Baloxavir marboxil

What is Baloxavir marboxil?

• Baloxavir marboxil (Xofluza), is an influenza virus polymerase acidic (PA) endonuclease inhibitor.

Baloxavir marboxil

What are the uses of this medicine?

Baloxavir marboxil (Xofluza) is a prescription medicine used to:

• treat the flu (influenza) in people 12 years of age and older who have had flu symptoms for no more than 48 hours.
• prevent the flu in people 12 years of age and older following contact with a person who has the flu.

Limitations of use:

• Xofluza does not treat or prevent illness that is caused by infections other than the influenza virus.
• Xofluza does not prevent bacterial infections that may happen with the flu.

How does this medicine work?

• An orally bioavailable prodrug and influenza cap-dependent endonuclease (CEN) inhibitor, with antiviral activity.
• Upon administration of baloxavir marboxil, the agent is converted by hydrolysis to its active metabolite baloxavir. Baloxavir targets, binds to and inhibits the CEN activity of the influenza polymerase acidic (PA) protein, an influenza virus-specific enzyme in the viral RNA polymerase complex required for the initiation of influenza gene transcription.
• By inhibiting PA endonuclease, influenza virus mRNA replication is halted.
• This reduces viral load and prevents further influenza infection.

Efficacy:

• As of 2019 in the only published phase 3 RCT of otherwise healthy outpatients to date, baloxavir reduced the duration of symptoms by about one day compared to placebo, which was the same as oseltamivir.
• On the first day after baloxavir was started the viral load decreased more than with either placebo or oseltamivir.
• However, after 5 days of oseltamivir the effect of a single dose of baloxavir was indistinguishable.
• In mice, baloxavir and oseltamivir have been shown to be synergistic and there is no significant pharmacokinetic interaction.

Resistance:

• In 2.2% of baloxavir recipients in the phase 2 trial and in about 10% of baloxavir recipients in the phase 3 trial the influenza strain became resistant.
• This was due to polymerase acidic protein variants with I38T/M/F substitutions.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to baloxavir marboxil or any of the ingredients in Xofluza.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• polyvalent cations such as calcium, aluminum, or magnesium
• intranasal live attenuated influenza vaccine

• Avoid coadministration of Xofluza with dairy products, calcium-fortified beverages, polyvalent cation-containing laxatives, antacids, or oral supplements (e.g., calcium, iron, magnesium, selenium, or zinc).

Is this medicine FDA approved?

• Baloxavir marboxil was approved for sale in Japan in February 2018.
• On October 24, 2018 the U.S. FDA approved it for the treatment of acute uncomplicated influenza in people 12 years of age and older who have been symptomatic for no more than 48 hours.

How should this medicine be used?

• Xofluza should be taken as soon as possible after influenza symptom onset or exposure to influenza and may be taken with or without food.
• Coadministration of Xofluza with dairy products, calcium-fortified beverages, polyvalent cation-containing laxatives, antacids, or oral supplements (e.g., calcium, iron, magnesium, selenium, or zinc) should be avoided.

Recommended dosage:

Recommended Xofluza Tablet Dosage in Adults and Adolescents (12 Years of Age and Older): Less than 80 kg:

• One 40 mg tablet (blister card contains one 40 mg tablet)

At least 80 kg:

• One 80 mg tablet'(blister card contains one 80 mg tablet)

Recommended Xofluza Oral Suspension Dosage in Adults and Adolescents (12 Years of Age and Older): Less than 80 kg:

• 40 mg/20 mL (1 bottle) taken as a single dose

At least 80 kg:

• 80 mg/40 mL (2 bottles) taken as a single dose

Administration:

