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. 2021 Apr 20;64(7):1461–1479. doi: 10.1007/s00125-021-05442-2

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, 151153]
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 = = = = [2022]
Bezafibrate PPAR-α PO Phase IV NA NA = = [2325]
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