isavuconazonium 🐶 Veterinary Use | 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: -0.61
  • 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
Dec. 23, 2022 PMDA Asahi Kasei Pharma Corporation

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 313.83 44.14 152 623 674310 62813937

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 384.48 32.12 238 1443 419286 34535964
Febrile neutropenia 54.48 32.12 48 1633 136801 34818449
Lip squamous cell carcinoma 42.06 32.12 7 1674 125 34955125
Aspergillus infection 34.21 32.12 15 1666 12239 34943011

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
Off label use 131.34 33.53 139 1989 907076 78835184
Febrile neutropenia 88.02 33.53 62 2066 230937 79511323
Death 51.57 33.53 69 2059 566445 79175815
Lip squamous cell carcinoma 40.16 33.53 7 2121 305 79741955
Aspergillus infection 36.24 33.53 15 2113 19146 79723114

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J02AC05 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOTICS FOR SYSTEMIC USE
ANTIMYCOTICS FOR SYSTEMIC USE
Triazole and tetrazole derivatives
FDA CS M0002083 Azoles
FDA EPC N0000175487 Azole Antifungal
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000935 Antifungal Agents
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187061 Organic Cation Transporter 2 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 sterol 14alpha-demethylase inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Cryptococcosis indication 42386007 DOID:12053
Aspergillosis indication 65553006 DOID:13564
Mucormycosis indication 76627001
Genetic short QT syndrome contraindication 698273002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
74.5MG CRESEMBA ASTELLAS N207500 Nov. 22, 2022 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
74.5MG CRESEMBA ASTELLAS N207500 Nov. 22, 2022 RX CAPSULE ORAL March 6, 2022 FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
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
74.5MG CRESEMBA ASTELLAS N207500 Nov. 22, 2022 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
74.5MG CRESEMBA ASTELLAS N207500 Nov. 22, 2022 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
ATP-binding cassette sub-family G member 2 Transporter IC50 4.96 CHEMBL

External reference:

IDSource
4034331 VANDF
CHEBI:85977 CHEBI
CHEBI:85979 CHEBI
QKM PDB_CHEM_ID
CHEMBL1183349 ChEMBL_ID
C508735 MESH_SUPPLEMENTAL_RECORD_UI
946075-13-4 SECONDARY_CAS_RN
497235-79-7 SECONDARY_CAS_RN
DB06636 DRUGBANK_ID
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
C4018471 UMLSCUI
C1832021 UMLSCUI
CHEMBL3137333 ChEMBL_ID
CHEMBL409153 ChEMBL_ID
6918606 PUBCHEM_CID
8784 INN_ID
8783 INN_ID
241479-67-4 SECONDARY_CAS_RN
6918485 PUBCHEM_CID
VH2L779W8Q UNII
60UTO373KE UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
CRESEMBA HUMAN PRESCRIPTION DRUG LABEL 1 0469-0320 CAPSULE 186 mg ORAL NDA 29 sections
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 0469-0420 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 40 mg INTRAVESICAL NDA 29 sections
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
CRESEMBA HUMAN PRESCRIPTION DRUG LABEL 1 0469-0520 CAPSULE 100 mg ORAL NDA 29 sections
CRESEMBA HUMAN PRESCRIPTION DRUG LABEL 1 0469-0520 CAPSULE 100 mg ORAL NDA 29 sections
CRESEMBA HUMAN PRESCRIPTION DRUG LABEL 1 0469-2860 CAPSULE 40 mg ORAL NDA 29 sections