• Baloxavir marboxil comes as a tablet and a suspension (liquid) to take by mouth.
• Take Xofluza exactly as directed by your healthcare provider or pharmacist.
• Your healthcare provider will either prescribe:
• Xofluza tablet as a single one-time dose, or
• Xofluza oral suspension provided with a measuring device (an oral syringe or measuring cup) to be given as a single one-time dose.
• Xofluza may be given through a feeding tube. Follow your healthcare provider's instructions for giving Xofluza through a feeding tube.
• Take Xofluza with or without food.
• Do not take Xofluza with dairy products, calcium-fortified beverages, laxatives, antacids or oral supplements containing iron, zinc, selenium, calcium or magnesium.
• If you take too much Xofluza, go to the nearest emergency room right away.
• If you are taking the suspension, gently swirl the suspension well before use to mix the medication evenly; do not shake the bottle(s).
• Use an oral syringe provided by your pharmacist to measure the correct amount of liquid needed for your dose.
• Your total dose may require less than one bottle, one bottle, or 2 bottles of the suspension.
• Do not take more or less of it other than prescribed by your doctor. Do not mix the suspension with any other liquid or with soft food.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 40 mg and 80 mg.
• For oral suspension: 40 mg/20 mL when constituted for final concentration of 2 mg/mL.

This medicine is available in fallowing brand namesː

• Xofluza

What side effects can this medication cause?

The most common side effects of this medicine include:

• diarrhea
• bronchitis
• nausea
• sinusitis
• headache

Less common,but serious side effects may include:

• Allergic reactions

What special precautions should I follow?

• Cases of anaphylaxis, urticaria, angioedema, and erythema multiforme have been reported in postmarketing experience with Xofluza. The use of Xofluza is contraindicated in patients with known hypersensitivity to Xofluza.
• There is no evidence of efficacy of Xofluza in any illness caused by pathogens other than influenza viruses. Serious bacterial infections may begin with influenza-like symptoms or may coexist with, or occur as, a complication of influenza.
• Instruct patients to begin treatment with Xofluza as soon as possible at the first appearance of influenza symptoms, within 48 hours of onset of symptoms. Instruct patients to start taking Xofluza for prevention as soon as possible after exposure.
• Advise patients not to take with dairy products, calcium-fortified beverages, polyvalent cation-containing laxatives, antacids, or oral supplements (e.g., calcium, iron, magnesium, selenium, or zinc).
• Because of the potential for antivirals to decrease the effectiveness of live attenuated influenza vaccines, advise patients to consult their healthcare provider prior to receiving a live attenuated influenza vaccine after taking Xofluza.
• There are no data on the presence of baloxavir marboxil in human milk, the effects on the breastfed infant, or the effects on milk production.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Treatment of an overdose of Xofluza should consist of general supportive measures, including monitoring of vital signs and observation of the clinical status of the patient. There is no specific antidote for overdose with Xofluza.
• Baloxavir is unlikely to be significantly removed by dialysis due to high serum protein binding.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies with Xofluza in pregnant women to inform a drug-associated risk of adverse developmental outcomes.
• There are risks to the mother and fetus associated with influenza virus infection in pregnancy.

Can this medicine be used in children?

• The safety and efficacy of Xofluza in pediatric subjects less than 12 years of age have not been established for the treatment of acute uncomplicated influenza.
• The safety and efficacy of Xofluza for post-exposure prophylaxis of influenza in pediatric subjects less than 12 years of age have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient: baloxavir marboxil

• Xofluza tablets inactive ingredients: croscarmellose sodium, hypromellose, lactose monohydrate, microcrystalline cellulose, povidone, sodium stearyl fumarate, talc, and titanium dioxide.
• Xofluza for oral suspension inactive ingredients: colloidal silicon dioxide, hypromellose, maltitol, mannitol, povidone K25, sodium chloride, strawberry flavor, sucralose and talc.

Who manufactures and distributes this medicine?

Distributed by:

• Genentech USA, Inc., A Member of the Roche Group, 1 DNA Way, South San Francisco, CA
• Xofluza® is a registered trademark of Genentech, Inc. © 2021 Genentech USA, Inc.

What should I know about storage and disposal of this medication?

Xofluza tablets:

• Store Xofluza tablet at room temperature between 68°F to 77°F (20°C to 25°C).
• Store Xofluza tablet in the blister package that it comes in.

Xofluza for oral suspension:

• Store Xofluza for oral suspension at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Xofluza for oral suspension in the original container. Use by the expiration time and date written on bottle label.
• Throw away any Xofluza for oral suspension not used by the time and date on the bottle label.

• Dailymed label info on Baloxavir marboxil
• FDA Baloxavir marboxil

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