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After removing the placebo effect, the relative baseline change (average value) after 14 days of oral ASC41 tablet treatment once a day | |||
1 mg
(n=12) | 2 mg
(n=12) | 5 mg
(n=12) | |
After removing the placebo effect, low-density lipoprotein cholesterol (LDL-C) decreased
P value vs placebo | -0. P=0. | -11. P=0. | -19. P=0. |
After removing the placebo effect, triglycerides (TG) decreased
P value vs placebo | -39. P=0. | -31. P=0. | -34. P=0. |
During the 14-day treatment, ASC41 had no grade 3 or higher adverse events, serious adverse events, or early discontinuation events in all dose groups
.
In the study of ASC41 tablets orally once a day for 14 days, the pharmacokinetic characteristics of ASC41 tablets showed a linear relationship as the dose increased from 1 mg to 5 mg
.
Conclusion: These data support the late-stage clinical trials of ASC41 for non-alcoholic steatohepatitis indications
.
2.
Title: The selective THR-β agonist ASC41 significantly improves the non-alcoholic fatty liver activity score and liver fibrosis score of rats with non-alcoholic steatohepatitis caused by high-fat diet
Abstract/Poster Number: 1908
Category: Non-alcoholic fatty liver disease treatment
Results: ASC41 was dose-dependent on improving liver steatosis, inflammatory cell infiltration, ballooning and non-alcoholic fatty liver activity score (NAS)
.
The 1.
5mg/kg and 4.
5mg/kg doses of ASC41 significantly improved the NAS score compared with the 5mg/kg dose of MGL3196, and there was a statistical difference between the two
.
When ASC41 was 0.
5 mg/kg, the NAS score was reduced by 23.
9%, and the liver fibrosis score was reduced by 14.
4%, which was comparable to MGL196 at 5 mg/kg
.
ASC41 showed a significant decrease in serum low-density lipoprotein at 1.
5mg/kg and 4.
5mg/kg
.
Conclusion: ASC41 can reduce NAS and liver fibrosis scores in rats with non-alcoholic steatohepatitis caused by high-fat diet
.
The current efficacy data supports ASC41 to carry out late-stage clinical trials
.
3.
Title: The new non-steroidal FXR agonist ASC42 significantly improves the non-alcoholic fatty activity score and liver fibrosis score of mice with non-alcoholic steatohepatitis caused by high-fat diet
Abstract/Poster Number: 1961
Category: Non-alcoholic fatty liver disease treatment
Results: ASC42 was dose-dependent on improving liver steatosis, inflammatory cell infiltration, ballooning and non-alcoholic fatty liver activity score (NAS)
.
Compared with obeticholic acid at 30 mg/kg, ASC42 at 30 mg/kg showed a higher NAS score reduction (P<0.
001)
.
ASC42 showed a 46.
2% reduction in NAS score and a 15.
2% reduction in liver fibrosis at 3 mg/kg, which was equivalent to 30 mg/kg obeticholic acid
.
In ASC42-treated mice, triglycerides in the liver showed a dose-proportional decrease
.
Conclusion: ASC42 can reduce NAS score and liver fibrosis score in mice with non-alcoholic steatohepatitis caused by high-fat diet
.
These data support ASC42 to carry out late-stage clinical trials
.
4.
Title: The new non-steroidal FXR agonist ASC42 has a significant inhibitory effect on HBsAg and HBV pgRNA in animals and in vitro
Abstract/Poster Number: 1917
Category: Viral Hepatitis
Results: In the primary human hepatocyte (PHH) model, the control compound entecavir (ETV) has the expected inhibitory activity on HBV DNA, but has no inhibitory effect on HBV pgRNA and HBsAg, while ASC42 presents a dose to HBsAg, HBV pgRNA and HBV DNA Dependent inhibition, EC50 was 0.
79μM, 0.
09μM and 0.
62μM, respectively (Figure 1 AD)
.
In the AAV/HBV mouse model, after ETV (0.
1mg/kg) monotherapy, the plasma HBV DNA of mice was significantly decreased, while HBV pgRNA and HBsAg did not decrease significantly.
ASC42 has an effect on HBV pgRNA, HBsAg, and HBV DNA in mouse plasma.
It has a dose-dependent inhibitory effect
.
Compared with the vehicle control group, the ASC42 high-dose group (60 mg/kg) reduced HBV pgRNA, HBsAg and HBV DNA by 0.
60 log10 copies/μl (P <0.
01), 0.
38 log10 IU/μl (P = 0.
002) and 0.
77 log10, respectively Copy/μl (P <0.
05) (Figure 1 EF)
.
Conclusion: FXR agonists ASC42 have significantly inhibited HBV DNA, HBV pgRNA and HBsAg, suggesting potential ASC42 clinical cure hepatitis B
.
This result supports further clinical trials of ASC42 in humans
.