Lynavoy Linerixibat 40 mg Tablet, Film Coated, 60-count
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Ileal Bile Acid Transporter Inhibitor class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
Linerixibat is used to treat itching in people with primary biliary cholangitis (PBC; a type of liver disease that harms bile ducts). Linerixibat is in a class of medications called ileal bile acid transporter inhibitors. It works by decreasing absorption of bile acids into the body allowing them to be eliminated in feces.
Read the full MedlinePlus article ↗- Lynavoy is meant to reduce the intense, chronic itch that comes with primary biliary cholangitis (PBC). That itch happens because bile acids build up in your body due to liver dama...
- What exactly is Lynavoy supposed to do for me?
- Yes, timing matters with Lynavoy. You take it twice a day, and the key rule is to swallow the tablet whole at least 30 minutes before eating or drinking anything other than water....
- How do I take it — is there a special way or timing I need to follow?
Patient education
Supplement & herbal interactions
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Ask a licensed pharmacist directly — free, answered by our team.
💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
Where does this data come from?
IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Lynavoy 40 mgthis 69516-0140-60 | Intercept | 60 tablets | — | — | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 9040518 ↗ | Drug substance | — | Sep 6, 2031 |
| Code | What it grants | Expires |
|---|---|---|
| NCE | New Chemical Entity (5-year) | Mar 17, 2031 |
| ODE-517 | Orphan Drug Exclusivity (7-year) | Mar 17, 2033 |
Is there a generic version of LYNAVOY 40 MG TABLET?
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 69516-0140-60 You're viewing this | 60 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (69516-140-60) | 2026-06-11 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available. |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
Questions about this listing
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE LYNAVOY is indicated for the treatment of cholestatic pruritus associated with primary biliary cholangitis (PBC) in adult patients. Limitations of Use Avoid use of LYNAVOY in patients with decompensated cirrhosis or those with prior or active hepatic decompensation events (e.g. variceal hemorrhage, ascites, hepatic encephalopathy) [see Use in Specific Populations (8.7) , Clinical Pharmacology (12.3) ] . LYNAVOY is an ileal bile acid transporter (IBAT) inhibitor indicated for the treatment of cholestatic pruritus associated with primary biliary cholangitis (PBC) in adult patients.
( 1 ) Limitations of Use Avoid use of LYNAVOY in patients with decompensated cirrhosis or those with prior or active hepatic decompensation events (e.g. variceal hemorrhage, ascites, hepatic encephalopathy). ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION The recommended dosage of LYNAVOY is 40 mg taken orally twice daily. Swallow tablets whole at least 30 minutes before any food or beverage (other than water). ( 2.1 )
2.1Recommended Dosage The recommended dosage of LYNAVOY is 40 mg orally twice daily. Swallow tablets whole at least 30 minutes before any food or beverage (other than water) [see Clinical Pharmacology (12.3) ] . If a dose is missed, take the missed dose as soon as possible and at least 30 minutes before your next meal, then resume the original dosing schedule.
If a dose is missed by more than 6 hours, skip the dose and resume the original dosing schedule. Do not take a double dose to make up for a missed dose.
2.2Administration 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 (7.1) , Clinical Pharmacology (12.3) ] .
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Tablets: 40 mg of linerixibat, purple, biconvex, round, film-coated tablets debossed with "GS 3JG" on one side. Tablets: 40 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Liver Test Elevations: Obtain baseline liver tests (alanine aminotransferase [ALT], aspartate aminotransferase [AST], total bilirubin [TB], direct bilirubin [DB], alkaline phosphatase [ALP]) and monitor the levels per standard clinical practice during treatment. If new liver test elevations occur, monitor ALT, AST, TB, DB, and ALP more frequently. For persistent liver test elevations, discontinue LYNAVOY.
( 5.1 ) Diarrhea: Diarrhea may occur. Advise patient to monitor for dehydration. Treatment interruption or discontinuation may be required if diarrhea persists.
( 5.2 ) Fat-Soluble Vitamin (FSV) Deficiency: Obtain baseline levels and monitor during treatment. Supplement with FSV if deficiency is observed. If FSV deficiency persists or worsens despite FSV supplementation, consider permanent discontinuation of treatment.
