Generic Name and Formulations:
Obeticholic acid 5mg, 10mg; tabs.
Indications for OCALIVA:
Treatment of primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults with inadequate response to UDCA, or as monotherapy in adults unable to tolerate UDCA.
Non-cirrhotic or compensated Child-Pugh Class A: initially 5mg once daily; increase to 10mg once daily if inadequate reduction in ALP and/or total bilirubin after 3 months and tolerated the drug; max 10mg once daily. Child-Pugh Class B or C, or with prior decompensation event: initially 5mg once weekly; increase to 5mg twice weekly (≥3 days apart) then to 10mg twice weekly (≥3 days apart) if inadequate reduction in ALP and/or total bilirubin after 3 months and tolerated the drug; max 10mg twice weekly. Intolerable pruritus: consider adding an antihistamine or bile acid binding resin; reduce dose and/or temporarily interrupt for up to 2 weeks based on Child-Pugh classification (see full labeling).
Complete biliary obstruction.
Risk of hepatic decompensation and failure in PBC patients with Child-Pugh Class B or C hepatic impairment or decompensated cirrhosis when dosed more frequently than recommended doses; monitor closely. Determine Child-Pugh classification prior to initiation; re-evaluate during treatment to determine if dose adjustment is needed. Interrupt if evidence of worsening liver function and monitor; consider discontinuing if clinically significant liver-related adverse reactions occur. Gastroenteritis. Discontinue if complete biliary obstruction develops. Consider evaluation of those with new onset or worsening severe pruritus. Monitor for changes in serum lipid levels. If unresponsive after 1 year of treatment at max tolerable dose (10mg once daily) and experienced HDL-C reduction, re-evaluate. Pregnancy. Nursing mothers.
Avoid concomitant bile salt efflux pump (BSEP) inhibitors (eg, cyclosporine); if co-administration necessary, monitor LFTs. Separate dosing by ≥4hrs or at greatest possible interval with bile acid binding resins (eg, cholestyramine, colestipol, colesevelam). Monitor INR and adjust dose as needed when concomitant warfarin. Concomitant CYP1A2 substrates with narrow therapeutic index (eg, theophylline, tizanidine); monitor.
Farnesoid X receptor (FXR) agonist.
Pruritus (may be severe), fatigue, abdominal pain/discomfort, rash, oropharyngeal pain, dizziness, constipation, arthralgia, thyroid function abnormality, eczema; liver-related effects, HDL-C reduction.