Bexarotene | Retinoid RXR agonist

Bexarotene (153559-49-0) is a highly potent and selective retinoid X receptor (RXR) agonist (EC₅₀=28, 25, 20 nM for RXRα, β, γ respectively).¹ Clinically useful antineoplastic agent for cutaneous T-cell lymphoma² Causes complete regression of mammary carcinoma³. Bexarotene significantly increases clearance of soluble β-amyloid in a mouse Alzheimer's model and increases cognitive ability.⁴ Reverses apoE4-driven brain pathology and behavioral deficits in vivo.⁵

References/Citations
1) Boehm et al. (1995), Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells; J. Med. Chem., 38 3146
2) Gniadecki et al. (2007), The optimal use of bexarotene in cutaneous T-cell lymphoma; Br. J. Dermatol., 157 433
3) Bischoff et al. (1998), Beyond tamoxifen: the retinoid X receptor-selective ligand LGD1069 (TARGRETIN) causes complete regression of mammary carcinoma; Cancer Res., 58 479
4) Cramer et al. (2012), ApoE-directed herapeutics rapidly clear β-amyloid and reverse deficits in AD mouse models; Science, 335 1503
5) Boehm-Cagan & Michaelson (2014), Reversal of apoE4-driven brain pathology and behavioral deficits by bexarotene; J. Neurosci., 34 7293