Obeticholic Acid is a semi-synthetic bile acid derivative and potent farnesoid X receptor (FXR) agonist. It is structurally related to chenodeoxycholic acid and contains an additional ethyl group at the 6α-position.
Obeticholic Acid is an important pharmaceutical research compound associated with bile acid metabolism, hepatobiliary disorders, FXR signaling, liver disease research, and metabolic pathway studies.
The compound is also known as 6-Ethylchenodeoxycholic Acid, 6α-Ethylchenodeoxycholic Acid, 6-ECDCA, and INT-747. Its chemical formula is C₂₆H₄₄O₄, with a molecular weight of 420.63 g/mol.
Obeticholic Acid has been developed as an oral pharmaceutical active ingredient. It has been extensively studied for its ability to activate FXR, a nuclear receptor involved in bile acid homeostasis and several metabolic, inflammatory, and fibrotic pathways.
For pharmaceutical development and API manufacturing in India, Obeticholic Acid is listed commercially by Indian API companies, demonstrating established interest in the molecule within the Indian pharmaceutical manufacturing sector.
The FDA substance record confirms the formula C₂₆H₄₄O₄ and molecular weight 420.63, while PubChem confirms CAS 459789-99-2 and the principal chemical identifiers.
Obeticholic Acid acts as an agonist of the farnesoid X receptor (FXR).
FXR is a nuclear receptor that plays a central role in regulating bile acid homeostasis. Activation of FXR influences gene expression involved in bile acid synthesis, transport, metabolism, and related hepatic pathways.
Obeticholic Acid-mediated FXR activation can influence:
The FDA describes Obeticholic Acid as an FXR agonist and identifies FXR as a regulator of bile acid, inflammatory, fibrotic, and metabolic pathways.
Obeticholic Acid is used in pharmaceutical development and research involving FXR-mediated biological pathways.
Important application areas include:
Obeticholic Acid has historically been developed for primary biliary cholangitis (PBC) and has been studied in additional liver-related conditions.
Regulatory note: The FDA records the U.S. accelerated approval of Ocaliva for PBC as withdrawn effective November 24, 2025. Therefore, current regulatory status should be checked for the relevant market before making therapeutic approval claims.
Obeticholic Acid is described as a white to off-white powder. The FDA labeling states that it is soluble in methanol, acetone, and ethyl acetate, while its water solubility is pH-dependent. It is slightly soluble at low pH and very soluble at high pH.
Obeticholic Acid is a semi-synthetic small-molecule API manufactured through controlled chemical synthesis and purification processes.
A pharmaceutical manufacturing process generally includes:
Because Obeticholic Acid contains several stereogenic centers, appropriate process controls are important for maintaining the required stereochemical profile.
Quality control of Obeticholic Acid should address identity, assay, purity, stereochemical characteristics, residual solvents, elemental impurities, physical properties, and stability.
Typical quality-control parameters include:
A validated chromatographic method can be used for quantitative assay and related-substance analysis according to the applicable API specification.
Obeticholic Acid demonstrates pH-dependent water solubility.
The FDA describes Obeticholic Acid as:
This pH-dependent behavior is consistent with the molecule's carboxylic-acid functionality.
Reported literature values place the melting behavior of Obeticholic Acid around 108–110°C. However, thermal behavior can depend on crystalline form and analytical conditions.
For this reason, melting point should preferably be treated as a characterization parameter rather than a universal release specification unless it is specifically defined in the applicable API specification.
India has an established pharmaceutical API manufacturing sector with companies commercially listing Obeticholic Acid. Indian API listings include Obeticholic Acid with the CAS number 459789-99-2, supporting the use of search terms such as Obeticholic Acid Manufacturer India, Obeticholic Acid API Manufacturer India, and Obeticholic Acid API India for pharmaceutical B2B visibility.
For SEO purposes, relevant search phrases include:
Obeticholic Acid has been developed for oral pharmaceutical formulations.
The FDA-approved Ocaliva product was supplied as 5 mg and 10 mg film-coated tablets containing Obeticholic Acid as the active ingredient.
Formulation-development considerations include:
Obeticholic Acid is an important research molecule for studying FXR-mediated pathways.
Research applications include:
Obeticholic Acid API should be stored according to the validated API specification and available stability data.
Recommended general handling practices include:
The specific storage temperature for API material should be established from the applicable stability data and approved product specification rather than assigning an unsupported universal temperature.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.15% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |