Nidufexor (LMB763) is a potent and specific FXR-gene modulator in vivo, reducing steatosis, inflammation and fibrosis in nonalcoholic steatohepatitis (NASH) murine models.
Nidufexor exhibits moderate Cmax (4.5, 12.4, 28.1, 80.9, and 140.8 μM) and terminal elimination half-lives (t1/2; 3.9 5.7 6.3 5.6 6.3 h) following oral administration (3 ,10 ,30, 100, and 300mg/kg) in adult male Wistar Han rats (age approximately 10 weeks)
Nidufexor exhibits terminal elimination half-lives (mouse 4.5, rat 4.4 and, dog 6.8 h) following intravenous administration (mouse 3.0, rat 5.0 and, dog 0.5 mg/kg).
Nidufexor exhibits terminal elimination half-lives (mouse 3.5, rat 2.7 and, dog 10.1 h) following oral administration (mouse 10, rat 10 and, dog 2 mg/kg).
Animal Model: |
Han-Wistar rats |
Dosage: |
0.1, 0.3, 1.5, 7.5, 25, 100 mg/kg (Pharmacokinetic Analysis) |
Administration: |
Oral gavage, once daily for 14 days |
Result: |
On day 1 and 13, serum exposure increased approximately dose-proportionally from 0.1 to 100 mg/kg. Exposure at 0.1 and 0.3 mg/kg was likely underestimated on day 13. No significant accumulation was observed. |