This week in therapeutics




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Alzheimer's disease (AD)

Liver X receptor-b (NR1H2; LXR-b)

SAR and mouse studies suggest flavonoid LXR-b agonists could be useful for treating AD. In cultured microglia, flavonoid LXR-b agonists upregulated lipid transport proteins that could counteract b-amyloid (Ab) in AD without also causing lipid and triglyceride accumulation in liver cells. In a mouse model of AD, the lead compound decreased total brain Ab compared with vehicle control. Next steps include further optimizing the compounds and testing their functional effects in mouse AD models.
Vitae Pharmaceuticals Inc.'s LXR-b agonist, VTP-4, is in preclinical development for AD.

SciBX 6(33); doi:10.1038/scibx.2013.898
Published online Aug. 29, 2013

Patent pending; available for licensing

Hu, Y. et al. J. Med. Chem.; published online July 11, 2013;
Contact: Xianzhang Bu, Sun Yat-sen University, Guangzhou, China