Baloxa Tablet 40 mg

Baloxa Tablet 40 mg Uses, Dosage, Side Effects, Food Interaction and all others data.

Baloxa Tablet 40 mg is an antiviral drug developed by Shionogi Co., a Japanese pharmaceutical company and Roche for the treatment of influenza A and influenza B infections. The drug was initially approved for use in Japan in February 2018 and approved by the FDA on October 24, 2018 , for the treatment of acute uncomplicated influenza in patients 12 years of age and older who have been symptomatic for no more than 48 hours . Baloxa Tablet 40 mg, a cap-endonuclease inhibitor, has a unique mechanism of action when compared to the currently existing neuraminidase inhibitor drug class used to treat influenza infections .

Baloxa Tablet 40 mg is a selective inhibitor of influenza cap-dependent endonuclease which prevents polymerase function and therefore influenza virus mRNA replication , . It has shown therapeutic activity against influenza A and B virus infections, including strains resistant to current antiviral agents . This drug inhibits an enzyme required for viral replication, thus rapidly treating flu virus infection , and alleviating the symptoms associated with infection. A single dose of this agent was shown to be superior to placebo in relieving influenza symptoms and superior to both oseltamivir and placebo drug in virologic outcomes (marked by decreased viral load) . The safety profile of Baloxa Tablet 40 mg compared favorably with that of oseltamivir, making it an effective treatment option for treatment of the flu virus, in one single dose , .

Baloxa Tablet 40 mg
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Baloxa Tablet 40 mg
Generic	Baloxavir marboxil
Baloxavir marboxil Other Names	Baloxavir marboxil
Weight	40 mg
Type	Tablet
Formula	C₂₇H₂₃F₂N₃O₇S
Weight	Average: 571.55 Monoisotopic: 571.122477593
Protein binding	92.9 - 93.9 %
Groups	Approved, Investigational
Therapeutic Class
Manufacturer	Beximco Pharmaceuticals Ltd.
Available Country	Bangladesh
Last Updated:	October 19, 2023 at 6:27 am

Uses

Baloxa Tablet 40 mg is a polymerase acidic endonuclease inhibitor used to treat uncomplicated influenza.

For the treatment of influenza A and B virus infection , in patients 12 and older who have been symptomatic for no more than 48 hours. Clinical trials of this drug did not include subjects 65 years of age and older to determine whether they respond in a different way than younger subjects .

Baloxa Tablet 40 mg is also used to associated treatment for these conditions: Acute, uncomplicated Influenza

How Baloxa Tablet 40 mg works

This drug is a CAP endonuclease inhibitor . The influenza endonuclease is an essential subdomain of the viral RNA polymerase enzyme. CAP endonuclease processes host pre-mRNAs to serve as primers for viral mRNA and therefore has been a common target for studies of anti-influenza drugs. Inhibiting the activity of endonuclease can block the transcription of mRNA and inactivate the influenza virus .

Viral gene transcription is primed by short-capped oligonucleotides that are cleaved from host cell pre mRNA by endonuclease activity. Translation of viral mRNAs by the host ribosome requires that they are capped at the 5' end, and this is achieved in cells infected with influenza virus by a “cap-snatching” mechanism, whereby the endonuclease cleaves 5′ caps from host mRNA which then act as primers for transcription. The N-terminal domain of PA subunit (PAN) has been confirmed to accommodate the endonuclease activity residues, which is highly preserved among subtypes of influenza A virus and is able to fold functionally . Translation of viral mRNAs by the host ribosome requires that they are capped at the 5' end, and this is achieved in cells infected with influenza virus by a “cap-snatching” mechanism, whereby the endonuclease cleaves 5′ caps from host mRNA which then act as primers for transcription. The endonuclease domain binds the N-terminal half of PA (PAN) and contains a two-metal (Mn2+) active site that selectively cleaves the pre-mRNA substrate at the 3′ end of a guanine .

The administration of a cap-endonuclease inhibitor, such as Baloxa Tablet 40 mg, prevents the above process from occurring, exhibiting its action at the beginning of the pathway before CAP endonuclease may exert its action .

Toxicity

Ld50 (oral, rats): >2000 mg/kg

Pregnancy Risk

There are no available data on the use of this drug in pregnant women to predict or inform a drug-associated risk of adverse developmental outcomes. However, there are known risks to the mother and fetus associated with influenza virus infection during pregnancy. In animal reproduction studies, no adverse developmental effects were observed in rats or rabbits with oral administration of Baloxa Tablet 40 mg at exposures approximately 5 (rats) and 7 (rabbits) times the systemic Baloxavir exposure at the maximum recommended human dose . The estimated background risk of major birth defects and miscarriage for the indicated population is not known at this time .

Breastfeeding

There are no data on the presence of this drug in human breastmilk, the effects on the breastfed infant, or the effects on milk production. Baloxavir and its related metabolites were present in the milk of lactating rats .

Carcinogenicity

Carcinogenicity studies have not been completed with baloxavir marboxil .

Mutagenesis

Baloxa Tablet 40 mg and the active metabolite, baloxavir, were not shown to be mutagenic in in-vitro and in in-vivo genotoxicity assays, which included bacterial mutation assays in S. typhimurium and E. coli, micronucleus tests with cultured mammalian cells, and in the rodent micronucleus assay .

Impairment of Fertility

In a fertility and early embryonic development study in rats, doses of baloxavir marboxil at 20, 200, or 1,000 mg/kg/day were given to female animals for 2 weeks before mating, during mating and until day 7 of pregnancy. Male animals were dosed for 4 weeks before mating and throughout mating. There were no measured effects on fertility, mating performance, or early embryonic development at any dose level, resulting in systemic drug exposure (AUC) approximately 5 times the MRHD (maximum recommended human dose) .

Food Interaction

Avoid antacids.
Avoid multivalent ions. Multivalent ions such as magnesium, calcium, and aluminum can form a chelate with baloxavir, which can reduce the absorption of baloxavir.
Take with or without food.