bexarotene (Rx)

Brand and Other Names:Targretin
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 75mg

gel

  • 1%
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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

Interaction Checker

and bexarotene

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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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

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            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.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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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.