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elafibranor (Iqirvo)

Indications: - treatment of primary biliary cholangitis combination with ursodeoxycholic acid - monotherapy in patients unable to tolerate ursodeoxycholic acid Contraindications: - pregnancy - not recommended in patients who have or develop decompensated cirrhosis Dosage: - 80 mg PO QD with or without food - 80 mg Oral Tablet - no specific geriatric dosing recommended - no dosage adjustment for renal failure Adverse effects: - myalgia, myopathy, rhabdomyolysis - increased risk of fractures - fetal toxicity - > 5% - weight gain/ weight loss, diarrhea, abdominal pain, nausea/vomiting, arthralgia, constipation, GERD, dry mouth, rash Drug interactions: - weak CYP3A4 inducer Mechanism of action: - peroxisome proliferator-activated receptor agonist (PPAR agonist) - elafibranor & its active metabolite activate PPAR-alpha, PPAR-gamma, & PPAR-delta - reduces serum alkaline phosphatase - signaling pathway for PPAR-delta includes FGF21-dependent downregulation of CYP7A1, the key enzyme for synthesis of bile acids from cholesterol * improvement in survival or prevention of liver failure has not been demonstrated

General

receptor agonist gastrointestinal agent

Database Correlations

PUBCHEM correlations

References

  1. Kowdley KV, Bowlus CL, Levy C et al Efficacy and Safety of Elafibranor in Primary Biliary Cholangitis. N Engl J Med. 2024 Feb 29;390(9):795-805 PMID: 37962077 Clinical Trial. https://www.nejm.org/doi/10.1056/NEJMoa2306185
  2. HIGHLIGHTS OF PRESCRIBING INFORMATION IQIRVO (elafibranor) tablets, for oral use https://d2rkmuse97gwnh.cloudfront.net/a88aa6d6-3ca0-4362-a711-d53c45ae33ff/c91c4c2d-fbd6-4dec-99db-66768cdb2b5c/c91c4c2d-fbd6-4dec-99db-66768cdb2b5c_source__v.pdf