What exactly is obeticholic acid and what are its ingredients?

Obeticholic acid is a relatively mature prescription drug used in the field of liver diseases overseas. Its essence is not a "hepatoprotective drug" in the traditional sense, but a farnesoid X receptor (FXR) agonist. FXR is a type of nuclear receptor widely expressed in the liver, biliary system and intestines, and plays a central role in the regulation of bile acid synthesis, transport and metabolism. It is based on this target that obeticholic acid was developed to improve the pathological processes of cholestasis-related diseases, especially playing an important role in the long-term management of primary biliary cholangitis (PBC).

From the perspective of pharmaceutical ingredients, obeticholic acid is a synthetic bile acid derivative, and its molecular structure has been specially modified to make it highly selective and active forFXR. By activating FXR, obeticholic acid can down-regulate the synthesis of bile acids in the liver, while promoting the efflux of bile acids and reducing their abnormal accumulation in hepatocytes. This "regulation from the source" mechanism is essentially different from drugs that simply promote bile excretion or relieve symptoms, which also explains its unique positioning in the PBC treatment system.

In terms of indications, overseas guidelines and drug descriptions generally use obeticholic acid for adult PBC patients who have an inadequate response to or are intolerant to ursodeoxycholic acid (UDCA) treatment. For people who can still tolerate UDCA but have unsatisfactory efficacy, obeticholic acid can be used as part of a combination treatment regimen; for patients who cannot continue to use UDCA, a single-drug treatment path can be chosen. It should be emphasized that the prerequisite for its application is usually the absence of cirrhosis, or the presence of compensated cirrhosis and no manifestations related to portal hypertension. This is repeatedly mentioned in international medication recommendations.

Obeticholic acid is not a "quick-acting" drug, but rather a long-term disease management. Its goal is to improve biochemical indicators, delay disease progression and reduce the risk of complications. Therefore, in practical applications, doctors usually make comprehensive judgments based on the patient's disease course, liver function status, and previous treatment response.

Reference materials:https://www.interceptpharma.com/about-us/ocaliva-withdrawal-faq/