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

Drug dosage:

Dose	Unit	Route
0.20	g	O
0.20	g	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
July 23, 2015	EMA
March 6, 2015	FDA	ASTELLAS

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	358.29	44.43	147	447	474279	50130251

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	411.17	34.03	220	1189	300580	29272538
Febrile neutropenia	36.42	34.03	35	1374	112205	29460913

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	136.53	30.81	120	1583	632686	63864343
Febrile neutropenia	66.51	30.81	48	1655	187609	64309420
Death	51.17	30.81	63	1640	482642	64014387
Cytokine release syndrome	31.92	30.81	14	1689	20815	64476214
Cell death	31.02	30.81	9	1694	4045	64492984

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
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
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:

None

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
241479-67-4	SECONDARY_CAS_RN
DB06636	DRUGBANK_ID
VH2L779W8Q	UNII
6918606	PUBCHEM_CID
6918485	PUBCHEM_CID
DB11633	DRUGBANK_ID
1608321	RXNORM
233407	MMSL
30943	MMSL
d08355	MMSL
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
8784	INN_ID
8783	INN_ID
015945	NDDF
015946	NDDF
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	0469-0520	CAPSULE	100 mg	ORAL	NDA	29 sections
CRESEMBA	HUMAN PRESCRIPTION DRUG LABEL	1	0469-0520	CAPSULE	100 mg	ORAL	NDA	29 sections