Xofluza (baloxavir marboxil)
Antiviral - Influenza A Oral Tablet
Last reviewed · Source: First Databank (FDB) drug data
Overview
Baloxavir marboxil is a prodrug of baloxavir, a polymerase acidic (PA) endonuclease inhibitor antiviral active against influenza A and B viruses.
Baloxavir marboxil is a prodrug of baloxavir, a polymerase acidic (PA) endonuclease inhibitor antiviral. Baloxavir marboxil exhibits no antiviral activity until hydrolyzed in vivo to baloxavir, its active metabolite. Baloxavir has a mechanism of action against influenza viruses that differs from that of the neuraminidase inhibitor antivirals (oseltamivir, peramivir, zanamivir) and adamantane derivative antivirals (amantadine, rimantadine).
Baloxavir selectively inhibits the cap-dependent endonuclease activity of the PA subunit of the viral RNA polymerase complex, which is essential for viral replication. Inhibition of the cap-dependent endonuclease activity of the PA subunit prevents transcription of influenza viral messenger RNA, which is required for viral replication.
USES: Baloxavir marboxil is an antiviral medication used to treat the flu (influenza) if your symptoms started less than 48 hours ago. It helps make the symptoms (such as stuffy nose, cough, sore throat, fever/chills, aches, tiredness) less severe and may shorten the recovery time by 1 to 2 days. Baloxavir marboxil works by stopping the flu virus from growing.
It will not treat other kinds of infection besides the flu virus. This medication may also be used to prevent the flu if you have been exposed to someone who already has the flu (such as a sick household member) or if there is a flu outbreak in the community. Talk to your doctor for more details.
This medication should not be used in children younger than 5 since it may not be effective. Baloxavir marboxil is not a substitute for the flu vaccine. (See also Notes section.)
Generic name: baloxavir marboxil
Pronunciation: (bal-OX-a-vir mar-BOX-il)
Drug class: Antiviral - Influenza A
Therapeutic class: Anti-Infective Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Xofluza
Indications
The following indications are listed for Xofluza:
- Influenza
- Influenza Prevention
Also known as: Flu, Grip, Influenza Prophylaxis.
Dosing
No dosing information is available for this tab.
Baloxavir marboxil is administered orally without regard to meals. However, concomitant administration with dairy products; calcium-fortified beverages; or antacids, laxatives, or oral supplements containing polyvalent cations (aluminum, calcium, iron, magnesium, selenium, or zinc) should be avoided. (See Antacids and Other Preparations Containing Polyvalent Cations under Drug Interactions.)
Baloxavir marboxil is commercially available as tablets or as granules for oral suspension that must be suspended in water prior to administration.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Xofluza 40 Mg Tab (80 Mg Dose) | Maintenance | Take 2 tablets (80 mg) by oral route once. |
No dosing information is available for this tab.
Drug interactions
After baloxavir marboxil is converted in vivo to baloxavir, the active metabolite, baloxavir is metabolized principally by uridine diphosphate-glucuronosyltransferase (UGT) 1A3 and, to a minor extent, by cytochrome P-450 (CYP) isoenzyme 3A4.
In vitro studies indicate that baloxavir marboxil and baloxavir do not inhibit CYP isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, or 2D6 and do not induce CYP isoenzymes 1A2, 2B6, or 3A4.
Baloxavir marboxil and baloxavir are both substrates of P-glycoprotein (P-gp).
In vitro studies indicate that baloxavir marboxil and baloxavir do not inhibit UGT1A1, 1A3, 1A4, 1A6, 1A9, 2B7, or 2B15. In addition, baloxavir does not inhibit organic anion transport polypeptide (OATP) 1B1, OATP1B3, organic cation transporter (OCT) 1, OCT2, organic anion transporter (OAT) 1, OAT3, multidrug and toxin extrusion (MATE) 1, or MATE2K.
Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
Selected Antiviral Agents/Influenza Virus Vaccine Live
SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
MECHANISM OF ACTION: Amantadine,(1) oseltamivir,(2) rimantadine,(3) zanamivir,(4) and baloxavir,(5) may inactivate the intranasal live influenza virus vaccine, preventing the body from developing an immune response.
