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Posaconazole (hydrate)

Product NamePosaconazole (hydrate)
CAS1198769-38-8
MFC37H44F2N8O5
MW718.81
EINECS
MOL File1198769-38-8.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Powder

Usage And Synthesis

Uses

Posaconazole hydrate is a broad-spectrum, second generation, triazole compound with antifungal activity.

in vivo

Treatment of infected animals with amiodarone alone reduces parasitemia, increases survival 60 days pi (0% for untreated controls vs 40% for amiodarone-treated animals) and, when given in combination with Posaconazole, delays the development of parasitemia^[1]. Coadministration of Posaconazole and Boost Plus increases drug exposure compared to the administration of Posaconazole alone in the fasted state. Food, particularly meals high in fat content, significantly increases Posaconazole bioavailability. Systemic exposure to Posaconazole increases 4- and 2.6-fold when it is consumed with a high-fat and nonfat meal, respectively^[3]. Posaconazole and Amiodarone may constitute an effective anti-T. cruzi therapy with low side effect^[4]. At twice-daily doses of ≥ 15 mg/kg of body weight, Posaconazole prolongs the survival of the mice and reduces tissue burden^[5].

References

[1] Benaim G, et al. Amiodarone has intrinsic anti-Trypanosoma cruzi activity and acts synergistically with posaconazole. J Med Chem. 2006 Feb 9;49(3):892-9. DOI:10.1021/jm050691f
[2] Sabatelli F, et al. In vitro activities of posaconazole, fluconazole, itraconazole, voriconazole, and amphotericin B against a large collection of clinically important molds and yeasts. Antimicrob Agents Chemother. 2006 Jun;50(6):2009-15. DOI:10.1128/AAC.00163-06
[3] Sansone-Parsons A, et al. Effect of a nutritional supplement on posaconazole pharmacokinetics following oral administration to healthy volunteers. Antimicrob Agents Chemother. 2006 May;50(5):1881-3. DOI:10.1128/AAC.50.5.1881-1883.2006
[4] Veiga-Santos P, et al. Effects of amiodarone and posaconazole on the growth and ultrastructure of Trypanosoma cruzi. Int J Antimicrob Agents. 2012 Jul;40(1):61-71. DOI:10.1016/j.ijantimicag.2012.03.009
[5] Sun QN, et al. In vivo activity of posaconazole against Mucor spp. in an immunosuppressed-mouse model. Antimicrob Agents Chemother. 2002 Jul;46(7):2310-2. DOI:10.1128/AAC.46.7.2310-2312.2002

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