baricitinib (Rx)

Brand and Other Names:Olumiant
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 2mg

Rheumatoid Arthritis

Indicated for adults with moderately to severely active rheumatoid arthritis (RA) who have had an inadequate response to one or more tumor necrosis factor (TNF) antagonist therapies

May be used as monotherapy or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs)

2 mg PO qDay

COVID-19 (EUA)

November 19, 2020: Emergency use authorization (EUA) issued by the FDA for use, in combination with remdesivir, for treatment of suspected or laboratory confirmed coronavirus disease 2019 (COVID-19) in hospitalized patients aged ≥2 years who require supplemental oxygen, invasive mechanical ventilation, or extracorporeal membrane oxygenation (ECMO)

Adults: 4 mg PO qDay

Recommended treatment duration is 14 days or until hospital discharge, whichever comes first; optimal treatment duration unknown

Dosage Modifications

Absolute lymphocyte count (ALC)

  • Rheumatoid arthritis
    • ALC ≥500 cells/mm3: Maintain dose
    • ALC <500 cells/mm3: Avoid initiation or interrupt dosing until ALC ≥500 cells/mm3
  • ​COVID-19
    • ALC ≥200 cells/mm3: Maintain dose
    • ALC <200 cells/mm3: Avoid initiation or interrupt dosing until ALC ≥200 cells/mm3

Absolute neutrophil count (ANC)

  • Rheumatoid arthritis
    • ANC ≥1000 cells/mm3: Maintain dose
    • ANC <1000 cells/mm3: Avoid initiation or interrupt dosing until ANC ≥1000 cells/mm3
  • COVID-19
    • ANC ≥500 cells/mm3: Maintain dose
    • ANC <500 cells/mm3: Avoid initiation or interrupt dosing until ANC ≥500 cells/mm3

Anemia

  • Rheumatoid arthritis
    • Hgb ≥8 g/dL: Maintain dose
    • Hgb <8 g/dL: Avoid initiation or interrupt dosing until Hgb ≥8 g/dL

Renal impairment

  • Rheumatoid arthritis
    • Moderate (eGFR 30-60 mL/min/1.73 m2): Decrease to 1 mg/day
    • Severe (eGFR <30 mL/min/1.73 m2): Not recommended (not studied)
  • COVID-19
    • eGFR ≥60 mL/min/1.73 m2: No dose adjustment
    • eGFR 30 to <60 mL/min/1.73 m2: Decrease to 2 mg/day
    • eGFR 15 to <30 mL/min/1.73 m2: Decrease to 1 mg/day
    • eGFR <15 mL/min/1.73 m2, patients on dialysis, have end-stage renal disease, or have acute kidney injury: Not recommended

Hepatic impairment

  • Rheumatoid arthritis
    • Mild or moderate: No dose adjustment required
    • Severe: Not recommended
  • COVID-19
    • Increased ALT/AST: Consider interruption until the diagnosis of drug-induced liver injury is excluded
    • Severe: Not studied; use only if benefits outweigh the risks

Coadministration with strong organic anion transporter 3 (OAT3) inhibitors (eg, probenecid)

  • Rheumatoid arthritis
    • Coadministration with baricitinib and OAT3 inhibitor (eg, probenecid): Decrease baricitinib to 1 mg/day
  • COVID-19
    • If recommended dose is 4 mg/day, reduce to 2 mg/day
    • If recommended dose is 2 mg/day, reduce to 1 mg/day
    • If recommended dose is 1 mg/day, consider discontinuing probenecid

Dosing Considerations

Rheumatoid arthritis

  • Do not initiate if ALC <500 cells/mm3, ANC <1000 cells/mm3, or Hgb level <8 g/dL
  • Avoid in patients with active, serious infection, including localized infections
  • Before initiating, test patients for latent tuberculosis (TB); if positive, consider treating for TB prior to initiating
  • Not recommended for use in combination with other janus kinase (JAK) inhibitors, biologic DMARDs, or with potent immunosuppressants (eg, azathioprine, cyclosporine)

COVID-19

  • Evaluate baseline eGFR, liver enzymes, and CBC count to determine treatment suitability and dose
  • Monitor closely patients with abnormal baseline and post-baseline laboratory values
  • Not recommended with known active TB
  • Data are limited in patients receiving systemic corticosteroids
  • Has not been studied in combination with other JAK inhibitors or with biologic DMARDs (biologic treatments targeting cytokines, B-cells, or T-cells)

Dosage Forms & Strengths

tablet

  • 1mg
  • 2mg

COVID-19 (EUA)

November 19, 2020: Emergency use authorization (EUA) issued by the FDA for use, in combination with remdesivir, for treatment of suspected or laboratory confirmed coronavirus disease 2019 (COVID-19) in hospitalized patients aged ≥2 years who require supplemental oxygen, invasive mechanical ventilation, or extracorporeal membrane oxygenation (ECMO)

2 to <9 years: 2 mg PO qDay

≥9 years: 4 mg PO qDay

Recommended treatment duration is 14 days or until hospital discharge, whichever comes first; optimal treatment duration unknown

