Linerixibat
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From MedlinePlus, U.S. National Library of Medicine
Ileal Bile Acid Transporter Inhibitor
Dosing in kidney impairment
Renal Impairment The recommended dosage in patients with renal impairment is the same as in patients with normal renal function because systemic absorption of linerixibat is minimal and has negligible recovery in urine [see Clinical Pharmacology ] . The safety and effectiveness of LYNAVOY have not been studied in patients with severe renal impairment (estimated glomerular filtration rate [eGFR] <30 mL/min/1.73 m 2 ), including those on hemodialysis.
Dosing in liver impairment
Hepatic Impairment The recommended dosage in patients with mild hepatic impairment (Child-Pugh A) is the same as in patients with normal hepatic function. The efficacy and safety of LYNAVOY have not been evaluated in patients with moderate and severe hepatic impairment (Child-Pugh B and C) with decompensated cirrhosis or those with decompensation events [see Clinical Pharmacology , Clinical Studies ].
Avoid use of LYNAVOY in patients with decompensated cirrhosis or those with prior or active decompensation events (e.g. variceal hemorrhage, ascites, hepatic encephalopathy).
Preparation and administration
Administration Modification for Concomitant Use with Bile Acid Binding Resins Administer LYNAVOY at least 4 hours before or 4 hours after taking a bile acid binding resin [see Drug Interactions , Clinical Pharmacology ] .
Drug interactions
Check linerixibat against a medication listLabel text (2 paragraphs)
Bile Acid Binding Resins : Administer at least 4 hours before or 4 hours after administration of LYNAVOY. ( 7.1 )
7.1 Effects of Bile Acid Binding Resins on LYNAVOY Instruct patients to take LYNAVOY at least 4 hours before or 4 hours after taking a bile acid binding resin [see Dosage and Administration (2.2) ] . Based on in vitro data, bile acid resins may bind linerixibat in the gut [see Clinical Pharmacology (12.3) ]. Concomitant use of bile acid binding resins with LYNAVOY can potentially inhibit the effects of LYNAVOY on the ileal bile acid transporter (IBAT).
Contraindications
None. None. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
E*Likelihood score E*: Suspected but unproven cause of clinically apparent liver injury.
Linerixibat is an orally available inhibitor of the ileal bile salt transporter which is used to treat severe pruritus in patients with primary biliary cholangitis. Linerixibat therapy is associated with transient serum enzyme fluctuations particularly with long term therapy but has not been linked to instances of clinically apparent liver injury with jaundice, although experience with its use has been limited.
ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary There are no data on the use of LYNAVOY in pregnant women to inform a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. Use of LYNAVOY during pregnancy is expected to result in minimal fetal exposure because systemic absorption following oral administration is low [see Clinical Pharmacology (12.3) ] . Linerixibat may inhibit the absorption of fat-soluble vitamins [see Warnings and Precautions (5.3) , Clinical Considerations ] .
In animal reproduction studies, in which linerixibat was administered orally to pregnant rabbits and rats during the period of organogenesis, no malformations or effects on embryo-fetal survival were reported at exposures 470 and 1,100 times the recommended human dose, respectively (see Data ) . The background risk of birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
There is a pregnancy safety study that monitors pregnancy exposures and outcomes in women who have taken LYNAVOY during pregnancy. Pregnant women exposed to LYNAVOY, or their healthcare providers, should report LYNAVOY exposure by contacting Intercept Pharmaceuticals at 1-844-782-4278. Clinical Considerations Fetal/Neonatal Adverse Reactions Linerixibat may inhibit the absorption of fat-soluble vitamins (FSV). FSV are essential for normal fetal growth and development. Monitor pregnant patients for FSV deficiency and supplement as needed. Increased supplementation of FSVs may be needed during pregnancy [see Warnings and Precautions (5.3) ] .
Data Animal Data No effects on embryo-fetal development were observed in pregnant rats treated orally with linerixibat up to 1,000 mg/kg/day (approximately 1,100 times the recommended dose based on AUC [area under the plasma concentration-time curve]) or in pregnant rabbits treated orally with linerixibat up to 125 mg/kg/day (approximately 470 times the recommended dose based on AUC) during the period of organogenesis. No effects on postnatal development were observed in a pre- and postnatal development study, in which female rats were treated orally with linerixibat up to 1,000 mg/kg/day during organogenesis through lactation.
Maternal systemic exposure to linerixibat at the maximum dose tested was approximately 1,100 times the recommended human dose based on AUC.
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
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