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Synonyms: LGD1069 | Targretin® | Targrexin®
bexarotene is an approved drug (FDA (1999), EMA (2001))
Compound class: Synthetic organic
Comment: Bexarotene is a retinoid that selectively activates retinoid X receptors (RXRs), and is used for its antineoplastic action.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: bexarotene
|No information available.
|Summary of Clinical Use
|Bexarotene is an antineoplastic agent used in the treatment of cutaneous T cell lymphoma, usually following failure of previous treatments. Bexarotene shows activity in all clinical stages of cutaneous T cell lymphoma and has been used for non-indicated cancers such as lung and breast cancer, and Kaposi’s sarcoma.
|Mechanism Of Action and Pharmacodynamic Effects
|The mechanism of action is poorly understood but involves selective activation of retinoid X receptors (RXRα, RXRβ and RXRγ)