CLINICAL EFFECTS: Administration of amantadine,(1) oseltamivir,(2) rimantadine,(3) zanamivir,(4) and baloxavir,(5) may render the intranasal live influenza virus vaccine ineffective.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: The US manufacturers of amantadine,(1) oseltamivir,(2) rimantadine,(3) zanamivir(4), baloxavir(5), and the intranasal live influenza virus vaccine(6) state that these agents should not be initiated within 2 weeks of the administration of the intranasal live influenza virus vaccine and that the vaccine should not be administered within 48 hours of the discontinuation of these agents. Inactivated influenza vaccine may be used at any time.(1)
DISCUSSION: Because antiviral drugs such as amantadine,(1) oseltamivir,(2) rimantadine,(3) zanamivir,(4) and baloxavir (5) inhibit the replication of live viruses, these agents may interfere with the efficacy of the intranasal live influenza virus vaccine.
There are no severe interactions for this drug.
Moderate Interaction: Assess the risk to the patient and take action as needed.
Baloxavir/Polyvalent Cations
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Aluminum, calcium, iron, magnesium, selenium, and zinc may form chelation compounds with baloxavir.(1)
CLINICAL EFFECTS: Simultaneous administration of products containing aluminum, calcium, iron, magnesium, selenium, and zinc may result in decreased levels of and clinical effects from baloxavir.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Avoid concurrent administration of baloxavir with cation-containing products.(1)
DISCUSSION: A significant decrease in baloxavir exposure was observed when baloxavir was coadministered with calcium, aluminum, magnesium, or iron in monkeys. No studies have been conducted in humans.(1)
Contraindications
*History of hypersensitivity to baloxavir marboxil or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- No disease contraindications
Adverse reactions
Adverse effects reported in 1% or more of patients receiving baloxavir marboxil in clinical studies include GI effects (nausea, diarrhea), bronchitis, sinusitis, and headache.
Rare or Very Rare
- Anaphylaxis
- Angioedema
- Bloody diarrhea
- Colitis
- Erythema multiforme
- Facial edema
- Hypersensitivity drug reaction
- Tongue swelling
- Urticaria
More Frequent
- Bronchitis
- Diarrhea
- Headache disorder
- Nausea
- Pharyngitis
- Sinusitis
Rare or Very Rare
- Behavioral disorders
- Black tarry stools
- Delirium
- Hallucinations
- Skin rash
- Voice change
- Vomiting
Precautions
No enhanced messaging available.
Safety and efficacy of baloxavir marboxil have not been established in pediatric patients younger than 12 years of age.
Safety and efficacy of baloxavir marboxil for the treatment of influenza in adolescents 12 years of age or older weighing 40 kg or more were established in a phase 3, randomized, double-blind, placebo-controlled study. Data from this study indicated that the safety profile of the drug in adolescent patients 12 years of age or older is similar to that reported in adults.
Safety and efficacy of baloxavir marboxil for postexposure prophylaxis of influenza in adolescents 12 years of age or older weighing 40 kg or more is supported by a randomized, double-blind, placebo-controlled trial conducted in Japan that included 12 individuals 12-17 years of age who received the drug for postexposure prophylaxis. Adverse effects reported in these adolescents were similar to those reported in adults in the trial who received the drug.
There are no adequate and well-controlled studies using baloxavir marboxil in pregnant women to inform a drug-associated risk of adverse developmental outcomes.
In animal reproduction studies, no adverse embryofetal effects were observed in rats or rabbits receiving oral baloxavir marboxil in dosages resulting in baloxavir exposures approximately 5 or 7 times, respectively, the systemic baloxavir exposures achieved in humans with the maximum recommended human dosage.
Pregnant women are at increased risk for severe complications from influenza, which may lead to adverse pregnancy and/or fetal outcomes including maternal death, stillbirths, birth defects, preterm delivery, low birthweight, and small size for gestational age.
CDC states that baloxavir marboxil is not recommended for the treatment of influenza in pregnant women because of the lack of safety and efficacy data in such patients. Oseltamivir is the preferred antiviral for the treatment of suspected or confirmed influenza and prevention of influenza in women who are pregnant or up to 2 weeks postpartum.
