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    Tools & Reference

    bexarotene (Rx)

    Brand and Other Names:Targretin
    • Print

    Dosing & Uses

    AdultPediatric

    Dosage Forms & Strengths

    capsule

    • 75mg

    Cutaneous T-Cell Lymphoma

    300 mg/m² PO once daily with food; titrate based on response or toxicity; may increase to 400 mg/m²/day if no response after 8 weeks of therapy  

    Monitor: WBC, LFTs, lipids, thyroid function

    Refractory Mycosis Fungoides/Sezary Syndrome (Off-label)

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

    Dosage Modifications

    Renal impairment

    • No studies conducted
    • There is in vitro evidence of extensive hepatic contribution to bexarotene elimination, hepatic impairment would be expected to lead to greatly decreased clearance

    Hepatic impairment

    • No studies conducted

    • There is in vitro evidence of extensive hepatic contribution to bexarotene elimination, hepatic impairment would be expected to lead to greatly decreased clearance

    Dosing Considerations

    Females of reproductive potential

    • Obtain pregnancy test with sensitivity of ≥50 mIU/L at least 1 week before initiating therapy and repeat at monthly intervals while patient remains on bexarotene gel
    • Initiate therapy on 2nd or 3rd day of a normal menstrual period
    • Do not dispense more than a 1 month supply so that results of pregnancy testing can be assessed and counseling regarding avoidance of pregnancy and birth defects can be reinforced

    Safety and efficacy not established

    Next:

    Interactions

    Interaction Checker

    and bexarotene

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      Contraindicated

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          Significant - Monitor Closely

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               activity indicator 

              Contraindicated (2)

              • lonafarnib

                bexarotene will decrease the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lonafarnib is a sensitive CYP3A4 substrate. Coadministration with strong or moderate CYP3A4 inducers is contraindicated.

              • mavacamten

                bexarotene will decrease the level or effect of mavacamten by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

              Serious (41)

              • aminolevulinic acid oral

                aminolevulinic acid oral, bexarotene. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • aminolevulinic acid topical

                bexarotene, aminolevulinic acid topical. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Each drug may increase the photosensitizing effect of the other.

              • atrasentan

                bexarotene decreases levels of atrasentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong or moderate CYP3A inducers is expected to decrease atrasentan systemic exposure, which may decrease efficacy. .

              • avapritinib

                bexarotene will decrease the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • capivasertib

                bexarotene will decrease the level or effect of capivasertib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong or moderate CYP3A inducers decrease capivasertib exposure, which may reduce efficacy.

              • daridorexant

                bexarotene will decrease the level or effect of daridorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • elacestrant

                bexarotene will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • etrasimod

                etrasimod, bexarotene. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Risk of additive immune system effects with etrasimod has not been studied in combination with antineoplastic, immune-modulating, or noncorticosteroid immunosuppressive therapies. Avoid coadministration during and in the weeks following administration of etrasimod.

              • fedratinib

                bexarotene will decrease the level or effect of fedratinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Effect of coadministering a moderate CYP3A4 inducer with fedratinib has not been studied.

              • finerenone

                bexarotene will decrease the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • fruquintinib

                bexarotene will decrease the level or effect of fruquintinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with moderate CYP3A4 inducers is unavoidable, continue to administer fruquintinib at recommended dosage.

              • ganaxolone

                bexarotene will decrease the level or effect of ganaxolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of ganaxolone with moderate or strong CYP3A4 inducers. If coadministration unavoidable, consider increasing ganaxolone dose; however, do not exceed maximum daily dose for weight.

              • lefamulin

                bexarotene will decrease the level or effect of lefamulin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of lefamulin with strong or moderate CYP3A inducers unless the benefit outweighs risks. Monitor for reduced efficacy.

              • lemborexant

                bexarotene will decrease the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • leniolisib

                bexarotene will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • lorlatinib

                bexarotene will decrease the level or effect of lorlatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid use of lorlatinib with moderate CYP3A inducers. If unable to avoid, monitor ALT, AST, and bilirubin as recommended.

              • lumateperone

                bexarotene will decrease the level or effect of lumateperone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • methyl aminolevulinate

                bexarotene, methyl aminolevulinate. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Each drug may increase the photosensitizing effect of the other.

              • mitapivat

                bexarotene decreases levels of mitapivat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Consider alternant therapies that are not moderate CYP3A inducers during treatment with mitapivat. If unable to avoid coadministration, monitor Hb and titrate beyond 50 mg BID, if necessary, but do not exceed mitapivat dose of 100 mg BID. .

