Overview of the structural characteristics and sources of obeticholic acid

Obeticholic acid (Obeticholic acid, marketed under the trade name Ocaliva, is an important semi-synthetic bile acid analogue, mainly used to treat primary cholangitis. Its chemical structure is 6α-ethylchenodeoxycholic acid. This unique structure makes it a potent agonist of the farnesoid X receptor (FXR). The natural bile acid chenodeoxycholic acid was confirmed to be the most active physiological ligand of FXR in 1999, and obeticholic acid, as its derivative, exhibits more significant pharmacological effects.

FXR plays key physiological and pathological functions in the liver and intestines, and is involved in various processes such as cholesterol metabolism, lipid metabolism, and glucose homeostasis. Therefore, FXR is considered a potential target for the treatment of various human diseases. Obeticholic acid is the first FXR agonist to enter human clinical studies, opening a new chapter for research in this field.

In terms of chemical properties, the molecular formula of obeticholic acid isC26H44O4, and the molecular weight is 420.63 g/mol. The drug appears as a white to off-white powder with unique solubility characteristics: it is easily soluble in organic solvents such as methanol, dichloromethane and ethyl acetate, while solubility in water is affected by pH value. Obeticholic acid is slightly soluble under low pH conditions, but more soluble under high pH conditions. This characteristic provides an important reference for the development of its pharmaceutical preparations.

Oral dosage forms of obeticholic acid include5 mg and 10 mg tablets, each tablet containing obeticholic acid as the active ingredient and other inactive ingredients. These tablets are designed to ensure efficient release and absorption of the drug to achieve its intended therapeutic effect. Due to the important role of FXR in bile acid metabolism, the application of obeticholic acid may not only improve biliary health, but may also bring additional metabolic benefits by regulating lipid and glucose metabolism.

Reference materials:https://en.wikipedia.org/wiki/Obeticholic_acid