Table 1.
PPAR 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 | |||||
| Pioglitazone | PPAR-γ | PO | Phase IV | ↓ | ↓ | ↓ | ↓ | ↓ | [13, 151–153] |
| Rosiglitazone | PPAR-γ | PO | Phase IV | ↓ | = | ↓ | ↓ | ↓ | [154, 155] |
| Lobeglitazone | PPAR-γ | PO | Phase III | ↓ | = | NA | NA | ↓ | [156] |
| MSDC-0602 K | PPAR-γ MPC | PO | Phase IIb | ↓ | = | ↓ | ↓ | ↓ | [15, 157] |
| INT-131 besylate (CHS-131) | PPAR-γ SPPARM | PO | Phase III | ↓ | = | NA | ↓ | ↓ | [17] |
| MK-0533 | PPAR-γ SPPARM | PO | Phase II | NA | NA | NA | ↓ | ↓ | [18] |
| YR4–42 | PPAR-γ SPPARM | PO | Preclinical | ↓ | NA | NA | ↓ | ↓ | [19] |
| Fenofibrate | PPAR-α | PO | Phase IV | = | = | ↓ | = | = | [20–22] |
| Bezafibrate | PPAR-α | PO | Phase IV | NA | NA | ↓ | = | = | [23–25] |
| Pemafibrate (K-877) | PPAR-α SPPARM | PO | Phase II | NA | NA | ↓ | NA | ↓ | [26] |
| Saroglitazar | PPAR-α/γ | PO | Phase IIa | ↓ | ↓ | ↓ | ↓ | ↓ | [28, 29, 158] |
| Aleglitazar | PPAR-α/γ | PO | Phase III-stop | NA | NA | NA | ↓ | ↓ | [159] |
| Tesaglitazar | PPAR-α/γ | PO | Phase III-stop | ↓a | NA | ↓a | ↓ | ↓ | [160] |
| Muraglitazar | PPAR-α/γ | PO | Phase III-stop | ↓ | NA | ↓ | ↓ | ↓ | [161, 162] |
| TAK-559 | PPAR-α/γ | PO | Phase III-stop | NA | NA | = | ↓ | ↓ | [163] |
| MK0767 | PPAR-α/γ | PO | Phase III-stop | NA | NA | NA | ↓ | ↓ | [164] |
| Lanifibranor (IVA337) | PPAR-α/γ/δ | PO | Phase IIa | ↓ | ↓ | ↓ | ↓ | ↓ | [31, 32] |
| Elafibranor (GFT505) | PPAR-α/δ | PO | Phase III | ↓ | ↓ | ↓ | ↓ | ↓ | [30, 33] |
aPreclinical data
MPC, mitochondrial pyruvate carrier; PO, oral