Fosfluconazole

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Structural formula
Structure of fosfluconazole
General
Non-proprietary name Fosfluconazole
other names
  • 2,4-Difluoro-α, α-bis (1 H -1,2,4-triazol-1-ylmethyl) benzyl alcohol dihydrogen phosphate ( IUPAC )
  • Fosfluconazolum ( Latin )
  • UK 292 (Pfizer)
  • UK 663 (Pfizer)
Molecular formula C 13 H 13 F 2 N 6 O 4 P
External identifiers / databases
CAS number 194798-83-9
PubChem 214356
Wikidata Q1439361
Drug information
ATC code

J02 AC

Drug class

Antifungal drugs

properties
Molar mass 386.25 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Fosfluconazole is an antifungal from the triazole group and an ester of the also antifungal active fluconazole with phosphoric acid . It inhibits the ergosterol biosynthesis.

pharmacology

Fosfluconazole inhibits 14 α- demethylase, a fungus-specific cytochrome P450 isoenzyme ( CYP51A1 ), which is responsible for the conversion of lanosterol into ergosterol . Ergosterol precursors are built into the membrane and the permeability for cell components increases.

Finished medicinal products

Prodif ( J )

There are no approvals in Germany, Austria and Switzerland.

literature

  • Synthesis: Bentley A et al. The Discovery and Process Development of a Commercial Route to the Water Soluble Prodrug, Fosfluconazole. Organic process, research and development (2002); 6 (2): 105-112; doi : 10.1021 / op010064 .
  • Pharmacology: Sobue S et al. Pharmacokinetics and safety of Fosfluconazole after single intravenous bolus injection in healthy male Japanese volunteers . In: J Clin Pharmacol 2002; 44 (3): 284-292; PMID 14973307 .
  • Studies: Kawakami Y et al. Nonclinical studies and clinical studies on fosfluconazole, a triazole antifungal agent (Prodif). Nippon Yakurigaku Zasshi 2004; 124 (1): 41-51; PMID 15226621 .

Individual evidence

  1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.