Bexarotene

Bexarotene
Clinical data
Trade namesTargretin
AHFS/Drugs.comMonograph
MedlinePlusa608006
License data
Routes of
administration		By mouth, topical
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding>99%
MetabolismHepatic (CYP3A4-mediated)
Elimination half-life7 hours
ExcretionParent drug and metabolites are eliminated primarily through the hepatobiliary system. Less than 1% is excreted in the urine unchanged.
Identifiers
  • 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.206.790 Edit this at Wikidata
Chemical and physical data
FormulaC24H28O2
Molar mass348.486 g·mol−1
3D model (JSmol)
  • O=C(O)c1ccc(cc1)C(/c2c(cc3c(c2)C(CCC3(C)C)(C)C)C)=C
  • InChI=1S/C24H28O2/c1-15-13-20-21(24(5,6)12-11-23(20,3)4)14-19(15)16(2)17-7-9-18(10-8-17)22(25)26/h7-10,13-14H,2,11-12H2,1,3-6H3,(H,25,26) checkY
  • Key:NAVMQTYZDKMPEU-UHFFFAOYSA-N checkY
  (verify)

Bexarotene, sold under the brand Targretin, is an antineoplastic (anti-cancer) agent used for the treatment of cutaneous T cell lymphoma (CTCL).[4] It is a third-generation retinoid.[5]

It was approved by the U.S. Food and Drug Administration (FDA) in December 1999, and the European Medicines Agency (EMA) in March 2001. It is available as a generic medication.[6][7]

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  2. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 15 August 2023.
  3. ^ Cite error: The named reference Targretin FDA label was invoked but never defined (see the help page).
  4. ^ Gniadecki R, Assaf C, Bagot M, Dummer R, Duvic M, Knobler R, et al. (September 2007). "The optimal use of bexarotene in cutaneous T-cell lymphoma". The British Journal of Dermatology. 157 (3): 433–440. doi:10.1111/j.1365-2133.2007.07975.x. PMID 17553039. S2CID 33092727.
  5. ^ Yuan S, Chan JF, Chik KK, Chan CC, Tsang JO, Liang R, et al. (September 2020). "Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system". Pharmacological Research. 159: 104960. doi:10.1016/j.phrs.2020.104960. PMC 7254006. PMID 32473310.
  6. ^ "2022 First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). 3 March 2023. Archived from the original on 30 June 2023. Retrieved 30 June 2023.
  7. ^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 3 March 2023. Retrieved 6 March 2023.