Elafibranor is used alone or in combination with ursodiol to treat primary biliary cholangitis type of liver disease that destroys bile ducts, which allows bile to stay in the liver and cause damage. It is classified as a peroxisome proliferator-activated receptor (PPAR) agonist. The U.S. FDA approved it in June 2024, and it received conditional approval from the European Commission in September 2024.
BRAND NAMES:
Iqirvo – It is available in the form of oral tablets containing Elafibranor as the main active ingredient with strength 80mg.
MECHANISM OF ACTION:
Elafibranor functions as a dual agonist of peroxisome proliferator-activated receptors (PPAR) alpha (α) and delta (δ), which are nuclear receptors involved in regulating lipid metabolism, glucose balance, and inflammatory responses. Through activation of these receptors, Elafibranor improves insulin sensitivity, lowers liver inflammation, and enhances lipid metabolic processes.
PHARMACOKINETICS:
Absorption: It takes 1.25 hours to reach its maximum peak plasma concentration. High fat, high calorie meal delays Tmax by 30 minutes for Elafibranor and 1 hour for its active metabolite.
Distribution: Approximately 4731 L, indicating extensive tissue distribution. Both Elafibranor and GFT1007 are highly bound to plasma proteins (~99.7%), primarily serum albumin.
Metabolism: Elafibranor is metabolized by the enzyme prostaglandin reductase 1 (PTGR1) to produce its active metabolite, GFT1007. Neither elafibranor nor GFT1007 undergo significant metabolism by major cytochrome P450 (CYP) enzymes or UDP-glucuronosyltransferase (UGT) isoforms.
Excretion: 77.1% of the dose is excreted through feces and 19.3% of the drug is excreted through urine.
PHARMACODYNAMICS:
The pharmacodynamics of elafibranor centers on its dual agonism of peroxisome proliferator-activated receptors (PPARs) α and δ, which are nuclear receptors involved in regulating lipid metabolism, glucose homeostasis, and inflammation.
DOSAGE AND ADMINISTRATION:
Elafibranor is available in the form of oral tablets with strength 80mg. The dose of this medicine will be different for different patients. The amount of medicine that patient should take depends on the strength of the medicine also the number of doses taken each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
For treatment of primary biliary cholangitis, In adults the recommended dose is 80mg once a day.
DRUG INTERACTIONS:
Some drugs should be avoiding while taking Elafibranor as few drugs interact and can cause severe side effects. Below are few drugs that should be avoid while taking Elafibranor.
- Hormonal contraceptives - Birth control pills.
- Bile aid binding resins – Cholestyramine, Colestipol
- HMG-CoA reductase inhibitors – Atorvastatin, pravastatin, lipostatin
- Telithromycin
- Maraviroc
- Rifampin
CONTRAINDICATIONS:
Elafibranor is contraindicated in patients with severe hepatic impairment and contraindicated to Elafibranor components.
ADVERSE EFFECTS:
- Bone fractures
- Gastroesophageal reflux disease
- Muscle problems
- Joint pain
- Nausea and vomiting
- Constipation
- Weight gain
- Weight loss
- Rashes on skin
- Diarrhea
OVERDOSE:
Taking overdose of Elafibranor can cause toxic effects.
- Seizures.
- Rapid heartbeat