( 5.3 ) Bleeding: Interrupt treatment with LYNAVOY if bleeding occurs. Optimize treatment of FSV deficiency and consider restarting LYNAVOY once the patient is clinically stable. Fracture: IBAT inhibitors have been associated with bone fractures.
Monitor bone health and ensure adequate FSV levels.
5.1Liver Test Elevations In Study 1, liver test elevations were observed more commonly in LYNAVOY-treated patients compared to placebo-treated patients [see Adverse Reactions (6.1) ] . Obtain baseline liver tests (alanine aminotransferase [ALT], aspartate aminotransferase [AST], total bilirubin [TB], direct bilirubin [DB], alkaline phosphatase [ALP]) prior to initiating treatment with LYNAVOY and monitor the levels per standard clinical practice for PBC patients during treatment with LYNAVOY. If new liver test elevations occur, monitor ALT, AST, TB, DB, and ALP more frequently.
If liver test elevations persist, discontinue LYNAVOY.
5.2Diarrhea Diarrhea was reported as the most common adverse reaction in patients treated with LYNAVOY [see Adverse Reactions (6.1) ] . If diarrhea occurs, advise patients to monitor for dehydration. Consider interrupting or discontinuing LYNAVOY treatment if diarrhea persists.
5.3Fat-Soluble Vitamin Deficiency LYNAVOY may adversely affect absorption of fat-soluble vitamins (FSV). FSV include vitamins A, D, E, and K [see Adverse Reactions (6.1) ]. Obtain serum FSV levels (vitamins A, D, and E) and INR prior to initiation of LYNAVOY and monitor the levels periodically during treatment, along with any clinical manifestations of FSV deficiency.
Supplement with FSV if FSV deficiency is diagnosed. Consider discontinuing LYNAVOY if FSV deficiency persists or worsens despite adequate FSV supplementation. Bleeding Bleeding was observed more frequently in LYNAVOY-treated patients compared to placebo-treated patients [see Adverse Reactions (6.1) ] .
If bleeding occurs, interrupt LYNAVOY treatment and evaluate for potential FSV deficiency. LYNAVOY can be restarted if FSV deficiency is corrected, levels are maintained, and bleeding has resolved. Bone Fracture IBAT inhibitors have been associated with bone fractures.
Monitor bone health and ensure adequate FSV levels.
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in labeling: Liver Test Elevations [see Warnings and Precautions (5.1) ] Diarrhea [see Warnings and Precautions (5.2) ] Fat-Soluble Vitamin Deficiency [see Warnings and Precautions (5.3) ] The most common adverse reactions (≥5%) are: diarrhea, abdominal pain, nausea, increased ALT, hemorrhage, increased AST, headache, dyspepsia, gastroesophageal reflux disease, abdominal distension, dizziness, and arthralgia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Intercept Pharmaceuticals 1-844-782-4278 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical 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 with rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of LYNAVOY is based on Study 1, a randomized, double-blind, placebo-controlled, 24-week study of LYNAVOY 40 mg administered orally twice daily [see Clinical Studies (14) ] . Drug discontinuation due to adverse reactions was seen more frequently in LYNAVOY-treated patients (14%) than in placebo-treated patients (5%).
Diarrhea, abdominal pain, ALT increase, and AST increase were the most common causes of treatment discontinuation. Common Adverse Reactions Table 1 displays the most common adverse reactions that occurred in at least 5% of LYNAVOY-treated patients in Study 1. Table 1.
Adverse Reactions Occurring in ≥5% of Adult Patients with PBC Treated with LYNAVOY in Study 1 (24 weeks), Safety Dataset Adverse reactions were only included in table above if they occurred more frequently in patients treated with LYNAVOY compared to placebo-treated patients. Adverse Reaction LYNAVOY (n = 119) n (%) Placebo (n = 118) n (%) Diarrhea Diarrhea includes diarrhea and frequent bowel movements. 74 (62) 21 (18) Abdominal pain Abdominal pain includes abdominal pain, abdominal pain upper, abdominal pain lower, abdominal discomfort.