              • nirogacestat

                bexarotene will decrease the level or effect of nirogacestat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • olutasidenib

                bexarotene will decrease the level or effect of olutasidenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong or moderate CYP3A inducers decrease olutasidenib (a CYP3A4 substrate) plasma concentrations and efficacy.

              • omadacycline

                bexarotene increases toxicity of omadacycline by Mechanism: unknown. Avoid or Use Alternate Drug. Concomitant use of oral retinoids with tetracyclines may increase risk of pseudotumor cerebri/intracranial hypertension. .

              • omaveloxolone

                bexarotene will decrease the level or effect of omaveloxolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • palifermin

                palifermin increases toxicity of bexarotene by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.

              • palovarotene

                bexarotene will decrease the level or effect of palovarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                bexarotene, palovarotene. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Vitamin A in doses higher than the recommended daily allowance and/or other oral retinoids coadministered with palovarotene increases risk of hypervitaminosis A. .

              • pemigatinib

                bexarotene will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • praziquantel

                bexarotene will decrease the level or effect of praziquantel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • pretomanid

                bexarotene will decrease the level or effect of pretomanid by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. CYP3A4 substrate. Avoid coadministration of strong or moderate CYP3A4 inducers.

              • quizartinib

                bexarotene will decrease the level or effect of quizartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • repotrectinib

                bexarotene will decrease the level or effect of repotrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • rimegepant

                bexarotene will decrease the level or effect of rimegepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • ropeginterferon alfa 2b

                ropeginterferon alfa 2b, bexarotene. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.

              • sarecycline

                bexarotene increases toxicity of sarecycline by Mechanism: unknown. Avoid or Use Alternate Drug. Concomitant use of oral retinoids with tetracyclines may increase risk of pseudotumor cerebri/intracranial hypertension. .

              • siponimod

                bexarotene will decrease the level or effect of siponimod by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of siponimod with a drug that causes moderate CYP2C9 plus a moderate or strong CYP3A4 inducer is not recommended. Coadministration with moderate or strong CYP3A4 inducers alone is not recommended for patients with CYP2C9*1/*3 and*2/*3 genotype.

              • sonrotoclax

                bexarotene decreases levels of sonrotoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. May reduce effectiveness of therapy.

              • suzetrigine

                bexarotene decreases levels of suzetrigine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of suzetrigine with strong or moderate CYP3A inducers.

              • vanzacaftor/tezacaftor/deutivacaftor

                bexarotene decreases levels of vanzacaftor/tezacaftor/deutivacaftor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of vanzacaftor/tezacaftor/deutivacaftor with strong or moderate CYP3A inducers.

              • voclosporin

                bexarotene will decrease the level or effect of voclosporin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • vonoprazan

                bexarotene will decrease the level or effect of vonoprazan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • zanubrutinib

                bexarotene will decrease the level or effect of zanubrutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of zanubrutinib (a CYP3A4 substrate) with moderate CYP3A4 inducers. If unavoidable, increase zanubrutinib dose to 320 mg PO BID. After discontinuing the CYP3A4 inducer, resume previous dose of zanubrutinib.

              • zuranolone

                bexarotene will decrease the level or effect of zuranolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              Monitor Closely (83)

              • alpelisib

                bexarotene will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • aprepitant

                aprepitant will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Altered bexarotene serum concentrations may occur, leading to either an increased risk of bexarotene-related adverse reactions or a risk of decreased bexarotene efficacy.

              • atazanavir

                atazanavir will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • atogepant

                bexarotene decreases levels of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Modify atogepant dose if coadministered with a weak CYP3A4 inducer (see Dosage Modifications).

              • axitinib

                bexarotene decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • baxdrostat

                baxdrostat decreases levels of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor the therapeutic effect of this drug more frequently when concomitantly used with strong or moderate CYP3A inducers.

              • belumosudil

                bexarotene will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • bosentan

                bosentan will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • carbamazepine

                carbamazepine will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • cholera vaccine

                bexarotene decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.

              • cimetidine

                cimetidine will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • clarithromycin

                clarithromycin will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • conivaptan

                conivaptan will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Upon completion or discontinuation of conivaptan, allow at least 7 days before initiating therapy with CYP3A4 substrates.

              • crinecerfont

                bexarotene decreases levels of crinecerfont by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase crinecerfont evening dose 2-fold when coadministered with a moderate CYP3A4 inducer. Do not increase crinecerfont morning dose. .

              • cyclosporine

                cyclosporine will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • dasatinib

                dasatinib will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • dexamethasone

                dexamethasone will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • diazepam buccal

                bexarotene will decrease the level or effect of diazepam buccal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Strong or moderate CYP3A4 inducers may increase rate of diazepam elimination; therefore, efficacy of diazepam may be decreased.

