The world's first generic version of liver cirrhosis drug obeticholic acid is launched

Cholic acid can directly regulate genes involved in differentBA activities. This can be regulated by the FXR signal. Therefore, various international guidelines recommend the use of obeticholic acid in combination with ursodeoxycholic acid (UDCA) or separately as monotherapy in patients with primary cholangitis (PBC) who have poor response to UDCA or are intolerant to UDCA.

1. Drug background and research and development: Obeeticholic acid was first discovered and patented byPellicciari Roberto. The drug was successfully developed by Intercept Pharmaceuticals in the United States and is the first drug approved to treat primary biliary cirrhosis (PBC) in the past 20 years. Its research and development results have brought new treatment options to patients with cirrhosis around the world.

2. Drug efficacy and mechanism: Obeticholic acid is a farnesoid X receptor agonist, which indirectly inhibits the gene expression of cytochrome 7A1 (CYP7A1) by activating the farnesoid X receptor. Since CYP7A1 is the rate-limiting enzyme in cholic acid biosynthesis, obeticholic acid can inhibit cholic acid synthesis and thus be used to treat primary cholangitis. In clinical trials, obeticholic acid increased levels of biomarkers associated with reduced risk of liver transplantation, demonstrating improved therapeutic efficacy.

3. Drug marketing and specifications: Obeticholic acid was approved by the FDA on May 27, 2016, and by the European Union on December 12 of the same year. The drug is sold under the trade name Ocaliva and is available in 5 mg 30 tablets and 10 mg 30 tablets. In addition, there are also domestic companies that have copied the drug and successfully launched it on the market, providing treatment options for more patients.

4. Drug administration and precautions: For patients without liver fibrosis orChild-Pugh A, the initial recommended dose is 5 mg each time, once a day. Based on clinical response, if alkaline phosphatase (ALP) or bilirubin cannot be effectively reduced and adverse reactions are tolerated, treatment can be gradually titrated to 10 mg (once a day) after 3 months of treatment. During the process of taking it, patients should pay close attention to their physical condition and seek medical consultation in time if they feel any discomfort.