pharmacopeia
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Mechanism of action

Sourced from openFDA

Elafibranor and its main active metabolite GFT1007 are peroxisome proliferator-activated receptor (PPAR) agonists, both of which activate PPAR-alpha, PPAR-gamma, and PPAR-delta in vitro. However, the mechanism by which elafibranor exerts its therapeutic effects in patients with PBC is not well understood.

Peroxisome Proliferator-activated ReceptorPeroxisome Proliferator-activated Receptor alphaPeroxisome Proliferator-activated Receptor deltaPeroxisome Proliferator-activated Receptor gamma

Indications

Sourced from openFDA
  • IQIRVO is indicated for the treatment of primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults who have had an inadequate response to UDCA, or as monotherapy in patients unable to tolerate UDCA. This indication is approved under accelerated approval based on reduction of alkaline phosphatase (ALP) [see Clinical Studies (14) ] .

Contraindications

Sourced from openFDA
  • None. None.contraindicated

Dosage & administration

Sourced from openFDA

Before treatment, evaluate for muscle pain or myopathy, and/or verify that females of reproductive potential are not pregnant. ( 2.1 ) The recommended dosage is 80 mg orally once daily with or without food. ( 2.2 ) 2.1 Recommended Evaluation Before Initiating IQIRVO Before initiating IQIRVO: Evaluate for muscle pain or myopathy [see Warnings and Precautions (5.1) ] . Verify that females of reproductive potential are not pregnant prior to initiating treatment with IQIRVO [ see Warnings and Precautions (5.3) , Use in Specific Populations (8.1 , 8.3) ] . 2.2 Recommended Dosage and Administration The recommended dosage of IQIRVO is 80 mg taken orally once daily with or without food [see Clinical Pharmacology (12.3) ] . 2.3 Administration Modification for Bile Acid Sequestrants Administer IQIRVO at least 4 hours before or 4 hours after administering the bile acid sequestrant, or at as great an interval as possible [see Drug Interactions (7.2) ] .

Warnings & precautions

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Myalgia, Myopathy, and Rhabdomyolysis : Assess for muscle pain and myopathy prior to IQIRVO initiation. Consider periodic assessment (clinical exam, CPK measurement). Interrupt IQIRVO if there is new onset or worsening of muscle injury, or muscle pain. ( 5.1 ) Fractures: The risk of fracture should be considered in the care of patients treated with IQIRVO. Apply current standards of care for assessing and maintaining bone health. ( 5.2 ) Adverse Effects on Fetal and Newborn Development : May cause fetal harm. Verify that a female of reproductive potential is not pregnant prior to initiating IQIRVO. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception. ( 5.3 , 8.1 , 8.3 ) Drug-Induced Liver Injury : Obtain clinical and laboratory assessments at treatment initiation and monitor thereafter according to routine patient management. Interrupt the treatment if liver tests worsen, or patients develop signs and symptoms consistent with clinical hepatitis. Consider permanent discontinuation if liver tests worsen after restarting IQIRVO. ( 5.4 ) Hypersensitivity Reactions : If severe hypersensitivity reactions occur, permanently discontinue IQIRVO. If a mild or moderate hypersensitivity reaction occurs, interrupt IQIRVO and treat promptly. Monitor until signs and symptoms resolve. ( 5.5 ) Biliary Obstruction : Avoid use in patients with complete biliary obstruction. If biliary obstruction is suspected, interrupt IQIRVO and treat as clinically indicated.

