The specific mechanism of action of odexibat (Belvi) and its mechanism of efficacy in the body

Odevixibat is a selective small molecule inhibitor that mainly targets intestinal bile acid transporter (IBAT, ileal bile acid transporter, also known as ASBT). This transporter is located in the terminal ileum and is an important pathway for bile acid recycling. By inhibiting IBAT, odexibat can block the reabsorption of bile acids from the intestine and increase the excretion of bile acids with the feces, thereby reducing the burden of bile acids on the liver and improving symptoms related to liver damage.

In terms of its pharmacodynamic mechanism in vivo, odexibat significantly reduces the amount of bile acids entering the liver by inhibiting intestinal bile acid reabsorption. This effect not only reduces the accumulation of bile acids in hepatocytes, but also reduces liver inflammation and fibrosis caused by cholestasis, thereby protecting liver function. For diseases with cholestasis as the main pathological feature, such as pediatric intrahepatic cholestasis (PFIC), this mechanism has obvious clinical significance.

Odesibat mainly acts locally in the intestine and has a low systemic absorption rate, which means that the concentration of the drug in the blood is not high, thereby reducing the risk of systemic side effects. At the same time, by increasing the excretion of bile acids with feces, symptoms related to cholestasis such as itching can be significantly improved and the quality of life of patients can be improved. Its clear target of action and strong targeting are a major advantage of this type of drug in the treatment of hepatobiliary diseases.

In addition, the efficacy of odexibat also involves the regulation of the entero-liver axis. By reducing ileal bile acid absorption, the drug can indirectly regulate the negative feedback mechanism of hepatic bile acid synthesis and secretion, reducing bile acid accumulation in the liver while maintaining bile acid homeostasis in the body. This mechanism of action enables odexibat to sustainably improve cholestasis-related symptoms in long-term use while being well tolerated and safe.

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