2 Farnesoid-X Receptor Agonists: A New Class of Drugs for the Treatment of Pbc? An International Study Evaluating the Addition of Int-747 to Ursodeoxycholic Acid

Hepatotoxicity in 2011: advancing resolutely

“…Another potential target would be nuclear receptors, which are involved in multiple physiological liver functions. Of late, the famesoid X receptor agonist obeticholic acid, which showed choleretic and antifibrotic properties in experimental models, has been successfully tried to improve cytolysis and cholestasis indices in patients with primary biliary cirrhosis and deficient response to ursodeoxycholic acid (63), and might theoretically be also effective in patients with prolonged toxic cholestasis.…”

Letter: biochemical response to combination anti‐retroviral therapy in patients with primary biliary cirrhosis

“…6 Of note, this anti-retroviral regimen was equally efficacious as the farnesoid X receptor agonist, obeticholic acid with regard to observed biochemical improvement. 7 We have now identified other anti-beta retroviral regimens in animal models and patients. 8,9 Interim analysis of a randomised, placebo-controlled, crossover study using lopinavir/ritonavir 800/200 mg and tenofovir/ emtricitabine 300/200 mg has now shown an incremental improvement in decreased ALP levels as compared with the prior anti-retroviral study ( Figure 1).…”

Current research on the treatment of primary sclerosing cholangitis

“…The safety and efficacy of OCA has been evaluated in 2 randomized clinical trials in patients with primary biliary cirrhosis (PBC) with promising results (43,44). The administration of OCA to PBC patients led to a significant reduction of serum alkaline phosphatase (ALP), an important surrogate marker in PBC (43,44).…”

“…The administration of OCA to PBC patients led to a significant reduction of serum alkaline phosphatase (ALP), an important surrogate marker in PBC (43,44). One important adverse event was pruritus, occurring in a dose-dependent manner and leading to discontinuation of the drug in 38% of PBC patients (43,44). Currently, a phase II clinical trial of OCA in PSC patients is ongoing, using lower doses to help avoid pruritus (ClinicalTrials.gov Identifier: NCT02177136).…”