Name | Baloxavir marboxil |
CAS number | 1985606-14-1 |
EINECS number | 606-227-7 |
Synonym | Baloxavir marboxil; S 033188; S-033188; S033188; Xofluza; ({(12aR)-12-[(11S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-6,8-dioxo-3,4,6,8,12,12ahexahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin-7-yl}oxy)methyl methyl carbonate |
Related CAS# | 1985605-59-1 (Baloxavir); 1985606-14-1 (marboxil) |
Description | Baloxavir marboxil, also known as S 033188, is a selective inhibitor of influenza cap-dependent endonuclease. It has shown therapeutic activity in preclinical models of influenza A and B virus infections, including strains resistant to current antiviral agents. |
Structure | |
Molecular Formula | C27H23F2N3O7S |
Molecular Weight | 571.55 g/mol |
Appearance | Solid powder |
Quality Standard | Enterprise Standard |
Assay | ≥98% |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition | Store in cool place. Keep container tightly closed in a dry and well ventilated place. |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Baloxavir marboxil More Info
Baloxavir marboxil is an antiviral medication used for the treatment of influenza (the flu) in patients aged 12 years and older. It is a novel polymerase acidic endonuclease inhibitor that works by interfering with the replication of the influenza virus. Approved by the U.S. Food and Drug Administration (FDA) in 2018, baloxavir marboxil represents a new class of antiviral drugs for influenza.
Mechanism of Action
Baloxavir marboxil is a prodrug that is converted in the body to its active form, baloxavir, which inhibits the influenza virus's ability to replicate. The mechanism of action involves:
Inhibition of Viral RNA Polymerase: Baloxavir targets the endonuclease activity of the polymerase acidic (PA) protein of the influenza virus. By inhibiting this enzyme, baloxavir prevents the viral RNA from being cleaved and capped, which is essential for viral mRNA synthesis.
Blocking Viral Replication: This inhibition disrupts the replication cycle of the virus, ultimately leading to a reduction in viral load and alleviation of flu symptoms.
Applications
Baloxavir marboxil is indicated for:
Treatment of Influenza: It is used for the treatment of acute uncomplicated influenza in patients aged 12 years and older who have been symptomatic for no more than 48 hours.
Post-Exposure Prophylaxis: Baloxavir may also be used for post-exposure prophylaxis to prevent influenza infection in individuals who have been exposed to the virus.
Safety and Side Effects
Baloxavir marboxil is generally well-tolerated, but some side effects may occur:
Common Side Effects:
Diarrhea
Nausea
Headache
Bronchitis
Sinusitis
Serious Side Effects:
Hypersensitivity reactions (e.g., rash, itching, swelling)
Potential risk of developing viral resistance with improper use
Most side effects are mild to moderate and resolve without intervention.
Routes of Administration
Baloxavir marboxil is administered orally as a single dose tablet. It can be taken with or without food.
Pharmacokinetics
Absorption: Baloxavir marboxil is rapidly absorbed after oral administration, with peak plasma concentrations typically reached within 1-3 hours.
Distribution: The drug has a volume of distribution that indicates it distributes well throughout the body.
Metabolism: Baloxavir is primarily metabolized by uridine diphosphate-glucuronosyltransferases (UGTs), particularly UGT1A3.
Elimination: The elimination half-life of baloxavir is approximately 35 hours, allowing for once-daily dosing. The drug is primarily excreted via urine and feces.
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