Posaconazole (POS) is a new triazole drug with broad-spectrum in vitro activity against most yeasts and molds such as Candida, Cryptococcus neoformans, Aspergillus, Fusarium and Zygomycetes, as well as certain species of dimorphic fungi and endemic fungi. In immunocompetent or immunocompromised animal models with invasive fungal infections, POS has demonstrated highly effective, broad-spectrum antifungal activities. In vitro and in vivo antifungal activities of POS were superior to those of other azoles against Candida glabrata, Candida krusei, Aspergillus terrus, Fusarium and Zygomycetes. In vivo susceptibility studies have shown promising efficacy of POS against life-threatening fungal infections in animal models with different immune status and infection sites.
1. Galgiani JN, Lewis ML. In vitro studies of activities of the antifungal triazoles SCH56592 and itraconazole against Candida albicans, Cryptococcus neoformans, and other pathogenic yeasts. Antimicrob Agents Chemother 1997;41:180-3.
2. Pfaller MA, Messer SA, Boyken L, Hollis RJ, Rice C, Tendolkar S, et al. In vitro activities of voriconazole, posaconazole, and fluconazole against 4,169 clinical isolates of Candida spp. and Cryptococcus neoformans collected during 2001 and 2002 in the ARTEMIS global antifungal surveillance program. Diagn Microbiol Infect Dis 2004;48:201-5.
3. Ostrosky-Zeichner L, Rex JH, Pappas PG, Hamill RJ, Larsen RA, Horowitz HW, et al. Antifungal susceptibility survey of 2,000 bloodstream Candida isolates in the United States. Antimicrob Agents Chemother 2003;47:3149-54.
4. Yildiran ST, Fothergill AW, Sutton DA, Rinaldi MG. In vitro susceptibilities of cerebrospinal fluid isolates of Cryptococcus neoformans collected during a ten-year period against fluconazole, voriconazole and posaconazole (SCH56592). Mycoses 2002;45:378-83.
5. Pfaller MA, Messer SA, Boyken L, Rice C, Tendolkar S, Hollis RJ, et al. Global trends in the antifungal susceptibility of Cryptococcus neoformans (1990-2004). J Clin Microbiol 2005;43:2163-7.
6. Langner S, Staber PB, Neumeister P. Posaconazole in the management of refractory invasive fungal infections. Ther Clin Risk Manag 2008;4:747-58.
7. Torres HA, Hachem RY, Chemaly RF, Kontoyiannis DP, Raad II. Posaconazole: A broad-spectrum triazole antifungal. Lancet Infect Dis 2005;5:775-85.
8. Sun QN, Fothergill AW, McCarthy DI, