Baloxavir marboxil
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2018
- First approval year
- 2018
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Baloxavir marboxil
- Molecular weight
- 571.56
- Structure (SMILES)
- COC(=O)OCOc1c2n(ccc1=O)N([C@@H]1c3ccccc3SCc3c1ccc(F)c3F)[C@@H]1COCCN1C2=O
- xofluza
- Xofluza
- baloxavir marboxil
- Baloxavir marboxil
- Baloxavir Marboxil
- baloxavir marboxil [INN]
- BALOXAVIR MARBOXIL [JAN]
- BALOXAVIR MARBOXIL [MI]
- BALOXAVIR MARBOXIL [ORANGE BOOK]
- BALOXAVIR MARBOXIL [USAN]
- Baloxavir marboxil [WHO-DD]
- baloxavir marboxil inn
- baloxavir marboxil jan
- baloxavir marboxil mi
- baloxavir marboxil orange book
- Baloxavir Marboxil Tablet
- Baloxavir Marboxil tablets
- baloxavir marboxil usan
- baloxavir marboxil who dd
- s 033188
- S-033188
- ATC classification codes
- J05AX25
Sources for recorded values
- CAS registry numbers
- 1985606-14-1
- ChEMBL ID
- CHEMBL4297503
- InChIKey
- RZVPBGBYGMDSBG-GGAORHGYSA-N
- PubChem compound IDs
- 124081896
- RxNorm IDs (RxCUI)
- 2099995
- FDA ingredient codes (UNII)
- 505CXM6OHG
- Applicant
- GENENTECH INC
- Approval date
- 24 Oct 2018
- Application number
- NDA210854
- Status
- Authorised
- Status date
- 7 Jan 2021
- Authorisation date
- 7 Jan 2021
- Approved indications
- Treatment of influenza Xofluza is indicated for the treatment of uncomplicated influenza in patients aged 1 year and above. Post exposure prophylaxis of influenza Xofluza is indicated for post-exposure prophylaxis of influenza in individuals aged 1 year and above. Xofluza should be used in accordance with official recommendations.
- Product number
- EMEA/H/C/004974
- Authorisation holder
- Roche Registration GmbH
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Influenza, Human
European medicines record
- Patents
- 18
- Designations
- 1
- Earliest recorded loss of exclusivity
- 21 Apr 2041
- First in class
- Yes
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- baloxavir marboxil
- Type
- Synthetic organic
- Drug name stem
- -vir
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Mechanism
- Polymerase acidic protein inhibitor
- Action type
- Inhibitor
- Target
- Polymerase acidic protein
- Protein identifier
- P03433
- Mechanism
- Polymerase acidic protein inhibitor
- Action type
- Inhibitor
- Target
- Polymerase acidic protein
- Protein identifier
- Q9QLI9
Open Targets mechanisms
- Mechanism
- Polymerase acidic protein inhibitor
- Action type
- Inhibitor
- Target
- Polymerase acidic protein
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- PA
- Protein identifier
- P03433
- Organism
- Influenza A virus (strain A/Puerto Rico/8/1934 H1N1)
- Target development level
- Clinical
- Condition
- Severe Acute Respiratory Syndrome
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000694
- Subject identifier
- D045169
- Condition
- Virus Diseases
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000763
- Subject identifier
- D014777
- Condition
- Pneumonia
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003106
- Subject identifier
- D011014
- Condition
- Influenza, Human
- Highest recorded phase
- 4
- Condition identifier
- EFO:0007328
- Subject identifier
- D007251
- Condition
- Severe Acute Respiratory Syndrome
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0100096
- Subject identifier
- D045169
- Condition identifier
- EFO_0000763
- Condition identifier
- EFO_0007328
- Condition identifier
- EFO_1001488
- Highest recorded phase
- 3
- Condition identifier
- HP_0002783
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005108
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005812
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0100096
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0100163
- Highest recorded phase
- 3
- Event
- abnormal behaviour
- Reports
- 25
- Reporting signal score
- 37.4404
- Event
- altered state of consciousness
- Reports
- 15
- Reporting signal score
- 20.1737
- Event
- anaphylactic reaction
- Reports
- 33
- Reporting signal score
- 38.3882
- Event
- anaphylactic shock
- Reports
- 15
- Reporting signal score
- 18.9163
- Event
- colitis ischaemic
- Reports
- 36
- Reporting signal score
- 117.761
- Event
- delirium
- Reports
- 12
- Reporting signal score
- 8.78714
- Event
- delirium febrile
- Reports
- 6
- Reporting signal score
- 33.3885
- Event
- diarrhoea
- Reports
- 63
- Reporting signal score
- 11.1234
- Event
- drug hypersensitivity
- Reports
- 2
- Reporting signal score
- 9.93175
- Event
- erythema multiforme
- Reports
- 14
- Reporting signal score
- 24.9118
- Event
- fatigue
- Reports
- 5
- Reporting signal score
