Abequolixron (RGX-104)

Description: RGX-104 (formerly known as SB 742881) is a novel potent and orally available liver-X nuclear hormone receptor-beta (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene. It has potential immunomodulating and antineoplastic activities. RGX-104 selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells.

References: Cell. 2018 Feb 8; 172(4):825-840.e18.

Related CAS#: 610318-03-1 (HCl)