Isavuconazole
 |
|
 |
|
| Clinical data | |
|---|---|
| Trade names | Cresemba (prodrug form) |
| AHFS/Drugs.com | cresemba |
| Pregnancy category |
|
| Routes of administration |
Oral, intravenous |
| ATC code | |
| Legal status | |
| Legal status |
|
| Identifiers | |
|
|
| PubChem CID | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| NIAID ChemDB | |
| Chemical and physical data | |
| Formula | C22H17F2N5OS |
| Molar mass | 437.47 g/mol |
| 3D model (Jmol) | |
|
|
|
|
  (what is this?)
|
|
Isavuconazole (BAL4815; trade name Cresemba) is a triazole antifungal drug. Its prodrug, isavuconazonium sulfate (BAL8557), was granted approval by the U.S. Food and Drug Administration (FDA) on March 6, 2015
During its Phase III drug trials, Astellas partnered with Basilea Pharmaceutica, the developer of the drug, for rights to co-development and marketing of isavuconazole.
On May 28, 2013, Basilea Pharmaceutica announced it had been granted orphan drug status by the FDA for treatment of aspergillosis. Since then, it has also been granted orphan drug status for the treatment of invasive candidiasis.
Isavuconazole has been approved by the FDA for treatment of invasive aspergillosis and invasive mucormycosis in adults ages 18 years and older. Both infections are caused by mold and fungi common to the environment, and occur in individuals who are immunosuppressed or have other complicating conditions, such as diabetes or lung disease.
Common
Rare
Isavuconazole should not be administered with other medications that strongly inhibit or induce the enzyme CYP3A4 due to the effect on plasma concentration. CYP3A4 inducers can result in subtherapeutic drug levels, and CYP3A4 inhibitors can cause supratherapeutic levels with increased adverse events and toxicity.
Isavuconazole is not recommended in people with pre-sensitized immune state to other heterocyclic compound antifungal agents and infusion-related reactions.
Studies have shown isavuconazole to have a dose dependent effect of shortening the QTc interval. It is contraindicated for use in individuals with familial short QT syndrome. Additive effects with other drugs that shorten the QTc have not been evaluated.
Isavuconazole works by inhibiting lanosterol 14 alpha-demethylase, the enzyme responsible for converting lanosterol to ergosterol by demethylation. The resulting depletion of ergosterol and build up of lanosterol compromise the structure of the fungal cell membrane. Mammalian cells are resistant to demethylation inhibition by azoles, making the drug effects specific to fungi.
...
Wikipedia