Isavuconazole shows good activity against all Candida spp., with active MIC50 of 0.004 mg/L. The MIC50s/MIC90s range from 0.002/0.004 mg/L for C. albicans to 0.25/0.5 mg/L for C. glabrata. Isavuconazole has potent in vitro activity against most common Aspergillus species, Purpureocillium lilacinum, and Scedosporium apiospermum. Isavuconazole shows potent activity against molds, yeasts, and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 µg/mL with others as high as 32 µg/mL. Isavuconazole shows potent activity against molds, yeasts, and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 µg/mL with others as high as 32 µg/mL.
| Cell Experiment | |
|---|---|
| Cell lines | L‐type Ca2+ channels |
| Preparation method | The in vitro effects of isavuconazole on a panel of human cardiac Ca2+, K+, and Na+ channels were assessed by recording transmembrane currents in cultured cells stably transfected with genes encoding each channel. |
| Concentrations | 1, 3, 10, or 30 μM |
| Incubation time | 24‐h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 437.47 |
| Formula | C22H17F2N5OS |
| CAS Number | 241479-67-4 |
| Form | Solid |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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