baloxavir marboxil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
40 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.02 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CG,PRKDC 19
kinase-selectivity-class AXL 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 178.90 45.63 52 801 67930 90559664
Colitis ischaemic 142.86 45.63 31 822 12315 90615279
Melaena 58.69 45.63 19 834 34778 90592816

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
Colitis ischaemic 88.46 42.55 21 668 7205 42613441
No adverse event 87.13 42.55 30 659 38991 42581655
Abnormal behaviour 46.24 42.55 17 672 26434 42594212
Pneumonia 43.95 42.55 43 646 422106 42198540

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
Colitis ischaemic 209.57 46.39 48 1380 17702 110570169
No adverse event 126.21 46.39 44 1384 73795 110514076
Pneumonia 66.39 46.39 68 1360 876646 109711225
Abnormal behaviour 61.74 46.39 22 1406 39017 110548854
Anaphylactic reaction 59.11 46.39 29 1399 114271 110473600
Loss of consciousness 51.98 46.39 32 1396 196274 110391597
Delirium febrile 46.73 46.39 6 1422 65 110587806

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
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:33281 antimicrobial agent

Related Drugs by ATC class:

J05AX Other antivirals 15 drugs
amenamevirbulevirtideenfuvirtidefavipiravirfostemsaviribalizumabinosine pranobexlenacapavirletermovirmaravirocmaribavirmoroxydine show all 15 →

Drug Use | Suggest Off label Use Form| |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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 DISCN TABLET ORAL 10633397 April 27, 2036 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
20MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 DISCN 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
30MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL 10633397 April 27, 2036 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
30MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL 10633397 April 27, 2036 METHOD FOR TREATING INFLUENZA
40MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL 10633397 April 27, 2036 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
40MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL 10633397 April 27, 2036 METHOD FOR TREATING INFLUENZA
20MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 DISCN TABLET ORAL 11306106 Aug. 9, 2037 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
20MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 DISCN 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
30MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL 11306106 Aug. 9, 2037 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
30MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL 11306106 Aug. 9, 2037 METHOD FOR TREATING INFLUENZA
40MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL 11306106 Aug. 9, 2037 METHOD FOR POST-EXPOSURE PROPHYLAXIS OF INFLUENZA
40MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 DISCN TABLET ORAL Dec. 19, 2027 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
40MG XOFLUZA GENENTECH INC N210854 Oct. 24, 2018 RX TABLET ORAL Dec. 19, 2027 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
80MG XOFLUZA GENENTECH INC N210854 March 18, 2021 RX TABLET ORAL Dec. 19, 2027 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
2MG/ML XOFLUZA GENENTECH INC N214410 Nov. 23, 2020 RX FOR SUSPENSION ORAL Dec. 19, 2027 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
30MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL Dec. 19, 2027 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
40MG/PACKET XOFLUZA GENENTECH INC N214410 May 30, 2025 RX FOR SUSPENSION ORAL Dec. 19, 2027 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING

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
4037950 VANDF
C4688747 UMLSCUI
CHEBI:756989 CHEBI
CHEMBL4297503 ChEMBL_ID
124081896 PUBCHEM_CID
DB13997 DRUGBANK_ID
D11021 KEGG_DRUG
10491 INN_ID
C000628402 MESH_SUPPLEMENTAL_RECORD_UI
11748 IUPHAR_LIGAND_ID
782500006 SNOMEDCT_US
1985605-59-1 SECONDARY_CAS_RN
294671 MMSL
35334 MMSL
d09012 MMSL
017822 NDDF
2099995 RXNORM

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 33 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-599 GRANULE, FOR SUSPENSION 30 mg ORAL NDA 33 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-617 GRANULE, FOR SUSPENSION 40 mg ORAL NDA 33 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-860 TABLET, FILM COATED 40 mg ORAL NDA 33 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 50242-877 TABLET, FILM COATED 80 mg ORAL NDA 33 sections
Xofluza HUMAN PRESCRIPTION DRUG LABEL 1 85766-058 TABLET, FILM COATED 80 mg ORAL NDA 32 sections