Table 3.
LXR agonists that target hepatic lipid and glucose metabolism
| Drug | Mechanism of action | Mode of administration | Regulatory status | Clinical effect | References | |||||
|---|---|---|---|---|---|---|---|---|---|---|
| Steatosis | Fibrosis markers | Hepatic enzymes | HbA1c | Insulin resistance | ||||||
| GSK2033 | LXRα/LXRβ inverse agonist | – | Preclinical | =a | NA | NA | NA | NA | [48, 55] | |
| SR9238 | LXRα/LXRβ inverse agonist | – | Preclinical | ↓a | ↓a | NA | NA | =a | [49] | |
| T0901317 | LXRα/LXRβ agonist | – | Preclinical | ↑a | NA | NA | NA | ↑a | [48, 53] | |
| GW3965 | LXRα/LXRβ agonist | – | Preclinical | ↑a | NA | NA | NA | ↑a | [53] | |
| BMS-852927 | LXRβ agonist | PO | Phase I | = | NA | NA | NA | NA | [50] | |
| BMS-779788 | LXRα/LXRβ agonist | PO | Phase I | ↑ | NA | NA | NA | NA | [50] | |
| LXR-623 (WAY 252623) | LXRα-partial/ LXRβ-full agonist | PO | Phase I | = a | NA | NA | NA | NA | [51, 52] | |
aPreclinical data
PO, oral