Bexarotene is a high-affinity ligand for retinoid X receptors (RXRs) (EC50 = 28, 25, and 20 nM for RXRα, β, and γ, respectively). It inhibits cell cycle progression, induces apoptosis, prevents or overcomes multidrug resistance through multidrug resistance protein 1 (MDR1), and blocks angiogenesis and metastasis, making it a promising chemopreventive agent against cancer. Bexarotene also, through RXR activation, stimulates clearance of soluble β-amyloid, reduces plaque area, and reverses deficits related to Alzheimer’s disease in mice.
