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Bexarotene (Systemic)

Class: Antineoplastic Agents
VA Class: AN900
Chemical Name: 4-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid
Molecular Formula: C24H28O2
CAS Number: 153559-49-0
Brands: Targretin

Medically reviewed by on Apr 21, 2021. Written by ASHP.


May cause birth defects in humans; teratogenicity and embryolethality demonstrated in animals. Contraindicated in pregnant women. See Fetal/Neonatal Morbidity and Mortality under Cautions.


Antineoplastic agent; synthetic retinoid analog.

Uses for Bexarotene (Systemic)

Cutaneous T-cell Lymphoma

Treatment of skin manifestations of cutaneous T-cell lymphoma (CTCL) in patients who are refractory to at least one prior systemic therapy.

Bexarotene (Systemic) Dosage and Administration


Oral Administration

Administer orally once daily with a meal.




Initially, 300 mg/m2 daily.

If intolerable adverse effects occur, decrease dosage to 200 mg/m2 daily, then 100 mg/m2 daily, or temporarily discontinue. When toxicity is controlled, carefully readjust dosage upward.

If no tumor response is observed after 8 weeks and the 300-mg/m2 daily dosage is well tolerated, increase to 400 mg/m2 daily with careful monitoring.

Continue as long as benefit is derived from therapy. Optimum duration is not known.

Cautions for Bexarotene (Systemic)


  • Known or suspected pregnancy.

  • Known hypersensitivity to bexarotene or any ingredient in the formulation.



Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; teratogenicity and embryolethality demonstrated in animals.

Exclude pregnancy 1 week prior to initiation of therapy. Initiate therapy on second or third day of normal menstrual period. Repeat pregnancy tests monthly during therapy. To facilitate pregnancy test assessment and counseling, dispense no more than 1 month supply.

Use contraception (2 reliable forms, including at least 1 nonhormonal method) for 1 month before, during, and for 1 month after administration. Male patients should use condoms during sexual intercourse with women who are or may become pregnant.

If pregnancy occurs, immediately discontinue and apprise of potential fetal hazard.

Effects on Lipoproteins

Lipid abnormalities (e.g., hyperlipidemia, elevated fasting triglycerides and cholesterol, decreased HDL-cholesterol) occur in most patients; usually develop within 2–4 weeks and are reversible with cessation of therapy.

If fasting triglycerides are or become elevated, institute antilipemic therapy and reduce bexarotene dosage or suspend therapy. Gemfibrozil is not recommended. (See Specific Drugs and Foods under Interactions.) Monitor fasting blood lipid levels weekly until lipid response is established, then at 8 week intervals.


Possible acute pancreatitis; possibly fatal. Patients with risk factors for pancreatitis (e.g., prior pancreatitis, uncontrolled hyperlipidemia or diabetes mellitus, excessive alcohol consumption, biliary tract disease, or therapy with drugs associated with pancreatic toxicity or known to increase triglyceride concentrations) generally should not receive bexarotene.

Hepatic Effects

Possible elevations in AST and ALT; usually resolve within 1 month following decrease in dosage or discontinuance.

Monitor liver function tests at baseline; after 1, 2, and 4 weeks of treatment; and at least every 8 weeks thereafter. Consider discontinuance if transaminases or bilirubin increase to 3 times ULN.

Thyroid Effects

Possible hypothyroidism. Consider thyroid supplementation in patients with laboratory evidence of hypothyroidism. Monitoring of thyroid function tests recommended.

Hematologic Effects

Leukopenia (generally neutropenia) possible, rarely associated with serious adverse events; time to onset usually 4–8 weeks, with resolution occurring within 30 days of dosage reduction or discontinuance of the drug in most patients. Obtain WBC with differential at baseline and periodically during therapy.

Ocular Effects

New cataracts or worsening of existing cataracts possible. Ophthalmologic evaluation recommended if visual difficulties occur.

Sensitivity Reactions


Use with caution in patients with known hypersensitivity to retinoids.

Photosensitivity Reactions

Sunburn and skin sensitivity to sunlight possible in patients exposed to direct sunlight. Minimize exposure to sunlight and artificial UV light.

Specific Populations


Category X. (See Fetal/Neonatal Morbidity and Mortality and also Contraindications under Cautions.)