- 21.2867
- Event
- febrile convulsion
- Reports
- 4
- Reporting signal score
- 11.6344
- Event
- haematochezia
- Reports
- 13
- Reporting signal score
- 10.2444
- Event
- hepatic function abnormal
- Reports
- 15
- Reporting signal score
- 13.3705
- Event
- hypertension
- Reports
- 1
- Reporting signal score
- 8.5406
- Event
- hypotension
- Reports
- 1
- Reporting signal score
- 10.4825
- Event
- loss of consciousness
- Reports
- 31
- Reporting signal score
- 20.8901
- Event
- melaena
- Reports
- 24
- Reporting signal score
- 39.4117
- Event
- pain
- Reports
- 2
- Reporting signal score
- 17.0129
- Event
- pneumonia
- Reports
- 73
- Reporting signal score
- 55.0125
- Event
- pneumonia bacterial
- Reports
- 11
- Reporting signal score
- 25.6009
- Event
- pneumonia influenzal
- Reports
- 6
- Reporting signal score
- 21.1212
- Event
- rhabdomyolysis
- Reports
- 25
- Reporting signal score
- 26.1915
- Event
- seizure
- Reports
- 24
- Reporting signal score
- 16.3054
- Event
- vomiting
- Reports
- 52
- Reporting signal score
- 9.86438
- NCT02735707
- NCT02949011
- NCT02954354
- NCT03629184
- NCT03653364
- NCT03684044
- NCT03969212
- NCT04141930
- NCT05170009
- NCT06094010
- NCT04381936
- Dose
- 20-80mg (based on weight)
- Route
- Oral
- How often
- Single dose within 48 hours of symptom onset or exposure
- May be taken with or without food
- Take as soon as possible after symptom onset or exposure
- Hydrogen bond acceptors
- 10
- Hydrogen bond donors
- 0
- Polar surface area
- 99.54
- Calculated partition coefficient (ALogP)
- 3.39
- Calculated partition coefficient (XLogP)
- 3.8
- Prodrug
- Yes
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 4
- Heavy atoms
- 40
- Molecular formula
- C27H23F2N3O7S
- Monoisotopic mass
- 571.12247758
- Natural product
- No
- 50242-583
- 50242-599
- 50242-617
- 50242-860
- 50242-877
- 85766-058
- Recorded assays
- 102
- Active assays
- 4
Active assay types
- Confirmatory
- Antiviral Agents
Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.
- Enzyme Inhibitors
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Oral bioavailability
- Median
- 26.9
- Mean
- 26.9
- Minimum
- 26.9
- Maximum
- 26.9
- Unit
- %
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (20)
- A Prospective, Multicenter, Randomized Controlled Clinical Study on the Efficacy and Safety of Xuanfei Baidu Granule in the Treatment of Influenza A
- A Study of S-033188 (Baloxavir Marboxil) Compared With Placebo or Oseltamivir in Otherwise Healthy Patients With Influenza
- A Surveillance Study of Susceptibility to Baloxavir Marboxil in Pediatric Participants With Influenza and Transmission of Influenza to Household Contacts
- Baloxavir and Oseltamivir for the Treatment of Severe Influenza Infection in Immunocompromised Patients
- Baloxavir in Combination With Oseltamivir in Allogenic Bone Marrow Transplant Recipients With Influenza
- Efficacy of Baloxavir Against Influenza in Hospitalized Patients: The INFLUENT Study (INpatients inFLUENza Treatment)
- Evaluation of a Screen and Treat Protocol for Influenza
- Oseltamivir and Baloxavir Marboxil for Prophylaxis Against Influenza Under a Hospital-based Setting
- Pilot of Cohort of Households for Influenza Monitoring and Evaluation in Seattle
- Randomised Evaluation of COVID-19 Therapy
- Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia
- Safety and Efficacy of ADC189 in Children 2-11 Years Old With Influenza
- Study of S-033188 (Baloxavir Marboxil) Compared With Placebo or Oseltamivir in Patients With Influenza at High Risk of Influenza Complications
- Study to Assess Efficacy and Safety of Baloxavir Marboxil In Combination With Standard-of-Care Neuraminidase Inhibitor In Hospitalized Participants With Severe Influenza
- Study to Assess the Efficacy of Baloxavir Marboxil Versus Placebo to Reduce Onward Transmission of Influenza A or B in Households
- Study to Assess the Pharmacokinetics, Safety and Tolerability of Baloxavir Marboxil in Healthy Chinese Participants
- Study to Assess the Safety, Pharmacokinetics, and Efficacy of Baloxavir Marboxil in Chinese Pediatric Participants 1 to <12 Years of Age With Influenza Symptoms
- Study to Assess the Safety, Pharmacokinetics, and Efficacy of Baloxavir Marboxil in Healthy Pediatric Participants From Birth to < 1 Year With Influenza-Like Symptoms
- Study to Assess the Safety, Pharmacokinetics, and Efficacy of Baloxavir Marboxil in Healthy Pediatric Participants With Influenza-Like Symptoms
- Xofluza-Wearables Feasibility-Study
Approved for (2)
In development for (3)
- COVID-19 Phase 3
- Pneumonia Phase 3
- Severe acute respiratory syndrome Phase 3