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Bexarotene

Retinoid · Antineoplastic

Also known as Targretin

RetinoidAntineoplastic
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Extremely teratogenic. Avoid during pregnancy. Effective contraception required during and for at least 1 month after treatment for men and women, and for at least 6 months after treatment in women of childbearing potential.
FDA category + note
Top interactionssee all 12
  • AcitretinSevereDatabaseDDInter
  • AdalimumabSevereDatabaseDDInter
  • AlbiglutideSevereDatabaseDDInter
  • AlogliptinSevereDatabaseDDInter

Mechanism

Bexarotene is an agonist at the retinoid X receptor, which is involved in the regulation of cell differentiation and proliferation. This action can lead to the regression of cutaneous T-cell lymphoma.

Indications

Skin manifestations of cutaneous T-cell lymphoma refractory to previous systemic treatmentAdvanced (stages IIb or III) cutaneous T-cell lymphoma refractory to local skin directed therapy and at least one systemic therapy (second-line treatment)

Dosing

Adult
Initially 300 mg/m2 once daily, adjusted according to response, to be taken with a meal.
Renal adjustment
Avoid if creatinine clearance less than 25 mL/minute. Reduce dose and increase dosing interval if creatinine clearance less than 65 mL/minute (consult product literature).
Hepatic adjustment
Caution in mild to moderate hepatic impairment; avoid in severe impairment, jaundice, decompensated disease, or hepatic insufficiency.

Contraindications

  • History of pancreatitis
  • Hypervitaminosis A
  • Uncontrolled hyperlipidaemia
  • Uncontrolled hypothyroidism
  • Hepatic insufficiency
  • Acute porphyrias

Side effects

Common
AlopeciaAnaemiaAppetite decreasedArthralgiaAstheniaChillsConstipationDeafnessDiarrhoeaDizzinessDry eyeDry mouthDyslipidaemiaEye disordersGastrointestinal discomfortGastrointestinal disordersHeadachesHyperhidrosisHypersensitivityHypoproteinaemiaHypothyroidismIncreased risk of infectionOedemaSkin reactionsTaste alteredThrombocytopeniaVomitingWeight decreased
Serious
  • Gastrointestinal haemorrhage
  • Neuropsychiatric reactions (e.g., depression, suicidal ideation)
  • Pancreatitis
  • Hepatic failure
  • Hyperbilirubinaemia
  • Hypertension
  • Hyperthyroidism
  • Increased leucocytes
  • Muscle weakness
  • Neoplasms
  • Nerve disorders
  • Renal impairment
  • Thrombocytosis
  • Varicose veins
  • Vision disorders

Pregnancy & lactation

Pregnancy

Extremely teratogenic. Avoid during pregnancy. Effective contraception required during and for at least 1 month after treatment for men and women, and for at least 6 months after treatment in women of childbearing potential.

Lactation

Discontinue breast-feeding.

Drug interactions

Acitretin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Albiglutide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alogliptin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Aminolevulinic Acid
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Asparaginase Erwinia Chrysanthemi
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Asparaginase Escherichia Coli
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Baricitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Brigatinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Calaspargase Pegol
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Certolizumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cidofovir
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Other Retinoid drugs

Ask House about Bexarotene

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Sources: Katzung, BNF·Verified: 2026-05-10 · House clinical team