Cayman Bexarotene

Bexarotene is an agonist of retinoid X receptors (RXRs; EC₅₀s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays).¹ It is selective for RXRs over retinoic acid receptors (RARs; EC₅₀s = >10 µM for RARα, RARβ, and RARγ). Bexarotene (10 µM) induces apoptosis in MJ, HuT 78, and HH cutaneous T cell lymphoma (CTCL) cells, as well as inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models when administered at a dose of 100 mg/kg per day.^2,3 It reduces increased brain interstitial fluid levels of amyloid-β (1-40) (Aβ40) and Aβ42 in the APP/PS1 transgenic mouse model of Alzheimer’s disease.⁴ It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC₉₀ = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC₅₀ = 2.01 µM).⁵ Formulations containing bexarotene have been used in the treatment of CTCL.

WARNING This product is not for human or veterinary use.