Dosage Modifications

Absolute lymphocyte count (ALC)

  • ​COVID-19
    • ALC ≥200 cells/mm3: Maintain dose
    • ALC <200 cells/mm3: Avoid initiation or interrupt dosing until ALC ≥200 cells/mm3

Absolute neutrophil count (ANC)

  • COVID-19
    • ANC ≥500 cells/mm3: Maintain dose
    • ANC <500 cells/mm3: Avoid initiation or interrupt dosing until ANC ≥500 cells/mm3

Renal impairment

  • COVID-19 (2-9 years)
    • eGFR ≥60 mL/min/1.73 m2: No dose adjustment
    • eGFR 30 to <60 mL/min/1.73 m2: Decrease to 1 mg/day
    • eGFR 15 to <30 mL/min/1.73 m2: Not recommended
    • eGFR <15 mL/min/1.73 m2, patients on dialysis, have end-stage renal disease, or have acute kidney injury: Not recommended
  • COVID-19 (≥9 years)
    • eGFR ≥60 mL/min/1.73 m2: No dose adjustment
    • eGFR 30 to <60 mL/min/1.73 m2: Decrease to 2 mg/day
    • eGFR 15 to <30 mL/min/1.73 m2: Decrease to 1 mg/day
    • eGFR <15 mL/min/1.73 m2, patients on dialysis, have end-stage renal disease, or have acute kidney injury: Not recommended

Hepatic impairment

  • COVID-19
    • Increased ALT/AST: Consider interruption until the diagnosis of drug-induced liver injury is excluded
    • Severe: Not studied; use only if benefits outweigh the risks

Coadministration with strong organic anion transporter 3 (OAT3) inhibitors (eg, probenecid)

  • COVID-19
    • If recommended dose is 4 mg/day, reduce to 2 mg/day
    • If recommended dose is 2 mg/day, reduce to 1 mg/day
    • If recommended dose is 1 mg/day, consider discontinuing probenecid

Dosing Considerations

Evaluate baseline eGFR, liver enzymes, and CBC count to determine treatment suitability and dose

Monitor closely patients with abnormal baseline and post-baseline laboratory values

Not recommended with known active TB

Data are limited in patients receiving systemic corticosteroids

Has not been studied in combination with other JAK inhibitors or with biologic DMARDs (biologic treatments targeting cytokines, B-cells, or T-cells)

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Interactions

Interaction Checker

and baricitinib

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Upper respiratory tract infections (16.3%)

            1-10%

            Nausea (2.7%)

            Increased LFTs (1-2%)

            Platelet elevations (1-2%)

            Herpes zoster infection (1%)

            <1%

            Acne (<1%)

            Herpes simplex infection (0.8%)

            Neutropenia (0.3%)

            Postmarketing Reports

            Immune System Disorders: Drug hypersensitivity (eg, rash, urticaria, angioedema)

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            Warnings

            Black Box Warnings

            Serious infections

            • Baricitinib increases risk for developing serious infections that may lead to hospitalization or death
            • Most patients who developed these infections were taking concomitant immunosuppressants (eg, methotrexate, corticosteroids)
            • If a serious infection develops, interrupt dosing until the infection is controlled
            • Reported infections include:
              • Active TB, which may present with pulmonary or extrapulmonary disease; test patients for latent TB before initiating and during therapy; treatment for latent infection should be considered before initiating
              • Invasive fungal infections, including candidiasis and pneumocystosis; patients with invasive fungal infections may present with disseminated, rather than localized, disease
              • Bacterial, viral, and other infections due to opportunistic pathogens
            • Consider risks and benefits before initiating therapy in patients with chronic or recurrent infection
            • Closely monitor for developing signs and symptoms of infection during and after treatment, including the possible development of TB in patients who tested negative for latent TB before initiating baricitinib

            Malignancies

            • Lymphoma and other malignancies observed

            Thrombosis

            • Thrombosis, including deep venous thrombosis (DVT) and pulmonary embolism (PE), observed at an increased incidence in patients treated with baricitinib compared with placebo
            • Additionally, cases of arterial thrombosis reported
            • Many of these adverse events were serious and some resulted in death
            • Patients with symptoms of thrombosis should be promptly evaluated

            Contraindications

            None

            Cautions

            Serious and sometimes fatal infections may develop owing to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens reported; may cause reactivation of latent TB or viral infections (see Black Box Warnings and Dosing Considerations)

            Reactions such as angioedema, urticaria, and rash, including serious reactions, that may reflect drug hypersensitivity, reported; if a serious hypersensitivity reaction occurs, promptly discontinue therapy while evaluating potential causes of the reaction

            Consider risks and benefits before initiating in patients with chronic or recurrent infection, history of serious or opportunistic infection, underlying conditions predisposing them to infection, or patients who have been exposed to tuberculosis or have resided or traveled in areas of endemic tuberculosis or mycoses (see Black Box Warnings)

