Drug intelligence / Profile preview

bexarotene

Development stage
Approved
Lead developer
Ligand Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical
01

Overview

Bexarotene is a third-generation retinoid and antineoplastic agent used primarily for the treatment of cutaneous T-cell lymphoma (CTCL), especially in patients who have not responded to previous systemic therapies. It acts as a selective agonist of retinoid X receptors (RXRs)—specifically RXRα, RXRβ, and RXRγ—which function as transcription factors regulating genes involved in cellular differentiation, proliferation, and apoptosis. By activating these receptors, bexarotene induces cell differentiation and apoptosis in malignant cells. The drug was developed by Ligand Pharmaceuticals and later rights were acquired by Eisai. Bexarotene has also been investigated off-label for other cancers such as lung cancer, breast cancer, Kaposi's sarcoma, and has been studied experimentally for Alzheimer's disease and multiple sclerosis[1][3][5][8].

Brand names
Targretin
Other names
4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid
02

Targets

RXRB (Retinoid X receptor beta)PPARG (Peroxisome proliferator-activated receptor gamma)RXRG (RXRγ)RXRA (Retinoid X receptor alpha)

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