              • diazepam intranasal

                bexarotene will decrease the level or effect of diazepam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Strong or moderate CYP3A4 inducers may increase rate of diazepam elimination; therefore, efficacy of diazepam may be decreased.

              • dienogest/estradiol valerate

                bexarotene will decrease the level or effect of dienogest/estradiol valerate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Advise women to use alternative method of contraception or back-up method when moderate or weak enzyme inducer is used with combination contraceptives. Back-up contraception should be continued for 28 days after discontinuing medication to ensure contraceptive reliability.

              • elagolix

                bexarotene will decrease the level or effect of elagolix by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • erdafitinib

                bexarotene will decrease the level or effect of erdafitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If a moderate CYP3A4 inducer must be coadministered, administer 8-mg/day dose initially, with potential to increase to 9 mg/day based on serum phosphate levels on Days 14-21 and tolerability. If a moderate CYP3A4 inducer must be coadministered after the initial dose increase period based on serum phosphate levels and tolerability, increase erdafitinib dose up to 9 mg. When a moderate inducer discontinued, continue erdafitinib at same dose, in absence of drug-related toxicity.

              • erythromycin base

                erythromycin base will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • erythromycin ethylsuccinate

                erythromycin ethylsuccinate will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • erythromycin lactobionate

                erythromycin lactobionate will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • erythromycin stearate

                erythromycin stearate will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • eslicarbazepine acetate

                eslicarbazepine acetate will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • etravirine

                etravirine will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • fluconazole

                fluconazole will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • fluvoxamine

                fluvoxamine will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • fosamprenavir

                fosamprenavir will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • fosaprepitant

                fosaprepitant will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Altered bexarotene serum concentrations may occur, leading to either an increased risk of bexarotene-related adverse reactions or a risk of decreased bexarotene efficacy.

              • gemfibrozil

                gemfibrozil increases levels of bexarotene by unspecified interaction mechanism. Use Caution/Monitor.

              • glimepiride

                bexarotene increases effects of glimepiride by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • glipizide

                bexarotene increases effects of glipizide by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • glyburide

                bexarotene increases effects of glyburide by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • grapefruit

                grapefruit will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • griseofulvin

                griseofulvin will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ifosfamide

                bexarotene increases toxicity of ifosfamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. CYP3A4 inducers may increase the metabolism of ifosfamide to its active alkylating metabolites. CYP3A4 inducers may increase the formation of the neurotoxic/nephrotoxic ifosfamide metabolite, chloroacetaldehyde. Closely monitor patients taking ifosfamide with CYP3A4 inducers for toxicities and consider dose adjustment.

              • insulin regular human

                bexarotene increases effects of insulin regular human by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • isavuconazonium sulfate

                bexarotene will decrease the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • isoniazid

                isoniazid will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • itraconazole

                itraconazole will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ketoconazole

                ketoconazole will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • lapatinib

                lapatinib will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • letermovir

                letermovir increases levels of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • levoketoconazole

                levoketoconazole will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • linagliptin

                bexarotene will increase the level or effect of linagliptin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Use of alternative treatments is strongly recommended when linagliptin is to be administered with a CYP3A4 inducer

              • maraviroc

                bexarotene will decrease the level or effect of maraviroc by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nateglinide

                bexarotene increases effects of nateglinide by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • nefazodone

                nefazodone will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nelfinavir

                nelfinavir will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nevirapine

                nevirapine will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nilotinib

                nilotinib will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • norgestrel

                bexarotene will decrease the level or effect of norgestrel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Moderate CYP3A4 inducers may decrease progestin concentration; consider use of additional barrier methods

              • pentobarbital

                pentobarbital will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • phenobarbital

                phenobarbital will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • phenytoin

                phenytoin will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • pioglitazone

                bexarotene increases effects of pioglitazone by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • ponesimod

                ponesimod and bexarotene both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

              • posaconazole

                posaconazole will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • repaglinide

                bexarotene increases effects of repaglinide by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • ribociclib

                bexarotene will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • rifabutin

                rifabutin will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • rifampin

                rifampin will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • rifapentine

                rifapentine will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ripretinib

                bexarotene will decrease the level or effect of ripretinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If coadministration cannot be avoided, increase dosing frequency from recommended dose of 150 mg once daily to 150 mg twice daily during co-administration period; monitor for clinical response and tolerability

              • ritonavir

                ritonavir will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • rosiglitazone

                bexarotene increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • saxagliptin

                bexarotene increases effects of saxagliptin by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • siponimod

                siponimod and bexarotene both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

              • sitagliptin

                bexarotene increases effects of sitagliptin by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • St John's Wort

                St John's Wort will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • stiripentol

                bexarotene will decrease the level or effect of stiripentol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor closely if stiripentol is coadministered with a moderate CYP3A4 inducer.

