Isavuconazonium

Azole Antifungal — ANTIINFECTIVES FOR SYSTEMIC USE

Key facts

Isavuconazonium is an ofp drug in the Azole Antifungal class catalogued in DrugCentral. It was first approved by the FDA in 2015. Its mechanism of action is classified as Cytochrome P450 3A4 Inhibitors, Organic Cation Transporter 2 Inhibitors and P-Glycoprotein Inhibitors. DrugCentral lists 1 molecular target, including ABCG2. Recorded indications include Aspergillosis, Cryptococcosis and Mucormycosis.

• Approval status: ofp (first approved 2015 by the FDA).
• Drug class: Azole Antifungal.
• Mechanism of action: Cytochrome P450 3A4 Inhibitors; Organic Cation Transporter 2 Inhibitors; P-Glycoprotein Inhibitors.
• Molecular targets: ABCG2 (1 listed in DrugCentral).
• Indications: Aspergillosis, Cryptococcosis and Mucormycosis.
• ATC code: J02AC05 (Triazole and tetrazole derivatives).
• Molecular formula: C35H35F2N8O5S; molecular weight 717.77 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Aspergillosis
• Cryptococcosis
• Mucormycosis

Contraindications (1)

• Genetic short QT syndrome

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 3A4 Inhibitors; Organic Cation Transporter 2 Inhibitors; P-Glycoprotein Inhibitors
• Established pharmacologic class: Azole Antifungal

Molecular targets (1)

Target	Gene	Action	Activity
ATP-binding cassette sub-family G member 2	ABCG2	unknown	IC50 4.96

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2022-12-23	PMDA	—	Asahi Kasei Pharma Corporation
2015-07-23	EMA	—	—
2015-03-06	FDA	—	ASTELLAS

ATC classification

ATC code	Therapeutic hierarchy
J02AC05	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIMYCOTICS FOR SYSTEMIC USE › ANTIMYCOTICS FOR SYSTEMIC USE › Triazole and tetrazole derivatives

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Off label use	707.8
Febrile neutropenia	184.4
Aspergillus infection	90.0
Death	79.8
Lip squamous cell carcinoma	55.2
Pneumonia fungal	54.3
Drug interaction	47.6
Septic shock	44.5
Disease progression	44.3
Cytokine release syndrome	44.2
Gamma-glutamyltransferase increased	41.3
Human herpesvirus 8 infection	38.6

Chemical structure

• Molecular formula: C₃₅H₃₅F₂N₈O₅S
• Molecular weight: 717.77 g/mol
• CAS number: 742049-41-8
• InChIKey: RSWOJTICKMKTER-QXLBVTBOSA-N
• PubChem CID: 6918485

CNCC(=O)OCC1=CC=CN=C1N(C)C(=O)OC(C)[N+]1=CN(C[C@@](O)([C@@H](C)C2=NC(=CS2)C2=CC=C(C=C2)C#N)C2=C(F)C=CC(F)=C2)N=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Isavuconazonium used for?

DrugCentral lists the following indications for Isavuconazonium: Aspergillosis, Cryptococcosis and Mucormycosis.

How does Isavuconazonium work?

Isavuconazonium is classified as Cytochrome P450 3A4 Inhibitors, Organic Cation Transporter 2 Inhibitors and P-Glycoprotein Inhibitors; its molecular targets in DrugCentral include ABCG2.

When was Isavuconazonium first approved?

Isavuconazonium was first approved by the FDA in 2015.

What drug class does Isavuconazonium belong to?

Isavuconazonium is in the Azole Antifungal class.

What is the chemical formula of Isavuconazonium?

Isavuconazonium has the molecular formula C35H35F2N8O5S and a molecular weight of 717.77 g/mol.

Sources

• DrugCentral drug card 4947 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1183349 — compound record and bioactivity
• PubChem CID 6918485 — chemical identifiers
• DrugBank DB06636 — drug record
• FDA UNII 60UTO373KE — substance identity
• DailyMed: FDA labels for Isavuconazonium — current prescribing information (label search)
• UniProt Q9UNQ0 (ABCG2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.