Comparative Pharmacology
Head-to-head clinical analysis: OBETICHOLIC ACID versus OCALIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: OBETICHOLIC ACID versus OCALIVA.
OBETICHOLIC ACID vs OCALIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Obeticholic acid is a potent, selective agonist of the farnesoid X receptor (FXR), a nuclear receptor that regulates bile acid synthesis, transport, and homeostasis. Activation of FXR reduces bile acid synthesis by inhibiting CYP7A1, increases bile acid clearance, and exerts anti-inflammatory and antifibrotic effects.
Ocaliva (obeticholic acid) is a farnesoid X receptor (FXR) agonist. FXR is a nuclear receptor that regulates bile acid synthesis, transport, and homeostasis. Activation of FXR reduces the production of bile acids by suppressing cholesterol 7 alpha-hydroxylase (CYP7A1), the rate-limiting enzyme in bile acid synthesis, and increases the expression of FXR target genes involved in bile acid transport and detoxification.
5 mg orally once daily, may increase to 10 mg once daily if tolerated after 3 months; maximum dose 10 mg daily.
5 mg orally once daily, increase to 10 mg once daily if adequate response after 3 months.
None Documented
None Documented
Clinical Note
moderateTizanidine + Obeticholic acid
"The serum concentration of Obeticholic acid can be increased when it is combined with Tizanidine."
Terminal elimination half-life is approximately 24 hours (range 14–36 h) in patients with primary biliary cholangitis, allowing once-daily dosing. Steady-state is achieved in about 2 weeks.
The terminal elimination half-life of obeticholic acid is approximately 24 hours for the parent drug and 3.5 to 5.8 days for its active conjugates (glyco- and tauro-obeticholic acid). This long half-life supports once-daily dosing but indicates that steady-state is reached after about 2 weeks.
Primarily biliary, with minimal renal excretion (<3%). The drug and its conjugates are eliminated in feces following biliary secretion. Enterohepatic recirculation occurs.
Following oral administration, approximately 87% of the dose is excreted in feces (primarily as unchanged drug and metabolites) and less than 3% is excreted renally. Biliary excretion is the major route for the parent drug and its conjugates.
Category C
Category C
Farnesoid X receptor agonist
Farnesoid X receptor agonist