31 (26) 12 (10) Nausea 12 (10) 11 (9) Increased alanine aminotransferase (ALT) 11 (9) 4 (3) Hemorrhage Hemorrhage includes contusion, ecchymosis, epistaxis, gastric hemorrhage, hematochezia, hemorrhagic disorder, intermenstrual bleeding, melena, petechiae, skin hemorrhage, vaginal hemorrhage, hematocrit decreased, and diarrhea hemorrhagic. 11 (9) 3 (3) Increased aspartate aminotransferase (AST) 10 (8) 1 (<1) Headache 10 (8) 4 (3) Dyspepsia 9 (8) 1 (<1) Gastroesophageal reflux disease 8 (7) 5 (4) Abdominal distension 8 (7) 6 (5) Dizziness 7 (6) 4 (3) Arthralgia 7 (6) 6 (5) Less Common Adverse Reactions Additional adverse reactions that occurred more frequently in the LYNAVOY group compared to placebo group, in less than <5% of patients, included hyperbilirubinemia, hypertriglyceridemia, urinary tract infections, and dry mouth.
Specific Adverse Reactions Liver Test Elevations In Study 1, liver test elevations (ALT, AST, TB, or ALP) were observed more commonly in LYNAVOY-treated patients 17 (14%) compared to placebo-treated patients 7 (6%). Six (5%) of LYNAVOY-treated patients discontinued treatment due to liver test elevations during the study, compared to 2 (2%) of placebo-treated patients. Elevations in ALT to more than 3 times baseline levels occurred in 8 (7%) of LYNAVOY-treated patients compared to 4 (3%) of placebo-treated patients.
Elevations in TB to more than 2 times baseline levels occurred in 9 (8%) of LYNAVOY-treated patients compared to 3 (3%) of placebo-treated patients. Diarrhea In Study 1, diarrhea was observed in 74 (62%) of patients in the LYNAVOY-treated group compared to 21 (18%) in the placebo-treated group. Most diarrhea events occurred within the first 20 days of initiating treatment.
Of those who experienced diarrhea, 56/74 (76%) of LYNAVOY-treated patients and 10/21 (48%) of placebo-treated patients, did so within the first 20 days. Of the patient…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Bile Acid Binding Resins : Administer at least 4 hours before or 4 hours after administration of LYNAVOY. ( 7.1 )
7.1Effects 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).
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy 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.
8.2Lactation Risk Summary Linerixibat has low absorption following oral administration, and exposure of the infant to linerixibat through breast milk is not expected at the recommended dosage [see Clinical Pharmacology (12.3) ]. There are no data on the presence of linerixibat in human milk, effects on the breastfed infant, or effects on milk production. LYNAVOY may reduce absorption of fat-soluble vitamins [see Warning and Precautions (5.3) ] .
Monitor maternal FSV levels and increase FSV intake if FSV deficiency is observed during lactation. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for LYNAVOY and any potential adverse effects on the breastfed child from LYNAVOY or from the underlying maternal condition.
8.4Pediatric Use The safety and efficacy of LYNAVOY have not been established in pediatric patients.
8.5Geriatric Use Of the 119 patients that received LYNAVOY in Study 1, 25 (21%) were aged 65 years and older and 3 (3%) were aged 75 years and older [see Clinical Studies (14) ] . No overall differences in safety or effectiveness were observed between patients 65 to less than 75 years of age and younger adult patients, but greater sensitivity of some older individuals cannot be ruled out [see Clinical Pharmacology (12.3) ] . Clinical studies of LYNAVOY did not include sufficient numbers of patients aged 75 and older to determine whether they respond differently f…
🤰 Pregnancy ▾
8.1Pregnancy 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.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and efficacy of LYNAVOY have not been established in pediatric patients.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 119 patients that received LYNAVOY in Study 1, 25 (21%) were aged 65 years and older and 3 (3%) were aged 75 years and older [see Clinical Studies (14) ] . No overall differences in safety or effectiveness were observed between patients 65 to less than 75 years of age and younger adult patients, but greater sensitivity of some older individuals cannot be ruled out [see Clinical Pharmacology (12.3) ] . Clinical studies of LYNAVOY did not include sufficient numbers of patients aged 75 and older to determine whether they respond differently from younger adult patients.
