elafibranor

Absorption: Extent of absorption following oral administration unknown.

Distribution: Extensively distributed to tissues.

Protein Binding: 99.7%.

Metabolism/Excretion: Extensively metabolized by the liver via 15-ketoprostaglandin 13-Δ, CYP2J2, UGT1A3, UGT1A4, and UGT2B7 to an active metabolite (GFT1007). GFT1007 is further metabolized by CYP2C8, UGT1A3, and UGT2B7. 77% excreted in feces (57% as unchanged drug); 19% excreted in urine (mostly as metabolites).

Half-Life: Elafibranor: 70.2 hr; GFT1007: 15.4 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1.25 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Complete biliary obstruction;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults >75 yr may have ↑ risk of adverse reactions.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash

GI: abdominal pain, diarrhea, nausea, vomiting, ↑liver enzymes, cholelithiasis, constipation, dry mouth, gastroenteritis, gastroesophageal reflux disease

GU: ↑serum creatinine

Hemat: anemia

Metab: weight gain, weight loss

MS: ↑CK, arthalgia, fracture, myalgia, myopathy, pain, RHABDOMYOLYSIS

Neuro: dizziness

Misc: hypersensitivity reactions

Interactions ⬆ ⬇

Drug-drug:

May ↓ levels and effectiveness of hormonal contraceptives; change to nonhormonal contraceptive or barrier method.
HMG-CoA reductase inhibitors may ↑ risk of myopathy.
Rifampin may ↓ levels and effectiveness.
Bile acid sequestrants, including cholestyramine or colesevelam, may ↓ absorption and effectiveness; administer elafibranor ≥4 hr before or after bile acid sequestrants.

Route/Dosage ⬆ ⬇

PO (Adults ): 80 mg once daily.

Availability ⬆ ⬇

Assessment ⬆ ⬇

Monitor for myalgia, myopathy, and rhabdomyolysis. Assess for muscle pain and myopathy before starting therapy. Perform periodic clinical assessment. Hold therapy if new onset or worsening of muscle injury or muscle pain occur.
Assess for fractures. The risk of fracture should be considered in the care. Apply current standards of care for assessing and maintaining bone health.

Lab Test Considerations:

Verify negative pregnancy test before starting therapy.
Obtain baseline liver function tests (ALT, AST, total bilirubin, alkaline phosphatase). If liver function tests worsen or the patient develops signs/symptoms of hepatitis (jaundice, upper-right quadrant pain, eosinophilia), hold therapy. Consider permanent discontinuation if liver tests worsen after restarting.
May ↑ CK.

Implementation ⬆ ⬇

PO: Administer with or without food. Administer >4 hr before or after administering a bile acid sequestrant.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Advise patient of signs/symptoms of rhabdomyolysis. Inform patients to report immediately to health care professional of any unexplained muscle symptoms (pain, soreness, weakness).
Inform patient of ↑ risk of bone fractures. Advise patient to report any fractures to a health care professional.
Inform patient of the risk of liver injury. Instruct patient to report any signs/symptoms of liver injury (loss of appetite, nausea, ↑ fatigue, lower extremity edema, abdominal swelling, jaundice/icterus) to health care professional.
Advise patient to seek immediate medical care if hypersensitivity reactions, such as rash, occurs.
Instruct patient to immediately report any signs/symptoms of biliary obstruction (upper-right quadrant pain, jaundice) to health care professional. Treatment may be interrupted while the patient is being evaluated.
Rep: May cause fetal harm. Advise women of reproductive potential to switch to effective nonhormonal contraceptives or add a barrier method when using hormonal contraceptives during therapy and for >3 wk after last dose. Advise women not to breastfeed during treatment and for 3 wk after last dose. Inform patient to report pregnancy to Ipsen Biopharmaceuticals, Inc. at 1-855-463-5217.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