Version May 2024
Influenza, seasonal, treatment: Oral:
<80 kg: 40 mg as a single dose within 48 hours of onset of influenza symptoms.
≥80 kg: 80 mg as a single dose within 48 hours of onset of influenza symptoms.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥50 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; however, CrCl ≥50 mL/minute had no clinically important effect on baloxavir (the active metabolite) pharmacokinetics.
CrCl <50 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Mild impairment (Child-Pugh class A): There are no dosage adjustments provided in the manufacturer's labeling.
Moderate impairment (Child-Pugh class B): There are no dosage adjustments provided in the manufacturer's labeling, however moderate hepatic impairment had no clinically important effect on baloxavir (the active metabolite) pharmacokinetics.
Severe impairment (Child-Pugh class C): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Refer to adult dosing.
(For additional information see "Baloxavir: Pediatric drug information")
Influenza, treatment: Note: Treatment should ideally begin within 48 hours of symptom onset.
Children <5 years: Limited data available: Oral: 2 mg/kg once as a single dose; maximum dose: 40 mg/dose (Ref).
Note: Dosing based on experience reported in 36 children <5 years of age who were included in a randomized, double-blind study comparing baloxavir with oseltamivir in children <12 years of age with clinical diagnosis of influenza. Time to alleviation of signs and symptoms was similar between the groups as was incidence of adverse effects (Ref). Due to increased risk of treatment-emergent resistance, FDA approval in this age group was not granted.
Children ≥5 years and Adolescents (Ref):
<20 kg: Oral suspension: Oral: 2 mg/kg once as a single dose.
20 to <80 kg: Oral suspension, tablet: Oral: 40 mg once as a single dose.
≥80 kg: Oral: Oral suspension, tablet: Oral: 80 mg once as a single dose.
Influenza, postexposure prophylaxis: Note: Administer within 48 hours of exposure. Optimal role of baloxavir therapy not defined; baloxavir did not receive FDA approval in ages <5 years because of increased risk of resistance-associated substitutions (Ref).
Children ≥5 years and Adolescents:
<20 kg: Oral suspension: Oral: 2 mg/kg once as a single dose.
20 to <80 kg: Oral suspension, tablet: Oral: 40 mg once as a single dose.
≥80 kg: Oral: Oral suspension, tablet: Oral: 80 mg once as a single dose.
Children ≥5 years and Adolescents:
CrCl ≥50 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; however, pharmacokinetic studies show that CrCl ≥50 mL/minute had no clinically important effect on baloxavir (the active metabolite) pharmacokinetics.
CrCl <50 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; has not been studied.
Children ≥5 years and Adolescents:
Mild or moderate hepatic impairment: There are no dosage adjustments provided in the manufacturer's labeling; however, pharmacokinetic studies show that moderate hepatic impairment had no clinically important effect on baloxavir pharmacokinetics.
Severe hepatic impairment: There are no dosage adjustments provided in the manufacturer's labeling; has not been studied.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%: Gastrointestinal: Diarrhea (children: 5%), vomiting (children: 5%)
Postmarketing:
Dermatologic: Erythema multiforme, skin rash, urticaria
Gastrointestinal: Colitis, hematochezia, melena
Hypersensitivity: Anaphylactic shock, anaphylaxis, angioedema, hypersensitivity reaction, nonimmune anaphylaxis
Nervous system: Abnormal behavior, delirium, hallucination
Hypersensitivity (eg, anaphylaxis, angioedema, urticaria, erythema multiforme) to baloxavir marboxil or any component of the formulation.
Concerns related to adverse effects:
• Bacterial infection: There is no evidence of efficacy of baloxavir marboxil in illnesses (eg, bacterial infections) caused by pathogens other than influenza viruses. Serious bacterial infections may begin with influenza-like symptoms, may coexist with, or occur as an influenza complication. Baloxavir marboxil has not been shown to prevent such complications. Monitor for potential secondary bacterial infections and manage appropriately.
• Hypersensitivity: Hypersensitivity reactions, including anaphylaxis, angioedema, urticaria, and erythema multiforme have been reported; evaluate and treat accordingly.
Reduced susceptibility to influenza A strains may occur in younger patients who receive baloxavir due to gene mutations of the polymerase acidic (PA) protein; use has been associated with treatment-emergent amino acid substitutions in the PA protein of the influenza RNA polymerase complex (PA/I38X), particularly in influenza A subtype H3N2 isolates, which result in reduced baloxavir susceptibility. The rate of PA substitutions has been reported to be 13.5% to 23.4% in children <12 years of age, occurring more frequently in children <5 years of age (43% of patients; 36/83) as compared to children 5 to <12 years of age (16% of patients; 19/117) (Baker 2020; Hirotsu 2020; manufacturer's labeling). In contrast, a study in adolescent patients (12 to 17 years of age) reported a substitution rate of 9.8% (Portsmouth 2020), and a study that included both adolescent and adult patients reported a substitution rate of 2.2% to 9.7% (Hayden 2018). Children infected with influenza viruses that developed PA substitutions after receipt of baloxavir had delayed symptom resolution (79.8 vs 42.8 hours) and a longer duration of viral shedding (180 vs 24 hours) compared to children with viruses that did not develop substitutions after baloxavir receipt (Hirotsu 2020). In a study of 374 patients who received baloxavir for influenza prophylaxis after a household contact became ill, 5 of 15 patients who developed PA substitutions were ≤10 years of age. While some have reported transmission of PA substitutions among household contacts, in this study PA substitutions were detected only in patients who received baloxavir (Ikematsu 2020).
