-2%
Obexa is prescribed for adults diagnosed with Primary Biliary Cholangitis (PBC) who either:
- Do not have cirrhosis, or
- Have compensated cirrhosis without signs of portal hypertension.
- It can be used:
- In combination with ursodeoxycholic acid (UDCA) when the response to UDCA alone is insufficient, or
- As monotherapy in patients intolerant to UDCA.
Obeticholic acid activates the Farnesoid X Receptor (FXR) found in the liver and intestines. FXR plays a crucial role in controlling bile acid levels, inflammation, fibrosis, and metabolism. Its activation reduces bile acid build-up in liver cells by:
- Suppressing bile acid synthesis from cholesterol
- Enhancing their excretion from hepatocytes
- This action reduces the circulating bile acid pool and encourages bile flow, lowering hepatic bile acid exposure.
Pharmacodynamics:
Daily dosing with 10 mg obeticholic acid led to a 173% rise in FGF-19, a bile-regulating hormone, over 12 months. It also reduced levels of cholic acid and chenodeoxycholic acid. The clinical implications of these changes remain unclear.
Cardiac Safety:
No significant QT interval prolongation was observed at doses up to 10 times the recommended level.