Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Targretin; Belgium: Targretin; Bulgaria: Targretin; Cyprus: Targretin; Czech Republic: Targretin; Denmark: Targretin; Estonia: Targretin; Finland: Targretin; France: Targretin; Germany: Targretin; Greece: Targretin; Hungary: Targretin; Ireland: Targretin; Italy: Targretin; Latvia: Targretin; Lithuania: Targretin; Luxembourg: Targretin; Malta: Targretin; Netherlands: Targretin; Poland: Targretin; Portugal: Targretin; Romania: Targretin; Slovakia: Targretin; Slovenia: Targretin; Spain: Targretín; Sweden: Targretin; UK: Targretin.

North America

Canada: Targretin; USA: Targretin.

Latin America

Argentina: Targretín.

Drug combinations


Bexarotene: C~24~H~28~O~2~. Mw: 348.48. (1) 4-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid; (2) p-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthyl)vinyl]benzoic acid. CAS-153559-49-0 (1998).

Pharmacologic Category

Other Antineoplastic Agents. (ATC-Code: L01XX25).

Mechanism of action

The exact mechanism is unknown. Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin. Selectively binds with and activates retinoid X receptor (RXR) subtypes (RXR~α~, RXR~β~, and RXR~γ~).

Therapeutic use

Treatment of patients with cutaneous manifestations of refractory cutaneous T-cell lymphoma or who have not tolerated other therapies.

Pregnancy and lactiation implications

Must not be given to a pregnant woman or a woman who intends to become pregnant. Contraindicated during lactation.

Unlabeled use


Hypersensitivity to bexarotene or any component of the formulation. Known or suspected pregnancy.

Warnings and precautions

Hypothyroidism may occur. Leukopenia (neutropenia) is possible. Lipid abnormalities (e.g. hyperlipidemia, elevated fasting triglycerides and cholesterol, decreased HDL-cholesterol) are common. Extreme caution in hepatic impairment (possible elevations in AST and ALT). Possible acute pancreatitis, secondary to hypertriglyceridemia, possibly fatal. New cataracts or worsening of existing cataracts possible. Use with caution in diabetes mellitus. Limit additional vitamin A intake to <15000 IU/day. May cause xerostomia and gingivitis. May cause insomnia, agitation, confusion, and depression. Use with caution in known hypersensitivity to retinoids. Photosensitivity reactions (sunburn and skin sensitivity to sunlight) may occur.



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