🆘 Overdosage ▾
10 OVERDOSAGE Dose-dependent increases in the incidence of gastrointestinal adverse reactions have been observed with LYNAVOY dosages 4.5-fold higher than the recommended dosage. There is no specific antidote for LYNAVOY. If an overdose occurs, discontinue LYNAVOY, monitor the patient for any signs and symptoms and institute general supportive measures as needed.
Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Linerixibat is a reversible inhibitor of the ileal bile acid transporter (IBAT). It decreases the reabsorption of bile acids in the terminal ileum leading to their increased fecal elimination. Cholestatic pruritus is a common symptom in patients with PBC, and the pathophysiology of pruritus in patients with PBC is not completely understood.
Although the complete mechanism by which linerixibat improves pruritus in PBC patients is unknown, it may involve inhibition of the IBAT as observed by a decrease in mediators of pruritus including serum bile acids [see Clinical Pharmacology (12.2) ] .
12.2Pharmacodynamics Linerixibat reduces total serum bile acids in healthy volunteers and PBC patients with cholestatic pruritus. In healthy volunteers, serum bile acids were reduced within 1 day of LYNAVOY treatment compared to placebo treatment. In Study 1, total serum bile acids were reduced from baseline over the 24-week treatment period in the LYNAVOY group when compared to the placebo group.
12.3Pharmacokinetics Due to the low systemic absorption of linerixibat, pharmacokinetic parameters cannot be reliably calculated at the recommended doses. Following a single dose administration of 40 mg of linerixibat, concentrations of linerixibat in healthy volunteers were below the limit of quantification (10 pg/mL) in the majority of plasma samples. Following multiple doses of linerixibat ranging from 3 mg (0.08 times the approved recommended dose) twice daily to 90 mg (2.25 times the approved recommended dose) twice daily in healthy volunteers, the majority of plasma samples were below the limit of quantification (1,000 pg/mL).
Absorption Linerixibat is minimally absorbed following oral administration and the absolute oral bioavailability of linerixibat is 0.05%. Following a single oral administration of linerixibat 40 mg in healthy adults under fasted conditions, median T max was 4.5 hours and mean linerixibat (%CV) C max and AUC 0-t were 31.1 pg/mL (173) and 105 h∙pg/mL (419), respectively. Following multiple doses of LYNAVOY 40 mg twice daily in PBC patients with cholestatic pruritus, the mean linerixibat C max (95% CI) was 922 pg/mL (347, 1,500).
Effect of Food Concomitant administration of a high-fat meal with a single dose of linerixibat 40 mg oral tablets delayed median T max from 4.5 hours to 8.0 hours and resulted in decreases of 21.9% and 33.7% in AUC 0-t and C max , respectively, compared to administration under fasted conditions in healthy adults. Pharmacokinetic parameters in the food effect study were highly variable. The effect of food on the changes of systemic exposures to linerixibat is not clinically significant.
Despite the lack of clinically important pharmacokinetic effects with food, LYNAVOY should be administered at least 30 minutes prior to food or beverage (other than water) to allow linerixibat to enter the gastrointestinal lumen prior to release of bile acids upon eating [see Dosage and Administration (2.1) ] . Distribution The in vitro plasma protein binding range of linerixibat was 71.0-76.4%. Elimination Following a single oral dose of linerixibat 90 mg (2.25 times the approved recommended dose) in healthy adults, the mean half-life (t 1/2 ) was 6.76 hours.
Metabolism: Following administration of oral radiolabeled linerixibat, no linerixibat metabolites were detected in plasma. Three minor oxidative metabolites were detected in feces, and each accounted for negligible radioactivity (<1%), demonstrating that linerixibat is minimally metabolized in humans. Excretion: Following administration of oral radiolabeled linerixibat, approximately 97% of the dose was excreted in feces; approximately 0.04% of the dose was excreted in urine.
