BI-5756 is a cholesteryl ester transfer protein (CETP) inhibitor, also is a potent agonist of cannabinoid receptor 1 (CB1R, CB1) with IC50 of 0.966 uM in cell-based radioligand binding assay using CP55940.
BI-5756 directly increases the frequencies of regulatory T cells (Tregs) in primary murine pan T cells after activation.
BI-5756 exhibits an in vivo protective effect against graft-versus-host disease (GvHD), an allogeneic T cell-mediated inflammatory complication after allogeneic hematopoietic cell transplantation (allo-HCT), resulting in an improved overall survival with enhanced platelet recovery and reconstitution of bone marrow-derived B and T cells.
BI-5756 also directly suppresses tumor cell growth and upregulates MHC I, MHC II, and CD80 on tumor cells, which may subsequently BI-5756 enhance T cell-mediated anti-tumor responses in mixed lymphocyte reaction with A20 cells.
BI-5756 exhibits immunomodulatory effect which is mediated via CB1.
BI-5756 shows a robust elevation of HDL-C and reduction of LDL-C.