It is not known whether baloxavir marboxil is distributed into human milk, affects milk production, or has any effects on breast-fed infants. Baloxavir and its metabolites are distributed into milk in rats.
The manufacturer states that the benefits of breast-feeding and the importance of baloxavir marboxil to the woman should be considered along with the potential adverse effects on the breast-fed child from the drug or from the underlying maternal condition.
CDC states that baloxavir marboxil is not recommended for the treatment of influenza in nursing women because of the lack of safety data in such patients.
Safety and efficacy of baloxavir marboxil for the treatment of acute, uncomplicated influenza in adults 65 years of age or older have been established and are supported by a randomized, double-blind, controlled trial that included 209 adults in this age group at high risk of influenza-related complications who were treated with the drug. The median time to improvement of influenza symptoms in patients 65 years of age or older was 70 hours in those treated with baloxavir marboxil compared with 88 hours in those who received placebo. The safety profile of the drug in patients 65 years of age or older was similar to that reported in the overall trial population, with the exception of nausea (reported in 6% of adults 65 years of age or older compared with 1% of those 18-64 years of age).
ICD codes
| Code | Type | Description |
|---|---|---|
| Influenza | ||
| J09 | ICD10CM | Influenza due to certain identified influenza viruses |
| J09.x | ICD10CM | Influenza due to identified novel influenza A virus |
| J09.x1 | ICD10CM | Influenza due to identified novel influenza A virus with pneumonia |
| J09.x2 | ICD10CM | Influenza due to identified novel influenza A virus with other respiratory manifestations |
| J09.x3 | ICD10CM | Influenza due to identified novel influenza A virus with gastrointestinal manifestations |
| J09.x9 | ICD10CM | Influenza due to identified novel influenza A virus with other manifestations |
| J10 | ICD10CM | Influenza due to other identified influenza virus |
| J10.0 | ICD10CM | Influenza due to other identified influenza virus with pneumonia |
| J10.00 | ICD10CM | Influenza due to other identified influenza virus with unspecified type of pneumonia |
| J10.01 | ICD10CM | Influenza due to other identified influenza virus with the same other identified influenza virus pneumonia |
| J10.08 | ICD10CM | Influenza due to other identified influenza virus with other specified pneumonia |
| J10.1 | ICD10CM | Influenza due to other identified influenza virus with other respiratory manifestations |
| J10.2 | ICD10CM | Influenza due to other identified influenza virus with gastrointestinal manifestations |
| J10.8 | ICD10CM | Influenza due to other identified influenza virus with other manifestations |
| J10.81 | ICD10CM | Influenza due to other identified influenza virus with encephalopathy |
| J10.82 | ICD10CM | Influenza due to other identified influenza virus with myocarditis |
| J10.83 | ICD10CM | Influenza due to other identified influenza virus with otitis media |
| J10.89 | ICD10CM | Influenza due to other identified influenza virus with other manifestations |
| J11 | ICD10CM | Influenza due to unidentified influenza virus |
| J11.0 | ICD10CM | Influenza due to unidentified influenza virus with pneumonia |
| J11.00 | ICD10CM | Influenza due to unidentified influenza virus with unspecified type of pneumonia |
| J11.08 | ICD10CM | Influenza due to unidentified influenza virus with specified pneumonia |
| J11.1 | ICD10CM | Influenza due to unidentified influenza virus with other respiratory manifestations |
| J11.2 | ICD10CM | Influenza due to unidentified influenza virus with gastrointestinal manifestations |
| J11.8 | ICD10CM | Influenza due to unidentified influenza virus with other manifestations |
| J11.81 | ICD10CM | Influenza due to unidentified influenza virus with encephalopathy |
| J11.82 | ICD10CM | Influenza due to unidentified influenza virus with myocarditis |
| J11.83 | ICD10CM | Influenza due to unidentified influenza virus with otitis media |
| J11.89 | ICD10CM | Influenza due to unidentified influenza virus with other manifestations |
| Influenza prevention | ||
| Z20.828 | ICD10CM | Contact with and (suspected) exposure to other viral communicable diseases |
ICD code information from First Databank (FDB).
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Last reviewed · Source: First Databank (FDB) drug data
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