Xofluza oral suspension: FDA approved November 2020; anticipated availability currently unknown.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet Therapy Pack, Oral:
Xofluza (40 MG Dose): 1 x 40 MG (1 ea); 2 x 20 MG (2 ea [DSC])
Xofluza (80 MG Dose): 1 x 80 MG (1 ea); 2 x 40 MG (2 ea [DSC])
No
Tablet Therapy Pack (Xofluza (40 MG Dose) Oral)
1 x 40 mg (per each): $190.97
Tablet Therapy Pack (Xofluza (80 MG Dose) Oral)
1 x 80 mg (per each): $190.97
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Oral: Initiate within 48 hours of influenza symptom onset or influenza exposure. Administer a single dose with or without food. Avoid administration with dairy products, calcium-fortified beverages, polyvalent cation-containing laxatives, antacids, or oral supplements (eg, calcium, iron, magnesium, selenium, zinc). Oral suspension may be administered orally or enterally via a feeding tube. Use an accurate measuring device (eg, oral syringe) for oral administration. For enteral administration, draw up suspension using an enteral syringe; flush with 1 mL of water before and after administration. Gently swirl suspension to evenly suspend granules (do not shake) just prior to administering the dose.
Oral: May administer with or without food. Avoid administering with dairy, calcium-fortified beverages, polyvalent cation-containing laxatives, antacids, or oral supplements (eg, calcium, iron, magnesium, selenium, zinc).
Oral suspension: May be administered orally or enterally via a feeding tube; must be administered within 10 hours of reconstitution. Do not mix with soft food or liquids. Should be administered while patient is upright; should not be administered while the patient is lying down. Use an accurate measuring device (eg, oral syringe, measuring cup) for oral administration. For administration via a feeding tube, draw up suspension using a compatible enteral syringe; flush with 1 mL of water before and after administration.
Influenza, seasonal, postexposure prophylaxis: Postexposure prophylaxis of influenza (A or B) infection in patients ≥5 years of age following contact with an individual who has influenza.
Influenza, seasonal, treatment: Treatment of acute uncomplicated influenza (A or B) infection in patients ≥5 years of age who have been symptomatic for no more than 48 hours and who are otherwise healthy or treatment of acute uncomplicated influenza (A or B) infection in patients ≥12 years of age who have been symptomatic for no more than 48 hours and who are at high risk of developing influenza-related complications.
Limitations of use: Influenza viruses change over time, and factors such as the virus type or subtype, emergence of resistance, or changes in viral virulence may diminish the clinical benefit of antiviral drugs. Consider available information on influenza drug susceptibility patterns and treatment effects when deciding whether to use baloxavir marboxil.
Substrate of CYP3A4 (minor), P-glycoprotein/ABCB1 (minor), UGT1A3; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Influenza Virus Vaccine (Live/Attenuated): Antiviral Agents (Influenza A and B) may diminish the therapeutic effect of Influenza Virus Vaccine (Live/Attenuated). Management: Avoid administration of live influenza virus vaccine (LAIV) within 2 weeks before or 48 hours after administration of antiviral agents. Consider avoiding LAIV if peramivir was given within the last 5 days or baloxavir was given within the last 17 days. Risk D: Consider therapy modification
Polyvalent Cation Containing Products: May decrease the serum concentration of Baloxavir Marboxil. Risk X: Avoid combination
Baloxavir may form a chelate with calcium products, decreasing baloxavir exposure. Management: Avoid coadministration with dairy products
Adverse events were not observed in animal reproduction studies.
Pregnant and postpartum patients (≤2 weeks after delivery) have a higher risk for complications from influenza, including preterm delivery, pneumonia, admission to a hospital or ICU, and maternal and fetal death. Underlying maternal medical conditions increase these risks (ACOG 2018; CDC 2020a).
Due to lack of data, baloxavir marboxil is not recommended for use in pregnant patients (CDC 2020a; CDC 2020b).
An algorithm is available for the treatment of pregnant patients with known or suspected influenza (ACOG 2018). Refer to the Centers for Disease Control and Prevention recommendations for treatment updates based on resistance patterns (ACOG 2018; CDC 2020a).
It is not known if baloxavir marboxil is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Due to lack of data, baloxavir marboxil is not recommended for use in patients who are breastfeeding (CDC 2020a; CDC 2020b).
Monitor for hypersensitivity reactions; potential secondary bacterial infections.
Baloxavir marboxil is an oral prodrug that is converted to baloxavir, an inhibitor of the endonuclease activity of a selective polymerase acidic (PA) protein, which is required for viral gene transcription, resulting in inhibition of influenza virus replication. Baloxavir has demonstrated antiviral activity against influenza A and B viruses, including strains resistant to standard current antiviral agents (Hayden 2018).
Note: Pharmacokinetic parameters in pediatric patients 5 to 17 years are similar to those observed in adults (Portsmouth 2020; manufacturer's labeling).
Distribution: Vd: 1,180 L.
Protein binding: ~93% to 94%.
Metabolism: Baloxavir marboxil is a prodrug; completely converted via UGT1A3 (major) and CYP3A4 (minor) to the active metabolite (baloxavir).
Half-life elimination: 79.1 hour.
Time to peak: 4 hours.
Excretion: Feces (80.1%); Urine (14.7%; 3.3% as baloxavir).
Body weight: As weight increases, exposure to baloxavir decreases.
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