II. Indications

III. Mechanism

  1. Synthetic Retinoid (Retinoic Acid analog) with antineoplastic activity, used in T-Cell Lymphoma
  2. Bexarotene binds Retinoid X receptors (RXRs include RXR-a, RXR-b, RXR-y)
    1. Bound receptors act as transcription factors that alter gene expression
    2. Receptor binding promotes increased cell differentiation and decreased cell proliferation
    3. Induces apoptosis and Cutaneous T-Cell Lymphoma tumor regression

IV. Medications

  1. Bexarotene oral capsules: 75 mg
  2. Bexarotene gel 1%
    1. Avoid applying gel under Occlusive Dressings
    2. Avoid use in combination with DEET

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Adverse Effects: Topical Gel

VII. Adverse Effects: Capsules (Systemic)

VIII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Systemic Retinoids are associated with severe birth defects
    2. Use reliable Contraception, with at least one form that is a non-hormonal (see Drug Interactions below)
  3. Monitoring (systemic capsules)
    1. Complete Blood Count
    2. Lipid profile
    3. Liver Function Tests
    4. Thyroid Function Tests

IX. Drug Interactions: Capsules (Systemic)

  1. Other agents that increase Bexarotene levels
    1. Gemfibrozil
  2. CYP3A4 Inducer
    1. May decrease activity of drugs metabolized by CYP3A4 including Oral Contraceptives

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Ontology: bexarotene (C0765273)

Definition (NCI_NCI-GLOSS) A drug used to treat skin problems caused by cutaneous T-cell lymphoma that have not gotten better after other treatment. It is also being studied in the treatment of other types of cancer. Bexarotene is a type of retinoid.
Definition (NCI) A synthetic retinoic acid agent with potential antineoplastic, chemopreventive, teratogenic and embryotoxic properties. Bexarotene selectively binds to and activates retinoid X receptors (RXRs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, apoptosis of some cancer cell types, and tumor regression. (NCI04)
Definition (PDQ) A synthetic retinoic acid agent with potential antineoplastic, chemopreventive, teratogenic and embryotoxic properties. Bexarotene selectively binds to and activates retinoid X receptors (RXRs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, apoptosis of some cancer cell types, and tumor regression. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42117&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42117&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1635" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C095105
SnomedCT 395281006, 116346006, 387023000
English 4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethenyl)benzoic acid, 4-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic Acid, 3-methyl TTNEB, 3-methyl-TTNEB, retinoids bexarotene, bexarotene (medication), bexarotene, bexarotene [Chemical/Ingredient], BEXAROTENE, Bexarotene (product), Bexarotene (substance), Bexarotene
Spanish bexarronteno, bexaroteno, bexaronteno (sustancia), bexaronteno, bexaroteno (sustancia), bexaroteno (producto), bexarronteno (producto), bexarronteno (sustancia)