SKU: P139

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Description

Posaconazole is broad-spectrum second generation triazole compound with antifungal activity. It also has potent trypanocidal activity.

    CAS Number

    171228-49-2

    Molecular Formula

    C37H42F2N8O4

    Molecular Weight

    700.78

    Mechanism of Action

    Posaconazole blocks ergosterol synthesis, by inhibiting the enzyme lanosterole 14a-demethylase. The result is an accumulation of methylated sterol precursors. It also inhibits CYP3A4, but does not inhibit the activity of other CYP enzymes.

    Storage Conditions

    -20°C

    Tariff Code

    2934.99.3000

    Spectrum

    Broad-spectrum antifungal activity including yeast (Candida) and molds (Aspergillus) spp. Also effective parasitological cure in a murine model of Chagas disease caused by Trypanosoma cruzi.

Applications

    Microbiology Applications

    Posaconazole was assessed against approximately 19,000 clinically important strains of yeast and mold in a lab-wide study with 200 medical centers participating over a 10-year time span. Strains were tested using using broth microdilution methods. Against all fungi in the database, the MIC50 and MIC90 were 0.063 and 1 ug/ml respectively. For molds, it was equal to or more active than comparator compounds. It was active against isolates of Candida and Aspergillus that are resistant to Fluconazole, Voriconazole, and Amphotericin B (Sabatelli et al, 2006). The in vivo efficacy of Poscanazole was studied in a murine model against four Aspergillus fumigatus isolates. MIC values ranged from 0.03-16 mg/L. Resistance mechanisms included substitutions in the cyp51A gene. (Mavridou et al, 2010).

Specifications

    Form

    Powder

    Appearance

    White to off-white crystalline powder

    Source

    Synthetic

References

    References

    Chen CK (2010) Structural characterization of CYP51 from Trypanosoma cruzi and Trypanosoma brucei bound to the antifungal drugs posaconazole and fluconazole. PLoS Negl Trop Dis. 4(4):e651 PMID 20386598 Mavridou E, Brüggemann RJ, Melchers WJ, Mouton JW, Verweij PE (2010) Efficacy of Posaconazole against three clinical Aspergillus fumigatus isolates with mutations in the cyp51A gene. Antimicrob. Agents Chemother. 54(2):860-865 PMID 19917751 Sabatelli F et al (2006) In vitro activities of posaconazole, fluconazole, itraconazole, voriconazole, and amphotericin B against a large collection of clinically important molds and yeasts. Antimicrob. Agents Chemother. 50(6):2009-2015 PMID 16723559

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