Analysis of the specific mechanism of action of Seladelpar

Seladelpar (Seladelpar) is a selective peroxisome proliferator-activated receptor (PPAR) delta agonist, mainly used to treat primary biliary cholangitis (PBC). PPARδ is a nuclear receptor widely expressed in various tissues including liver, muscle and fat. It plays an important role in various physiological processes, such as lipid metabolism, glucose metabolism and inflammatory response. By activating PPARδ, Siladepa can exert its therapeutic effect through multiple pathways, especially showing a unique role in the regulation of bile acid metabolism.

Specifically, Siladepa inhibits the synthesis of bile acids by activatingPPARδ. Bile acids are converted from cholesterol, and normally they aid in the digestion and absorption of fat. However, in PBC patients, bile acids accumulate in the liver due to bile duct damage, leading to liver inflammation and damage. Siladepa activates PPARδ, causing a molecule called fibroblast growth factor 21 (FGF21) to work. FGF21 can inhibit the expression of the key enzyme CYP7A1, which is the key enzyme that converts cholesterol into bile acids. By down-regulating the activity of CYP7A1, Siladepa effectively reduces the synthesis of bile acids, thereby alleviating the toxic effects of bile acid accumulation on the liver.

In addition, the mechanism of action of Siladepa is not limited to the inhibition of bile acid synthesis. Activation of PPARδ can also improve liver lipid metabolism and reduce inflammatory reactions caused by lipid accumulation. This process helps reduce oxidative stress in PBC patients and further alleviate liver inflammation and damage.

Although the mechanism of action of Siladepa has been clarified to some extent through a series of clinical and basic studies, the specific therapeutic mechanism for PBC patients is still not completely clear. Existing research mainly focuses on how Siladepa exerts its therapeutic effect by regulating bile acid metabolism, improving lipid metabolism, and reducing inflammatory responses. However, whether these mechanisms can fully explain all the therapeutic effects of Siladepa still requires further research to verify.

Reference materials:https://www.drugs.com/seladelpar.html