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

Stem definition	Drug id	CAS RN
systemic antifungal agents, miconazole derivatives	4947	742049-41-8

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.20	g	O
0.20	g	P

ADMET properties:

None

Approvals:

Date	Agency	Company
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.96		CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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