Table 1.
Summary of synthetic LXR agonist effects.
| Compound | Activity | Status | Disease/Model | Actions | Reference |
|---|---|---|---|---|---|
| T0901317 | LXRα/β dual agonist | Preclinical | EAE (MS model) | Reduced CNS inflammation | (65, 66) |
| Enhanced demyelination | |||||
| Reduced Clinical severity | |||||
| Preclinical | WT mice | Enhanced Myelin gene/protein expression | (69) | ||
| Increased Oligodendrocyte maturation | |||||
| Enhanced Remyelination | |||||
| LXR-623 | LXRα/partial/β full agonist | Clinical Trial-Phase 1-Discontinued | Atherosclerosis | Adverse neurological effects | (111) |
| Preclinical | Glioblastoma | Enhanced cell death | (112) | ||
| Increased cholesterol depletion | |||||
| Enhanced tumor regression | |||||
| Increased Survival | |||||
| BMS-852927 | LXRβ/selective partial agonist |
Clinical Trial-Phase 1-Discontinued | Healthy subjects | Increased Cholesterol transport | (113) |
| Enhanced Lipogenesis, triglycerides, LDL-C, apoB, apoE, CETP | |||||
| Decreased circulating neutrophils | |||||
| DMHCA/MePiPMHCA | Transrepression-selective | Preclinical | Colitis, brain injury | Reduced inflammation | (114, 115) |
| No induction of hepatic steatosis | |||||
| SREBP1c inhibition | |||||
| ATI-111 | Transrepression-selective | Preclinical | Atherosclerosis (Ldlr-null mice) |
Reduced atherosclerosis | (116) |
| Lowers plasma triglycerides and cholesterol | |||||
| SREBP1c inhibition |