Rezafungin acetate is a novel echinocandin-based antifungal agent with potent antifungal activity against Candida, Aspergillus and Pneumocystis. Rezafungin has higher stability and greater solubility in plasma, aqueous and buffered solutions.
Rezafungin exerted its fungicidal effect by specifically binding to β-( 1,3)-glucan synthase and inhibiting β-( 1,3)-glucose synthesis, thereby preventing fungal cell wall formation. The minimum inhibitory concentrations (MIC90) of Rezafungin against 90.0% of wild and fluconazole-resistant strains of Candida albicans, Candida smoothis and Candida tropicalis were 0.06, 0.12 and 0.03 mg/L, respectively.
The 10-days survival rate of Rezafungin (2 mg/kg; single dose administration) treatment in mice with disseminated infection of Aspergillus fumigatus was 100%, which was significantly higher than that of the blank control (20.0%), and comparable to the effect of 3 mg/kg single dose intraperitoneal injection of amphotericin B.
| Molecular Weight | 1285.44 |
| Formula | C65H88N8O19 |
| CAS Number | 1631754-41-0 |
| Solubility (25°C) | DMSO >100 mg/mL |
| Storage | 4°C, dry, sealed |
| 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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