English Synonyms
Isaconazole;4-[2-[(2R,3R)-3-(2,5-difluorophenyl)-3-hydroxy-4-(1,2,4-triazol-1-yl)butan-2-yl]-1,3-thiazol-4-yl]benzonitrile;Isavucozole;4-(2-((2R,3R)-3-(2,5-difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl)thiazol-4-yl)benzonitrile;Isavuconazonium;Isavuconazole(BAL-4815;Isavuconazole;4-[2-[(1R,2R)-2-(2,5-Difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-4-thiazolyl]benzonitrile
Isavuconazole Properties
| Melting Point | 89 - 91oC |
| Boiling Point | 678.0±65.0 °C(Predicted) |
| Density | 1.38 |
| Storage Condition | 2-8°C |
| Solubility | Soluble in Chloroform (A Little), Methanol (A Little) |
| Form | Solid |
| Acidity Coefficient (pKa) | 11.42±0.29(Predicted) |
| Color | Off-White to Beige |
Isavuconazole Usage and Synthesis
Pharmacological Action
After Entering the Body, Isavuconazole Sulfate Is Rapidly Converted into the Active Metabolite Isavuconazole by Plasma Esterase. Similar to Other Azole Antifungal Drugs, Isavuconazole Destroys the Formation of Fungal Cell Membranes by Inhibiting Ergosterol Biosynthesis. Isavuconazole Binds to the Cytochrome P450 Lanosterol 14-α-Demethylase Encoded by the Fungal Cyp51 Gene, Inhibits the Activity of 14-α-Demethylase, And Hinders Ergosterol Synthesis. The Accumulated Toxic Methylated Sterols Affect the Structural Stability and Integrity of the Fungal Cell Membrane and Change Its Function, Ultimately Leading to Fungal Death. The Side Chain in the Isavuconazole Structural Molecule Has a High Affinity with the Fungal Cyp51 Protein, Which Enables It to Have a Broad Antifungal Spectrum and Include Fungi That Are Resistant to Other Azole Antifungal Drugs.
Drug Interactions
Similar to Other Triazole Antifungal Drugs, Isavuconazole Has Significant Interactions with Drugs Metabolized by the Cyp450 System, Especially the Isoenzyme Cyp3a4. Isavuconazole Is a Substrate of Cyp3a4, And Cyp3a4 Inhibitors or Inducers Can Affect the Plasma Concentration of Isavuconazole. The Simultaneous Administration of Isavuconazole Sulfate with Strong Cyp3a4 Inhibitors Such as Ketoconazole or High-Dose Ritonavir Can Increase the Plasma Concentration of Isavuconazole; the Simultaneous Administration with Strong Cyp3a4 Inducers Such as Rifampicin, Carbamazepine, St. John's Wort or Long-Acting Barbiturates Can Significantly Reduce the Plasma Concentration of Isavuconazole.
Application
1.Invasive Aspergillosis: Applicable to the Treatment of Invasive Aspergillosis in Patients Aged 18 Years and Above.
2.Invasive Mucormycosis: Applicable to the Treatment of Invasive Mucormycosis in Patients Aged 18 Years and Above.
Biological Activity
Isavuconazole (Bal-4815, Ro-0094815) Is a Novel Broad-Spectrum Triazole Compound Active Against Yeast, Molds and Dimorphic Fungi, Inhibiting the Cytochrome P450 (Cyp)-Dependent Demethylation of 14α-Lanosterol, Thereby Inhibiting the Synthesis of Ergosterol in Fungal Cell Membranes.
