Elafibranor is an orally active small-molecule dual peroxisome proliferator-activated receptor (PPAR) α/δ agonist. It is also known by the development code GFT505. Elafibranor has been developed for disorders involving bile acid metabolism, inflammation and liver fibrosis.
Elafibranor is the active substance in Iqirvo, a medicine used for the treatment of primary biliary cholangitis (PBC). In the European Union, Iqirvo is indicated in adults in combination with ursodeoxycholic acid (UDCA) when the response to UDCA is inadequate, or as monotherapy for patients who cannot tolerate UDCA.
Elafibranor activates PPARα and PPARδ receptors, which are involved in the regulation of bile acid homeostasis, inflammation and fibrosis. Activation of these receptors can help regulate bile acid synthesis, detoxification and transport.
Elafibranor has the molecular formula C22H24O4S and a molecular weight of approximately 384.5 g/mol. Its CAS Registry Number is 923978-27-2.
Elafibranor is primarily associated with pharmaceutical development for primary biliary cholangitis (PBC) and research involving bile acid metabolism, cholestasis, hepatic inflammation and fibrosis. Its pharmacological activity is associated with activation of PPARα and PPARδ receptors.
For pharmaceutical applications, Elafibranor API should be manufactured and tested according to the applicable quality system and approved product specification. Important quality attributes may include identity, assay, related substances, residual solvents, water content, elemental impurities and other applicable analytical parameters.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Melting Point | 150°C – 154°C |