-
Categories
-
Pharmaceutical Intermediates
-
Active Pharmaceutical Ingredients
-
Food Additives
- Industrial Coatings
- Agrochemicals
- Dyes and Pigments
- Surfactant
- Flavors and Fragrances
- Chemical Reagents
- Catalyst and Auxiliary
- Natural Products
- Inorganic Chemistry
-
Organic Chemistry
-
Biochemical Engineering
- Analytical Chemistry
-
Cosmetic Ingredient
- Water Treatment Chemical
-
Pharmaceutical Intermediates
Promotion
ECHEMI Mall
Wholesale
Weekly Price
Exhibition
News
-
Trade Service
Recently, the new FXR agonist CS0159 jointly developed by the Xu Huaqiang team and Li Jia's team of Shanghai Institute of Materia Medica, has been recognized by the US Food and Drug Administration (FDA) Fast Track and is intended to be used to treat patients
with nonalcoholic steatohepatitis (NASH).
NASH is a chronic metabolic liver disease that can progress to cirrhosis and even liver cancer
.
There are currently no drugs approved in China or the United States for the treatment of NASH
.
Effective and tolerable treatment regimens
are urgently needed clinically.
CS0159 is a novel potent nonsteroidal farnesitol X receptor (FXR) small molecule agonist
based on crystal structure aided design.
Based on the deep understanding of the structure and mechanism of FXR target and drug interaction, the research team designed and synthesized a series of lead compounds, and evaluated the pharmacodynamics, toxicology and pharmacokinetics of the compounds in vitro and in vitro, and finally obtained the new drug candidate compound CS0159
.
The innovation of this project lies in making full use of protein structure-assisted design, discovering action sites that can enhance drug activity and reduce drug side effects, and apply them to
the molecular design of new drugs.
Systematic preclinical studies have shown that CS0159 has the characteristics of potent FXR agonist activity and liver-targeted distribution, which can significantly improve the pathological status of NASH mouse models, and has the characteristics of
low onset dose, significant efficacy and good tolerability.
At present, CS0159 oral tablet has completed clinical phase I trials in the United States, and preliminary results have shown good safety tolerance and expected PD biomarker signaling
.
Phase II clinical trials for NASH indications will begin
in the United States.
In 2020, the project was transferred to Kaisei (Shanghai) Pharmaceutical Technology Co.
, Ltd.
by Shanghai Institute of Materia Medica, and Van Andel Research Institute in the United States under exclusive license for global R&D and promotion
.
(Contributing department: Xu Huaqiang research group)
