• Molecular NameBexarotene
  • Synonymbexarotene
  • Weight348.486
  • Drugbank_IDDB00307
  • ACS_NO153559-49-0
  • Show 3D model
  • LogP (experiment)8.096
  • LogP (predicted, AB/LogP v2.0)7.28
  • pkaN/A
  • LogD (pH=7, predicted)4.41
  • Solubility (experiment)Insoluble
  • LogS (predicted, ACD/Labs)(ph=7)-3.22
  • LogSw (predicted, AB/LogsW2.0)0.0
  • Sw (mg/ml) (predicted, ACD/Labs)0.0
  • No.of HBond Donors1
  • No.of HBond Acceptors2
  • No.of Rotatable Bonds3
  • TPSA37.3
  • StatusFDA approved
  • AdministrationOral and Topical
  • PharmacologyAn oral antineoplastic agent indicated by the FDA (in 2000) for cutaneous T cell lymphoma. It has been used off-label for lung cancer, breast cancer, and Kaposi's sarcoma.
  • Absorption_valueN/A
  • Absorption (description)N/A
  • Caco_2N/A
  • BioavailabilityN/A
  • Protein binding99.0
  • Volume of distribution (VD)N/A
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmBexarotene undergoes oxidative metabolism via CYP450 3A4 and its metabolites are then glucuronidated. Four bexarotene metabolites have been identified in the plasma: 6- and 7- hydroxy-bexarotene and 6-and 7-oxo-bexarotene. All of the metabolites are active in vitro, but their clinical significance is not known.
  • Half life7 hours
  • ExcretionParent drug and metabolites are eliminated primarily through the hepatobiliary system. Less than 1% is excreted in the urine unchanged.
  • Urinary ExcretionN/A
  • CleranceN/A
  • ToxicityThe most common adverse events reported with an incidence of at least 10% in patients with Cutaneous T-Cell Lymphoma treated at an initial dose of 300 mg/m2/day of Targretin ? capsules include lipid abnormalities (elevated triglycerides, elevated total and LDL cholesterol and decreased HDL cholesterol), hypothyroidism, headache, asthenia, rash, leukopenia, anemia, nausea, infection, peripheral edema, abdominal pain, and dry skin. Adverse events leading to dose reduction or study drug discontinuation in at least two patients were hyperlipemia, neutropenia/leukopenia, diarrhea, fatigue/lethargy, hypothyroidism, headache, liver function test abnormalities, rash, pancreatitis, nausea, anemia, allergic reaction, muscle spasm, pneumonia, and confusion.
  • LD50 (rat)N/A
  • LD50 (mouse)N/A