            Consider TB therapy for patients with a negative test for latent TB but who have risk factors for TB infection; consultation with a physician with expertise in TB recommended to aid in decision about whether initiating anti-TB therapy is appropriate

            If a new infection develops during treatment, promptly initiate diagnostic tests appropriate for an immunocompromised patient; if necessary, initiate appropriate antimicrobial therapy and closely monitor; interrupt baricitinib therapy if patient unresponsive to treatment

            If herpes zoster occurs, interrupt treatment until episode resolves

            Malignancies were observed in clinical studies; non-melanoma skin cancers (NMSCs) reported; periodic skin examination is recommended for patients who are at increased risk for skin cancer

            Perform screening for viral hepatitis in accordance with clinical guidelines before starting therapy; unknown impact on chronic viral hepatitis reactivation

            Increased incidence of thrombosis, including DVT and PE, observed compared with placebo; caution in patients at increased risk of thrombosis (see Black Box Warnings)

            Gastrointestinal perforation reported in clinical studies, although the role of JAK inhibition in these events is unknown

            May increase incidence of neutropenia, lymphopenia, anemia, or elevated LFTs or lipids; monitor laboratory values at baseline and periodically during treatment

            Prompt investigation of cause of liver enzyme elevation recommended to identify potential cases of drug-induced liver injury; if increases in ALT or AST are observed and drug-induced liver injury is suspected, interrupt therapy until this diagnosis is excluded

            Drug interaction overview

            • Avoid use of live vaccines; update immunizations in agreement with current immunization guidelines before initiating
            • Coadministration with strong OAT3 inhibitors may increase baricitinib systemic exposure
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            Pregnancy

            Pregnancy

            Data in pregnant women are insufficient to inform a drug-associated risk for major birth defects or miscarriage

            Animal studies

            • In animal embryo-fetal development studies, oral baricitinib administration to pregnant rats and rabbits at exposures equal to and greater than ~20 and 84 times the maximum recommended human dose (MRHD), respectively, resulted in reduced fetal body weights, increased embryo lethality (rabbits only), and dose-related increases in skeletal malformations

            Lactation

            Unknown if distributed in human breast milk

            Baricitinib is present in the milk of lactating rats

            Owing to species-specific differences in lactation physiology, the clinical relevance of these data are not clear

            Because of the potential for serious adverse reactions in nursing infants, advise women not to breastfeed while taking baricitinib

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Janus kinases (JAKs) pathways inhibitor; JAK consists of a group of intracellular tyrosine kinases that transmit signals from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoieses and immune cell function

            Within the signaling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs), which modulate intracellular activity including gene expression; baricitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs

            Absorption

            Absolute bioavailability: 80%

            Peak plasma time: 1 hr

            Steady-state achieved: 2-3 days

            Distribution

            Protein bound: 50% to plasma proteins and 45% to serum proteins

            Vd: 76 L

            Substrate of the P-gp, BCRP, OAT3 and MATE2-K transporters, which play roles in drug distribution

            Metabolism

            ~6% of the orally administered baricitinib dose is identified as metabolites (3 from urine and 1 from feces), with CYP3A4 identified as the main metabolizing enzyme

            No metabolites of baricitinib were quantifiable in plasma

            Elimination

            Half-life: 12 hr

            Total body clearance: 8.9 L/hr

            Excretion: 75% (69% unchanged) urine; 20% (15% unchanged) feces

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            Administration

            Oral Administration

            May take with or without food

            Unable to swallow whole tablet

            • Oral
              • Disperse tablet(s) for required dose in container with ~10 mL (5 mL minimum) of room temperature water by gently swirling contents; take immediately
              • Rinse container with an additional 10 mL of water and administer entire contents to patient
            • Gastrostomy feeding tube
              • Disperse tablet(s) for required dose in container with ~15 mL (10 mL minimum) of room temperature water by gently swirling contents; ensure tablets are sufficiently dispersed to flow through syringe tip
              • Withdraw entire contents from container into an appropriate syringe and immediately administer through gastric tube
              • Rinse container with an additional 15 mL of water, withdraw entire content into syringe and administer to patient
            • Nasogastric feeding tube
              • Disperse tablet(s) for required dose in container with ~30 mL of room temperature water by gently swirling contents; ensure tablets are sufficiently dispersed to flow through syringe tip
              • Withdraw entire contents from container into an appropriate syringe and immediately administer through nasogastric tube
              • To avoid clogging small diameter tubes (<12 Fr), the syringe can be held horizontally and shaken during administration
              • Rinse container with sufficient amount (minimum of 15 mL) of room temperature water, withdraw contents into syringe, and administer through nasogastric tube

            Storage

            Tablets: Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F)

            Dispersed tablets in water: Stable for up to 4 hr

            Handling

            • Intact tablet: Not hazardous
            • Crushed tablets: Not known if powder may constitute a reproductive hazard to preparer; use proper control measures (eg, ventilated enclosure) or personal protective equipment (ie, N95 respirator)
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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

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            • Compare formulary status to other drugs in the same class.
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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.