Bexarotene
- Atc Codes:L01XX25
- CAS Codes:153559-49-0
- PHARMGKB ID:153559-49-0
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
Europe
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
Chemistry
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
Contraindications
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.