heart failure
            • Tachycardia
            • Acne
            • Depression
            • Pustular rash
            • Sunburn
            • Pharyngitis
            • Rhinitis
            • Arthralgia
            • Blephartis
            • Corneal lesion
            • Renal dysfunction

            Topical

            • Edema (10%)
            • Hyperlipemia (10%)
            • Asthenia (6%)
            • Exfoliative dermatitis (6%)
            • Leukopenia (6%), lymphadenopathy (6%), WBC changes (6%)
            • Cough increased (6%), pharyngitis (6%)
            • Sweating (6%)
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            Warnings

            Black Box Warnings

            Bexarotene is a retinoid

            Retinoids are associated with birth control defects in humans and are contraindicated during pregnancy

            Effective contraception must be in place 1 month before initiation of therapy, during therapy, and for at least 1 month after discontinuation of therapy

            Contraindications

            Hypersensitivity to retinoids

            Pregnancy (use 2 forms of contraception)

            Cautions

            Oral

            • Suppresses TSH levels; may cause hypothyroidism; may require supplementatoin
            • 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 patient
            • Use caution in 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
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            Pregnancy & Lactation

            Pregnancy Category: X

            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, taking into account the importance of the drug to the mother.

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Retinoid X receptor activator, regulates genes that control cell differentiation; induces tumor regression

            Pharmacokinetics

            Half-Life: 7 hr

            Peak Plasma Time: 2 hr

            Protein Bound: >99%

            Metabolism: Liver (CYP3A4)

            Metabolites: 6- & 7- hydroxy- bexarotene, 6- & 7- oxo- bexarotene

            Excretion: Feces (primarily); urine (<1%)

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            bexarotene oral
            -
            75 mg capsule
            bexarotene oral
            -
            75 mg capsule
            bexarotene oral
            -
            75 mg capsule
            bexarotene oral
            -
            75 mg capsule
            bexarotene oral
            -
            75 mg capsule
            bexarotene oral
            -
            75 mg capsule
            Targretin oral
            -
            75 mg capsule

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Select a drug:
            Patient Education
            bexarotene oral

            BEXAROTENE - ORAL

            (bex-AR-oh-teen)

            COMMON BRAND NAME(S): Targretin

            WARNING: This medication can cause severe birth defects if used during pregnancy. Women who are pregnant must not use bexarotene. If pregnancy occurs, notify your doctor right away. You should have a pregnancy test and birth control counseling from your doctor before you start treatment with bexarotene and every month while you are taking the medication. Use 2 effective forms of birth control together (or completely avoid sexual intercourse) starting 1 month before treatment starts, during treatment, and for 1 month after you stop. One of your forms of birth control should be non-hormonal (for example, a barrier method such as condoms/cervical cap/diaphragm, copper coil IUD, or spermicide).Males taking this medication should use a condom during sexual activity with a woman who is pregnant or may become pregnant, continuing until 1 month after their last dose.

            USES: Bexarotene is used to treat skin problems from a certain type of cancer (cutaneous T-cell lymphoma-CTCL). It belongs to a class of drugs called retinoids (vitamin A derivatives). Bexarotene works by slowing or stopping the growth of cells.

            HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start using bexarotene and each time you get a refill. If you have any questions, consult your doctor or pharmacist.Take this medication by mouth with or immediately after a meal as directed by your doctor, usually once daily. The dosage is based on your body size, medical condition, and response to therapy. Swallow the medication whole. Do not crush or chew the medication. Do not use the capsule if it is broken or leaking. If the contents of the capsule touch your skin, immediately wash the area with soap and water and tell your doctor.Do not increase your dose or take this medication more often than prescribed. Your condition will not improve any faster, and the risk of serious side effects may be increased.It may take up to several months of continued use to see a response to treatment. Your dosage may need to be adjusted by your doctor during this time.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the capsules. Learn proper technique for safe handling and disposal of this medicine and its container. Consult your pharmacist.

            SIDE EFFECTS: Headache, tiredness, nausea, vomiting, dry skin, diarrhea, or trouble sleeping may occur. If any of these effects last or get worse, notify your doctor.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This medication can frequently increase the level of "bad" fats (cholesterol/triglyceride) in your blood. Your doctor will order blood tests to measure these fats. If your blood fat levels get too high, your bexarotene dose may need to be lowered or stopped, or you may need to start cholesterol medication.This medication can cause an underactive thyroid (hypothyroidism). Tell your doctor right away if any of these symptoms of low thyroid occur: unusual weight gain, feeling cold, constipation, slow heartbeat, low on energy. Your doctor will order a blood test and may start you on thyroid medication.Tell your doctor right away if you have any serious side effects, including: swelling of the hands/feet, muscle pain/stiffness/cramps, fast/pounding heartbeat, mental/mood changes (such as depression, anxiety, thoughts of suicide), nausea/vomiting that doesn't stop, stomach/abdominal/back pain, dark urine, vision changes, yellowing eyes/skin.This medication can lower the body's ability to fight an infection. Notify your doctor promptly if you develop any signs of an infection such as sore throat that doesn't go away, fever, or chills.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking bexarotene, tell your doctor or pharmacist if you are allergic to it; or to vitamin A-related drugs (other retinoids such as isotretinoin); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: pancreatitis, frequent alcohol use, cataracts, high blood fats (high cholesterol/triglyceride), diabetes, gallbladder disease, liver problems, mental/mood problems (such as depression), thyroid problems (such as hypothyroidism).This medication may make you more sensitive to the sun. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Tell your doctor right away if you get sunburned or have skin blisters/redness.Bexarotene can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.This medication must not be used during pregnancy. If you become pregnant or think you may be pregnant, inform your doctor right away. (See also Warning section.)Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the capsules.It is not known if this drug passes into breast milk. Due to the possible harm to the nursing infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug are: gemfibrozil, tamoxifen, vitamins/supplements that contain vitamin A.This medication may decrease the effectiveness of hormonal birth control such as pills, patch, or ring. This could cause pregnancy. You should use an additional form of reliable birth control while using this medication. (See also Warning section.) Consult your doctor or pharmacist for details.This medication may interfere with certain laboratory tests (including CA-125 levels), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug. Consult your doctor for more details.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.Lab and/or medical tests (such as pregnancy tests, liver/thyroid function, cholesterol/triglyceride levels, white blood count) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

            MISSED DOSE: If you miss a dose, take it with a meal as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store between 36-77 degrees F (2-25 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

            Information last revised December 2022. Copyright(c) 2022 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.