RGX-104 free Acid

RGX-104 (free base) is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

Signaling Pathways >> Metabolic Enzyme/Protease >> LXR

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

LXR[1]

Oral administration of RGX-104 to animals bearing palpable tumors significantly suppresses the growth of multiple cancer types. Strong tumor growth suppression is also observed in animals bearing large tumors. In some instances, RGX-104 treatment causes partial or complete tumor regression. What’s more, it is also found that co-administration of RGX-104 with anti-PD-1 is superior to administration of either RGX-104 or anti-PD-1 alone. Importantly, co-administration of RGX-104 with anti-PD-1 therapy is well tolerated by mice, with no overt signs of toxicity[1].

Bone marrow cells are cultured with B16F10 melanoma cells and GM-CSF for 6 days. On day 3, RGX-104 (2 μM) is added to the culture. The mean number of Gr-1high CD11b+ cells per 50 mL of culture solution is assessed by flow cytometry on day 6[1].

Mice[1] B16F10 cancer cells are subcutaneously injected into C57BL/6 mice. Following tumor growth to 5-10 mm3 in volume, mice are fed either control chow, chow supplemented with GW3965 (100 mg/kg), or chow supplemented with RGX-104 (100 mg/kg)[1].

[1]. Tavazoie MF, et al. LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer. Cell. 2018 Feb 8;172(4):825-840.e18.

T0901317 | GW3965 HCl | WAY 252623 | SR 9243 | (20S)-Protopanaxatriol | 27-Hydroxycholesterol | GSK 2033 | AZ876 | SR 9238 | 24-Hydroxycholesterol | BMS-779788 | BMS-852927 | Nagilactone B | RGX-104 | Rovazolac