More than 99% of fecal radioactivity was determined to be unchanged and unabsorbed linerixibat. Following intravenous administration of radiolabeled linerixibat, systemic linerixibat elimination was approximately 20% renal and 80% fecal.…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Linerixibat is a reversible inhibitor of the ileal bile acid transporter (IBAT). It decreases the reabsorption of bile acids in the terminal ileum leading to their increased fecal elimination. Cholestatic pruritus is a common symptom in patients with PBC, and the pathophysiology of pruritus in patients with PBC is not completely understood.
Although the complete mechanism by which linerixibat improves pruritus in PBC patients is unknown, it may involve inhibition of the IBAT as observed by a decrease in mediators of pruritus including serum bile acids [see Clinical Pharmacology (12.2) ] .
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied LYNAVOY (linerixibat) tablets, 40 mg, are purple, biconvex, round, film-coated tablets debossed with "GS 3JG" on one side and are supplied in bottles of 60 tablets (NDC 69516-140-60). LYNAVOY is packaged in white high density polyethylene (HDPE) bottles with polypropylene child-resistant closures and a polyethylene faced induction heat seal liner containing a HDPE canister with silica gel desiccant. Storage and Handling Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].
Store in the original package to protect from moisture. Keep the bottle tightly closed.
📦 Storage and Handling ▾
Storage and Handling Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Store in the original package to protect from moisture. Keep the bottle tightly closed.
📋 Description ▾
11 DESCRIPTION Linerixibat is an orally administered IBAT inhibitor. Linerixibat has the chemical name 3-((((3 R ,5 R )-3-butyl-3-ethyl-7-methyloxy-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydrobenzo[ f ][1,4]thiazepin-8-yl)methyl)amino)pentanedioic acid. The molecular formula of linerixibat is C 28 H 38 N 2 O 7 S with a molecular weight of 546.68 g/mol.
Linerixibat has the following chemical structure: "*" represent chiral centers. Linerixibat is a white to off-white solid. Its solubility in aqueous solutions is pH-dependent and varies from very slightly to slightly soluble.
LYNAVOY is available for oral administration as tablets containing 40 mg linerixibat and the following excipients: croscarmellose sodium, magnesium stearate and microcrystalline cellulose. The tablet film-coating contains black iron oxide, hypromellose, polyethylene glycol, red iron oxide, and titanium dioxide. Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Administration Instructions Instruct patients to take LYNAVOY at least 30 minutes before any food or beverage (other than water) [see Dosage and Administration (2.1) ] . Instruct patients that if they miss a dose of LYNAVOY to take it as soon as possible and at least 30 minutes before their next meal, then resume the original dosing schedule.
If a dose is missed by more than 6 hours, skip the dose and resume the original dosing schedule. Advise patients to not take a double dose to make up for a missed dose [see Dosage and Administration (2.1) ]. Instruct patients to take LYNAVOY at least 4 hours before or 4 hours after taking a bile acid binding resin [see Drug Interactions (7.1) ].
Liver Test Abnormalities Advise patients that their healthcare provider will obtain liver tests before starting LYNAVOY and periodically during treatment with LYNAVOY [see Warnings and Precautions (5.1) ]. Diarrhea Advise patients to monitor for dehydration. Consider interrupting or discontinuing LYNAVOY treatment if diarrhea persists. [see Warnings and Precautions (5.2) ] .
Fat-Soluble Vitamin (FSV) Deficiency Advise patients that INR (for vitamin K) and serum levels of vitamins A, D, E will be obtained before starting treatment and periodically during treatment to assess for FSV deficiency [see Warnings and Precautions (5.3) ] . Inform patients that they may bleed more easily or may bleed longer, and could develop bone fractures. Advise patients to call their healthcare provider for any signs or symptoms of bleeding, or if they have a bone fracture.
Pregnancy Inform patients that there is a pregnancy safety study tracking pregnancy exposures and outcomes with LYNAVOY. Ask pregnant women to report LYNAVOY exposure by contacting Intercept Pharmaceuticals at 1-844-782-4278. LYNAVOY is a trademark of GSK Group of Companies licensed to Intercept Pharmaceuticals, Inc.