Not known whether bexarotene is distributed into milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established in children <18 years of age.

Geriatric Use

No substantial differences in safety relative to younger adults, but increased sensitivity cannot be ruled out.

Hepatic Impairment

Use only with great caution. (See Hepatic Effects under Cautions and also Elimination: Special Populations under Pharmacokinetics.)

Common Adverse Effects

Lipid abnormalities, hypothyroidism, headache, asthenia, rash, leukopenia, anemia, nausea, infection, peripheral edema, abdominal pain, dry skin.

Interactions for Bexarotene (Systemic)

Metabolized by CYP3A4. Possibly also an inducer of CYP3A4.

Drugs Affecting Hepatic Microsomal Enzymes

Inhibitors or inducers of CYP3A4: potential pharmacokinetic interaction (altered bexarotene metabolism).

Drugs Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP3A4: potential pharmacokinetic interaction (decreased plasma substrate concentrations).

Protein-bound Drugs

Potential pharmacokinetic interaction (bexarotene displacement by, or bexarotene displacement of, other protein-bound drugs).

Specific Drugs and Foods

Drug or Food



Antidiabetic agents (e.g., insulin, sulfonylureas, other oral antidiabetic agents)

Potential increased incidence of hypoglycemia

Use concomitantly with caution

Antifungals (e.g., itraconazole, ketoconazole)

Possible increased plasma bexarotene concentrations


Pharmacokinetic interaction unlikely


Possible increased plasma bexarotene concentrations


Increased plasma bexarotene concentrations

Concomitant use not recommended

Grapefruit juice

Possible increased plasma bexarotene concentrations

Hormonal contraceptives

Decreased plasma concentrations of hormonal contraceptives


Possible decreased plasma bexarotene concentrations


Possible decreased plasma bexarotene concentrations


Possible decreased plasma bexarotene concentrations


Decreased plasma tamoxifen concentrations

Vitamin A

Possible increased toxicity

Bexarotene (Systemic) Pharmacokinetics



Absorbed following oral administration, with peak plasma concentrations attained within approximately 2 hours.


Peak plasma concentrations and AUC (after 75–300 mg doses) increased by approximately 48 and 35%, respectively, after a meal containing fat compared with glucose solution.



Distribution into body tissues and fluids has not been evaluated.

It is not known whether bexarotene is distributed into milk.

Plasma Protein Binding


Special Populations

In patients with renal impairment, possible altered protein binding and pharmacokinetics.



Metabolized extensively in the liver; in vitro, metabolized principally via CYP3A4 oxidation. Oxidative metabolites active in vitro; relative contributions of parent drug or metabolites to safety and efficacy unknown.

Elimination Route

Bexarotene and its metabolites eliminated principally via biliary excretion; not excreted in urine in appreciable amounts.


Approximately 7 hours.

Special Populations

In patients with hepatic impairment, greatly decreased clearance expected.





2–25°C. Avoid exposure to high temperatures and humidity after bottle is opened; protect from light.


  • Selectively binds with and activates retinoid X receptor (RXR) subtypes (RXRα, RXRβ, and RXRγ). Activated RXRs function as transcription factors that regulate the expression of genes controlling cellular differentiation and proliferation.

  • Exact mechanism(s) of action not determined, but bexarotene is active in all clinical stages of CTCL.

Advice to Patients

  • Importance of women informing clinicians immediately if they are or plan to become pregnant or plan to breast-feed.

  • Importance of women and men taking measures to avoid pregnancy because of risk to fetus.

  • Importance of men using condoms during sexual intercourse while receiving the drug and for at least 1 month after discontinuing the drug.

  • Importance of monthly pregnancy tests.

  • Importance of patients informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

  • Importance of taking bexarotene with, or immediately following, a meal.

  • Risk of photosensitivity reactions.

  • Risk of hypoglycemia in patients being treated for diabetes mellitus.

  • Importance of adhering to laboratory appointment schedules.

  • Importance of informing patients of other important precautionary information. (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.



Dosage Forms


Brand Names




75 mg

Targretin (with povidone)


AHFS DI Essentials™. © Copyright 2022, Selected Revisions May 1, 2006. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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