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Fosfluconazole

Cat. No. M20959
Fosfluconazole Structure
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Biological Activity

Fosfluconazole is a water-soluble phosphate prodrug of fluconazole, which is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.

Chemical Information
Molecular Weight 386.25
Formula C13H13F2N6O4P
CAS Number 194798-83-9
Solubility (25°C) DMSO 19 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Ayano Tanzawa, et al. Microbiol Spectr. Fluconazole Population Pharmacokinetics after Fosfluconazole Administration and Dosing Optimization in Extremely Low-Birth-Weight Infants

[2] Daijiro Takahashi, et al. Int J Pediatr. Fosfluconazole for antifungal prophylaxis in very low birth weight infants

[3] Satoshi Sobue, et al. Br J Clin Pharmacol. The effects of hepatic impairment on the pharmacokinetics of fosfluconazole and fluconazole following a single intravenous bolus injection of fosfluconazole

[4] Yutaka Kawakami, et al. Nihon Yakurigaku Zasshi. [Nonclinical studies and clinical studies on fosfluconazole, a triazole antifungal agent (Prodif)]

[5] Satoshi Sobue, et al. Eur J Clin Pharmacol. Comparison of the pharmacokinetics of fosfluconazole and fluconazole after single intravenous administration of fosfluconazole in healthy Japanese and Caucasian volunteers

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