baloxavir marboxil 🐶 Veterinary Use | 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. It was investigated as a potential treatment during the early stages of the COVID-19 pandemic but in vitro antiviral activity against SARS-CoV-2 was not confirmed.
  • Molecular weight: 571.55
  • Formula: C27H23F2N3O7S
  • CLOGP: 2.16
  • 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
Jan. 7, 2021 EMA ROCHE REGISTRATION GmbH
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 112.57 50.70 32 516 33546 50571030

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
No adverse event 67.84 52.11 20 414 17458 29556635

FDA Adverse Event Reporting System (Geriatric)

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 86.94 45.55 27 896 28534 64469275
Pneumonia 62.21 45.55 56 867 559520 63938289
Anaphylactic reaction 60.49 45.55 26 897 68638 64429171
Abnormal behaviour 51.51 45.55 19 904 33603 64464206
Rhabdomyolysis 50.29 45.55 25 898 91701 64406108
Loss of consciousness 49.34 45.55 29 894 148336 64349473
Delirium febrile 45.96 45.55 6 917 67 64497742

FDA Adverse Event Reporting System (Pediatric)

None

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
20MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL 10633397 April 27, 2036 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
20MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL 10633397 April 27, 2036 METHOD FOR TREATING INFLUENZA
40MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL 10633397 April 27, 2036 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
40MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL 10633397 April 27, 2036 METHOD FOR TREATING INFLUENZA
80MG XOFLUZA GENENTECH INC N210854 March 18, 2021 RX TABLET ORAL 10633397 April 27, 2036 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
80MG XOFLUZA GENENTECH INC N210854 March 18, 2021 RX TABLET ORAL 10633397 April 27, 2036 METHOD FOR TREATING INFLUENZA
2MG/ML XOFLUZA GENENTECH INC N214410 Nov. 23, 2020 RX FOR SUSPENSION ORAL 10633397 April 27, 2036 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
2MG/ML XOFLUZA GENENTECH INC N214410 Nov. 23, 2020 RX FOR SUSPENSION ORAL 10633397 April 27, 2036 METHOD FOR TREATING INFLUENZA
20MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL 11306106 Aug. 9, 2037 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
20MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL 11306106 Aug. 9, 2037 METHOD FOR TREATING INFLUENZA
40MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL 11306106 Aug. 9, 2037 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
40MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL 11306106 Aug. 9, 2037 METHOD FOR TREATING INFLUENZA
80MG XOFLUZA GENENTECH INC N210854 March 18, 2021 RX TABLET ORAL 11306106 Aug. 9, 2037 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
80MG XOFLUZA GENENTECH INC N210854 March 18, 2021 RX TABLET ORAL 11306106 Aug. 9, 2037 METHOD FOR TREATING INFLUENZA
2MG/ML XOFLUZA GENENTECH INC N214410 Nov. 23, 2020 RX FOR SUSPENSION ORAL 11306106 Aug. 9, 2037 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
2MG/ML XOFLUZA GENENTECH INC N214410 Nov. 23, 2020 RX FOR SUSPENSION ORAL 11306106 Aug. 9, 2037 METHOD FOR TREATING INFLUENZA

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
80MG XOFLUZA GENENTECH INC N210854 March 18, 2021 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
80MG XOFLUZA GENENTECH INC N210854 March 18, 2021 RX TABLET ORAL Oct. 24, 2023 NEW CHEMICAL ENTITY
2MG/ML XOFLUZA GENENTECH INC N214410 Nov. 23, 2020 RX FOR SUSPENSION 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
505CXM6OHG UNII
C4688747 UMLSCUI
CHEMBL4297503 ChEMBL_ID
124081896 PUBCHEM_CID
DB13997 DRUGBANK_ID
D11021 KEGG_DRUG
11748 IUPHAR_LIGAND_ID
1985605-59-1 SECONDARY_CAS_RN
2099995 RXNORM
294671 MMSL
35334 MMSL
d09012 MMSL
782500006 SNOMEDCT_US
4037950 VANDF
017822 NDDF
C000628402 MESH_SUPPLEMENTAL_RECORD_UI
10491 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50090-4102 TABLET, FILM COATED 20 mg ORAL NDA 31 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50090-4104 TABLET, FILM COATED 40 mg ORAL NDA 31 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-583 GRANULE, FOR SOLUTION 40 mg ORAL NDA 32 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-583 GRANULE, FOR SOLUTION 40 mg ORAL NDA 32 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-828 TABLET, FILM COATED 20 mg ORAL NDA 32 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-828 TABLET, FILM COATED 20 mg ORAL NDA 32 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-860 TABLET, FILM COATED 40 mg ORAL NDA 32 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-860 TABLET, FILM COATED 40 mg ORAL NDA 32 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-877 TABLET, FILM COATED 80 mg ORAL NDA 32 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-877 TABLET, FILM COATED 80 mg ORAL NDA 32 sections