baloxavir marboxil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals 5301 1985606-14-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • baloxavir marboxil
  • xofluza
  • S-033188
  • S 033188
  • RG 6152
Baloxavir marboxil is a prodrug that is converted by hydrolysis to baloxavir, the active form that exerts anti-influenza virus activity. Baloxavir inhibits the endonuclease activity of the polymerase acidic (PA) protein, an influenza virus-specific enzyme in the viral RNA polymerase complex required for viral gene transcription, resulting in inhibition of influenza virus replication. The 50% inhibitory concentration (IC50) of baloxavir was 1.4 to 3.1 nM (n=4) for influenza A viruses and 4.5 to 8.9 nM (n=3) for influenza B viruses in a PA endonuclease assay. Viruses with reduced susceptibility to baloxavir have amino acid substitutions in the PA protein.
  • Molecular weight: 571.55
  • Formula: C27H23F2N3O7S
  • CLOGP: 2.36
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 0
  • TPSA: 97.85
  • ALOGS: -4.14
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
40 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Oct. 24, 2018 FDA GENENTECH INC
Feb. 23, 2018 PMDA Shionogi & Co., Ltd.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
No adverse event 62.05 62.04 17 286 9511 2348271

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pneumonia 78.15 55.02 33 247 46149 1700352
Rhabdomyolysis 64.99 55.02 20 260 11070 1735431

Pharmacologic Action:

SourceCodeDescription
ATC J05AX25 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Other antivirals
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Influenza indication 6142004 DOID:8469
Coronavirus infection off-label use 186747009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.75 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
20MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL Oct. 16, 2022 TREATMENT OF ACUTE UNCOMPLICATED INFLUENZA IN PATIENTS 12 YEARS OF AGE OR OLDER, WHO HAVE BEEN SYMPTOMATIC FOR NO MORE THAN 48 HOURS AND ARE AT HIGH RISK OF DEVELOPING INFLUENZA-RELATED COMPLICATIONS
40MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL Oct. 16, 2022 TREATMENT OF ACUTE UNCOMPLICATED INFLUENZA IN PATIENTS 12 YEARS OF AGE OR OLDER, WHO HAVE BEEN SYMPTOMATIC FOR NO MORE THAN 48 HOURS AND ARE AT HIGH RISK OF DEVELOPING INFLUENZA-RELATED COMPLICATIONS
20MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL Oct. 24, 2023 NEW CHEMICAL ENTITY
40MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL Oct. 24, 2023 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Polymerase acidic protein Enzyme INHIBITOR IC50 8.85 DRUG LABEL DRUG LABEL

External reference:

IDSource
4G86Y4JT3F UNII
1985605-59-1 SECONDARY_CAS_RN
10491 INN_ID
017822 NDDF
2099995 RXNORM
35334 MMSL
d09012 MMSL
4037950 VANDF
782500006 SNOMEDCT_US
124081896 PUBCHEM_CID
D11021 KEGG_DRUG
DB13997 DRUGBANK_ID
CHEMBL4297215 ChEMBL_ID
CHEMBL4297503 ChEMBL_ID
C000628402 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50090-4102 TABLET, FILM COATED 20 mg ORAL NDA 18 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50090-4104 TABLET, FILM COATED 40 mg ORAL NDA 18 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-828 TABLET, FILM COATED 20 mg ORAL NDA 20 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-860 TABLET, FILM COATED 40 mg ORAL NDA 20 sections