Baloxavir marboxil, a cap-endonuclease inhibitor, is an antiviral drug.
Storage Temp
Store at -20°C,Argon charged
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Polymerase acidic protein inhibitor
Product Description
Information
Baloxavir marboxil Baloxavir marboxil, a cap-endonuclease inhibitor, is an antiviral drug.
In vivo
Single-dose oral baloxavir marboxil is well tolerated, had a favorable safety profile, and has favorable pharmacokinetic characteristics, including a long half-life, supporting single oral dosing. In nonclinical studies, baloxavir marboxil is a prodrug and is converted to an active form, baloxavir acid, by hydrolysis. After single oral administration in rats and monkeys, plasma concentrations of baloxavir marboxil are below the lower limit of quantification (LLOQ) at all sampling points, and area under the plasma concentration-time curve of baloxavir acid increased dose proportionally. The major excretion route of radioactivity is via fecal excretion, whereas urinary excretion was low in rats and monkeys. Baloxavir marboxil has shown therapeutic activity in preclinical models of influenza A and B virus infections, including strains resistant to current antiviral agents. In murine models of seasonal influenza and avian influenza A(H5N1) or A(H7N9), orally administered baloxavir is associated with rapid reductions in pulmonary viral loads and decreased mortality.
1.Ivashchenko AA, Mitkin OD, Jones JC, Nikitin AV, Koryakova AG, Ryakhovskiy A, Karapetian RN, Kravchenko DV, Aladinskiy V, Leneva IA et al.. (2020) Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses.. J Med Chem, 63 (17):(9403-9420). [PMID:32787099][10.1021/op500134e]
2.Takashita E, Morita H, Ogawa R, Nakamura K, Fujisaki S, Shirakura M, Kuwahara T, Kishida N, Watanabe S, Odagiri T. (2018) Susceptibility of Influenza Viruses to the Novel Cap-Dependent Endonuclease Inhibitor Baloxavir Marboxil.. Front Microbiol, 9 (13):(3026). [PMID:30574137][10.1021/op500134e]
3.Abraham GM, Morton JB, Saravolatz LD. (2020) Baloxavir: A Novel Antiviral Agent in the Treatment of Influenza.. Clin Infect Dis, 71 (7):(1790-1794). [PMID:32020174][10.1021/op500134e]
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H2219082