              • sufentanil SL

                bexarotene decreases effects of sufentanil SL by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of CYP3A4 inducers may decrease sufentanil levels and efficacy, possibly precipitating withdrawal syndrome in patients who have developed physical dependence to sufentanil. Discontinuation of concomitantly used CYP3A4 inducers may increase sufentanil plasma concentration.

              • tinidazole

                bexarotene will decrease the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • tipranavir

                bexarotene will decrease the level or effect of tipranavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Use alternatives if available.

                tipranavir increases levels of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity. Use alternatives if available. .

              • tivozanib

                bexarotene will decrease the level or effect of tivozanib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ubrogepant

                bexarotene will decrease the level or effect of ubrogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Dose adjustment is recommended with concomitant use of ubrogepant and moderate and weak CYP3A4 inducers. (see Dosage Modifications)

              • vildagliptin

                bexarotene increases effects of vildagliptin by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.

              • vitamin A

                bexarotene increases toxicity of vitamin A by pharmacodynamic synergism. Use Caution/Monitor. (Vitamin A) Additive retinoid effects. Avoid consuming vitamin-A containing supplements in amounts exceeding FDA recommended daily allowance.

              • voriconazole

                voriconazole will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • warfarin

                bexarotene will decrease the level or effect of warfarin by Other (see comment). Use Caution/Monitor. Warfarin's less potent R-enantiomer is metabolized in part by CYP3A4 (and also CYP1A2 and CYP2C19). Monitor INR more frequently if coadministered with inducers of these isoenzymes and adjust warfarin dose if needed.

              Minor (10)

              • artemether/lumefantrine

                artemether/lumefantrine will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

              • darunavir

                darunavir will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

              • fosphenytoin

                fosphenytoin will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

              • hydrocortisone

                hydrocortisone will decrease the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

              • insulin aspart

                bexarotene increases effects of insulin aspart by pharmacodynamic synergism. Minor/Significance Unknown.

              • insulin detemir

                bexarotene increases effects of insulin detemir by pharmacodynamic synergism. Minor/Significance Unknown.

              • insulin glargine

                bexarotene increases effects of insulin glargine by pharmacodynamic synergism. Minor/Significance Unknown.

              • insulin glulisine

                bexarotene increases effects of insulin glulisine by pharmacodynamic synergism. Minor/Significance Unknown.

              • insulin lispro

                bexarotene increases effects of insulin lispro by pharmacodynamic synergism. Minor/Significance Unknown.

              • insulin NPH

                bexarotene increases effects of insulin NPH by pharmacodynamic synergism. Minor/Significance Unknown.

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              Adverse Effects

              >10%

              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%)

              1-10%

              Hemorrhage

              Hypertension

              Hypothyroidism

              Heart failure

              Tachycardia

              Acne

              Depression

              Pustular rash

              Sunburn

              Pharyngitis

              Rhinitis

              Arthralgia

              Blephartis

              Corneal lesion

              Renal dysfunction

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              Warnings

              Black Box Warnings

              Retinoids are associated with birth 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

              Cautions

              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

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              Pregnancy & Lactation

              Pregnancy

              Contraindicated during pregnancy

              Animal studies

              • Malformations observed when administered orally to pregnant rats during days 7-17 of gestation
              • Developmental abnormalities included incomplete ossification at 4 mg/kg/day and cleft palate, depressed eye bulge/microphthalmia, and small ears at 16 mg/kg/day
              • At doses >10 mg/kg/day, bexarotene caused developmental mortality

              Contraception

              • Females
                • Use effective contraception for 1 month before initiating, during therapy, and for at least 1 month after discontinuation
                • Use 2 reliable forms of contraception simultaneously unless abstinence is chosen method
              • Males
                • Male patients with sexual partners who are pregnant, possibly pregnant, or who could become pregnant must use condoms during sexual intercourse during therapy and for at least 1 month after last dose

              Lactation

              Unknown whether bexarotene is excreted in human milk

              Owing to potential for serious adverse reactions in nursing infants from bexarotene, a decision should be made whether to discontinue nursing or to discontinue bexarotene, considering its importance 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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              Administration

              Oral Administration

              Take with a meal

              Storage

              Store at 2-25ºC (36-77ºF)

              Avoid exposing to elevated temperatures and humidity after opening bottle

              Protect from light

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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.

              Create Your List of Plans

              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.

              View explanations for tiers and restrictions
              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.