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are described elsewhere in the labeling: Myalgia, Myopathy, and Rhabdomyolysis [see Warnings and Precautions (5.1) ] Fractures [see Warnings and Precautions (5.2) ] Drug-Induced Liver Injury [see Warnings and Precautions (5.4) ] Hypersensitivity Reactions [see Warnings and Precautions (5.5) ] Most common adverse reactions with IQIRVO (reported in ≥ 5% and higher compared to placebo) are weight gain, diarrhea, abdominal pain, nausea, vomiting, arthralgia, constipation, muscle injury, fracture, gastroesophageal reflux disease, dry mouth, weight loss, and rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Ipsen Biopharmaceuticals, Inc. at 1-855-463-5127 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of IQIRVO is based on Study 1 consisting of 161 patients who were randomized to receive IQIRVO 80 mg (n=108) or placebo (n=53) once daily with a median duration of exposure during the double-blind period of 62 weeks (inter quartile range: 52, 84) [see Clinical Studies (14) ] . IQIRVO or placebo was administered in combination with UDCA in 95% of patients and as monotherapy in 5% of patients who were unable to tolerate UDCA.

Use in specific populations

Sourced from openFDA

Lactation: Advise not to breastfeed during treatment and for 3 weeks after last dose. ( 8.2 ) Hepatic Impairment: Monitor patients with cirrhosis for evidence of decompensation. Consider discontinuation if patient progresses to moderate or severe hepatic impairment (Child-Pugh B or C). ( 8.7 ) 8.1 Pregnancy Risk Summary Based on data from animal reproduction studies, IQIRVO may cause fetal harm when administered during pregnancy. Treatment of pregnant rats with elafibranor during organogenesis through lactation resulted in stillbirths, reduced survival, decrease in pup body weight, and/or blue/black discoloration of the caudal section of body, which occurred at maternal plasma drug exposures lower than or approximately equal to human exposure at the recommended dose ( see Data ). There are insufficient data from human pregnancies exposed to IQIRVO to allow an assessment of a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Pharmacokinetics

Sourced from openFDA
Metabolism
Following once daily dosing, steady state of elafibranor was achieved by Day 14, while steady state of GFT1007 was achieved by Day 7. The pharmacokinetics (PK) of elafibranor and GFT1007 were time-independent after 16-day repeated administration.

Approval history

Sourced from openFDA
  • Jun 10, 2024NDANDA218860Ipsen

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
616 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue7011%
  2. 2Pruritus569.1%
  3. 3Nausea558.9%
  4. 4Constipation498.0%
  5. 5Product Dose Omission Issue498.0%
  6. 6Weight Increased467.5%
  7. 7Arthralgia447.1%
  8. 8Myalgia437.0%
  9. 9Diarrhoea416.7%
  10. 10Headache315.0%
  11. 11Muscle Spasms304.9%
  12. 12Dizziness284.5%
  13. 13Off Label Use264.2%
  14. 14Vomiting264.2%
  15. 15Abdominal Pain Upper254.1%

Clinical trials

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The 10 most recently updated of 27 ClinicalTrials.gov registrations naming Elafibranor as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Elafibranor work?
Elafibranor and its main active metabolite GFT1007 are peroxisome proliferator-activated receptor (PPAR) agonists, both of which activate PPAR-alpha, PPAR-gamma, and PPAR-delta in vitro. However, the mechanism by which elafibranor exerts its therapeutic effects in patients with PBC is not well understood.
What is Elafibranor used for?
According to FDA labeling, Elafibranor carries indications including: IQIRVO is indicated for the treatment of primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults who have had an inadequate response to UDCA, or as monotherapy in patients unable to tolerate UDCA. This indication is approved under accelerated approval based on reduction of alkaline phosphatase (ALP) [see Clinical Studies (14) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Elafibranor?
Elafibranor is classified as Other drugs for bile therapy, Peroxisome Proliferator-activated Receptor Agonist, Cytochrome P450 3A4 Inducers, Peroxisome Proliferator-activated Receptor Agonists, Peroxisome Proliferator-activated Receptor alpha Agonists, Peroxisome Proliferator-activated Receptor delta Agonists, Peroxisome Proliferator-activated Receptor gamma Agonists, Cholagogue Activity.
What are the brand names for Elafibranor?
Elafibranor is marketed under brand names including Iqirvo.
What are the contraindications for Elafibranor?
Elafibranor labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
Note. Data for elafibranor is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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