isavuconazonium Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
systemic antifungal agents, miconazole derivatives 4947 742049-41-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • isavuconazonium
  • isavuconazonium sulfate
  • isavuconazonium chloride
  • cresemba
  • BAL8557-000
  • BAL8557-002
  • RO0098557
prodrug of BAL4815
  • Molecular weight: 717.77
  • Formula: C35H35F2N8O5S
  • CLOGP: -1.15
  • LIPINSKI: 2
  • HAC: 13
  • HDO: 2
  • TPSA: 159.37
  • ALOGS: -5.16
  • ROTB: 15

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
0.20 g O
0.20 g P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 23, 2015 EMA
March 6, 2015 FDA ASTELLAS

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
Off label use 363.17 51.00 136 369 379705 46305852

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
Off label use 418.54 33.93 191 887 249099 29702301

Pharmacologic Action:

SourceCodeDescription
ATC J02AC05 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOTICS FOR SYSTEMIC USE
ANTIMYCOTICS FOR SYSTEMIC USE
Triazole derivatives
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000935 Antifungal Agents
FDA EPC N0000175487 Azole Antifungal
FDA CS M0002083 Azoles
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000187061 Organic Cation Transporter 2 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
CHEBI has role CHEBI:50266 prodrugs
CHEBI has role CHEBI:71031 orphan drugs
CHEBI has role CHEBI:75282 ergosterol biosynthesis inhibitors
CHEBI has role CHEBI:77884 obtusufoliol 14-demethylase inhibitor

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Aspergillosis indication 65553006 DOID:13564
Mucormycosis indication 76627001
Genetic short QT syndrome contraindication 698273002

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.43 acidic
pKa2 7.36 Basic
pKa3 2.98 Basic
pKa4 2.37 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
186MG CRESEMBA ASTELLAS N207500 March 6, 2015 RX CAPSULE ORAL March 6, 2020 NEW CHEMICAL ENTITY
372MG CRESEMBA ASTELLAS N207501 March 6, 2015 RX POWDER INTRAVENOUS March 6, 2020 NEW CHEMICAL ENTITY
186MG CRESEMBA ASTELLAS N207500 March 6, 2015 RX CAPSULE ORAL March 6, 2022 TREATMENT OF INVASIVE ASPERGILLOSIS
186MG CRESEMBA ASTELLAS N207500 March 6, 2015 RX CAPSULE ORAL March 6, 2022 TREATMENT OF INVASIVE MUCORMYCOSIS IN PATIENTS 18 YEARS OF AGE AND OLDER
372MG CRESEMBA ASTELLAS N207501 March 6, 2015 RX POWDER INTRAVENOUS March 6, 2022 TREATMENT OF INVASIVE ASPERGILLOSIS
372MG CRESEMBA ASTELLAS N207501 March 6, 2015 RX POWDER INTRAVENOUS March 6, 2022 TREATMENT OF INVASIVE MUCORMYCOSIS IN PATIENTS 18 YEARS OF AGE AND OLDER
186MG CRESEMBA ASTELLAS N207500 March 6, 2015 RX CAPSULE ORAL March 6, 2025 GENERATING ANTIBIOTIC INCENTIVES NOW
372MG CRESEMBA ASTELLAS N207501 March 6, 2015 RX POWDER INTRAVENOUS March 6, 2025 GENERATING ANTIBIOTIC INCENTIVES NOW
186MG CRESEMBA ASTELLAS N207500 March 6, 2015 RX CAPSULE ORAL March 6, 2027 GENERATING ANTIBIOTIC INCENTIVES NOW
372MG CRESEMBA ASTELLAS N207501 March 6, 2015 RX POWDER INTRAVENOUS March 6, 2027 GENERATING ANTIBIOTIC INCENTIVES NOW

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Aspergillus fumigatus Fungi MINIMUM INHIBITORY CONCENTRATION ED50 5.22 SCIENTIFIC LITERATURE DRUG LABEL
Candida albicans Fungi MINIMUM INHIBITORY CONCENTRATION ED50 5.82 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
497235-79-7 SECONDARY_CAS_RN
241479-67-4 SECONDARY_CAS_RN
4034331 VANDF
C4688415 UMLSCUI
C1832021 UMLSCUI
CHEBI:85977 CHEBI
CHEBI:85979 CHEBI
CHEMBL1183349 ChEMBL_ID
CHEMBL3137333 ChEMBL_ID
CHEMBL409153 ChEMBL_ID
DB06636 DRUGBANK_ID
6918606 PUBCHEM_CID
C508735 MESH_SUPPLEMENTAL_RECORD_UI
8784 INN_ID
8783 INN_ID
VH2L779W8Q UNII
60UTO373KE UNII
6918485 PUBCHEM_CID
DB11633 DRUGBANK_ID
1608321 RXNORM
233407 MMSL
30943 MMSL
d08355 MMSL
015945 NDDF
015946 NDDF
724004002 SNOMEDCT_US
724005001 SNOMEDCT_US
724006000 SNOMEDCT_US
763601000 SNOMEDCT_US
765386003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
CRESEMBA HUMAN PRESCRIPTION DRUG LABEL 1 0469-0420 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 40 mg INTRAVESICAL NDA 29 sections
CRESEMBA HUMAN PRESCRIPTION DRUG LABEL 1 0469-0520 CAPSULE 100 mg ORAL NDA 29 sections