Table 2.
Effects of pemafibrate (SPPARMα) and fenofibrate on basic parameters
| Parameters | Pemafibrate (SPPARMα) | Fenofibrate | |
|---|---|---|---|
| ABCA1 in human primary macrophages | 1) | +563% (at 10 μM) | + 168% (at 100 μM) |
| ABCG1 in human primary macrophages | 1) | +2093% (at 10 μM) | + 506% (at 100 μM) |
| HDL stimulated cholesterol efflux in human primary macrophages | 1) | 1.9-fold (at 10 μM) | 1.6-fold (at 100 μM) |
| VCAM1 in apoE2KI mice | 1) | −32% (at 1 mpk) | NS (at 250 mpk) |
| F4/80 in apoE2KI mice | 1) | − 30% (at 1 mpk) | NS (at 250 mpk) |
| IL6 in apoE2KI mice | 1) | − 40% (at 1 mpk) | NS (at 250 mpk) |
| Aortic lesion in apoE2KI mice | 1) | 0.061 mm2 (at 0.1 mpk) | 0.06 mm2 (at 250 mpk) |
| 0.022 mm2 (at 1 mpk) | 0.207 mm2 (at control) | ||
| 0.207 mm2 (at control) | |||
| Liver pathology score in amylin liver NASH model | 2) | [NAS] 6.2 (at 0.03 mg/kg), 3.9 (at 0.1 mg/kg) | [NAS] 5.7 (at 50 mg/kg) |
| [Steatosis] 3 (at 0.03 mg/kg), 1.3 (at 0.1 mg/kg) | [Steatosis] 2.4 (at 50 mg/kg) | ||
| [Lobular inflammation] 1.2 (at 0.03 mg/kg), 1.3 (at 0.1 mg/kg) | [Lobular inflammation] 1.4 (at 50 mg/kg) | ||
| [Hepatocyte ballooning] 2 (at 0.03 mg/kg), 1.3 (at 0.1 mg/kg) | [Hepatocyte ballooning] 1.9 (at 50 mg/kg) | ||
| [Fibrosis] 1.6 (at 0.03 mg/kg), 1.4 (at 0.1 mg/kg) | [Fibrosis] 1.3 (at 50 mg/kg) | ||
| Fatty acid oxidation (in the liver of MCD-fed mice) | 3) | [Acox1 mRNA] ↑ (at 0.00025%) | [Acox1 mRNA] ↑ (at 0.1%) |
| [Cpt1a mRNA] ↑ (at 0.00025%) | [Cpt1a mRNA] ↑ (at 0.1%) | ||
| ER stress (in the liver of MCD-fed mice) | 3) | [Xbp1s mRNA] ↓ (at 0.00025%) | [Xbp1s mRNA] ↓ (NS, at 0.1%) |
| LPL activity (male C57BL/6 J mice fed HFD) | 4) | ↑ (at 0.0005%) | ↑ (at 0.05%) |
| Npc1l1 mRNA in the intestinal epithelial cells (male C57BL/6 J mice fed HFD) | 4) | ↓ (at 0.0005%) | ↓ (at 0.05%) |
| Mttp mRNA in the intestinal epithelial cells (male C57BL/6 J mice fed HFD) | 4) | → (at 0.0005%) | ↑ (at 0.05%) |
| Hsl in eWAT (male WT mice fed HFD) | 5) | ↑ (at 0.00033%) | → (at 0.2%) |
| Ucp1 in iWAT (male WT mice fed HFD) | 5) | ↑↑ (at 0.00033%) | ↑ (at 0.2%) |
| Elovl3 in BAT (male WT mice fed HFD) | 5) | ↑ (at 0.00033%) | ↑ (at 0.2%) |
Abbreviations
ABCA1 ATP-binding cassette transporter A1, ABCG1 ATP-binding cassette transporter G1, VCAM1 vascular cell adhesion molecule 1, IL6 interleukin 6, KI knock-in, NASH non-alcoholic steatohepatitis, NAS non-alcoholic fatty liver disease activity score, MCD methionine-choline-deficient, Acox1 acyl-CoA oxidase 1, Cpt1a carnitine palmitoyltransferase 1a, ER endoplasmic reticulum, Xbp1s X-box binding protein 1s, LPL lipoprotein lipase, HFD high-fat diet, Npc1l1 niemann-pick c1-like 1, Mttp microsomal triglyceride transfer protein, Hsl hormone sensitive lipase, NS not significant, eWAT epididymal white adipose tissue, Ucp1 uncoupling protein 1, iWAT inguinal white adipose tissue, Elovl3 ELOVL fatty acid elongase 3, BAT brown adipose tissue
1) Ref [57]
2) Ref [108•]
3) Ref [107•]
4) Ref [60•]
5) Ref [65•]