Home Microbiology Fungal inhibitor Isavuconazole

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Isavuconazole Fungal inhibitor

Cat.No.S3722

Isavuconazole (BAL-4815, RO-0094815) is a new extended-spectrum triazole with activity against yeasts, molds, and dimorphic fungi that inhibits cytochrome P450 (CYP)-dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis.
Isavuconazole Fungal inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 437.47

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Quality Control

Batch: S372201 DMSO]87 mg/mL]false]Ethanol]87 mg/mL]false]Water]Insoluble]false Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (198.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 437.47 Formula

C22H17F2N5OS
 

 Storage (From the date of receipt)
CAS No. 241479-67-4 Download SDF Storage of Stock Solutions

Synonyms BAL-4815, RO-0094815 Smiles CC(C1=NC(=CS1)C2=CC=C(C=C2)C#N)C(CN3C=NC=N3)(C4=C(C=CC(=C4)F)F)O

Mechanism of Action

In vitro
Isavuconazole inhibits cytochrome P450 (CYP)–dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis. This blockade produces methylated sterols in the fungal membrane, altering its function and allowing the accumulation of ergosterol toxic precursors in the cytoplasm, which leads to cell death.
In vivo
Isavuconazonium sulfate, the prodrug of isavuconazole, is available in both intravenous and oral formulations. After intravenous infusion, the prodrug is broken down quickly to the active component, isavuconazole, and an inactive cleavage product. Following oral administration, plasma concentrations of the active compound reach maximum concentrations (Cmax) by 2–3 hours; the prodrug and cleavage product are not measurable in plasma after oral administration. In healthy adult volunteers, isavuconazole exhibits linear and dose-proportional pharmacokinetics. The oral bioavailability of isavuconazole is 98%. Absorption of isavuconazole is not affected by food intake. In addition to excellent bioavailability, isavuconazole serum concentrations show low intersubject variability. In healthy volunteers, the Cmax at steady state was 2.5 ± 1.0 µg/mL. Isavuconazole has a large volume of distribution, is >99% protein bound, and has a long terminal half-life of 100-130 hours. Metabolism of isavuconazole takes place in the liver via the CYP enzyme family, specifically CYP3A4 and CYP3A5 isoenzymes.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05630976 Recruiting
Invasive Fungal Disease
Pfizer
 February 7 2023 Phase 4
NCT04486885 Unknown status
Cerebral Aspergillosis|Invasive Aspergillosis
Imagine Institute
 August 1 2021 --
NCT04777058 Completed
Invasive Fungal Infections|Pharmacokinetics|Intensive Care Unit
Radboud University Medical Center
 March 1 2021 --
NCT04550936 Completed
Invasive Aspergillosis|Mucormycosis
Pfizer
 March 10 2021 --

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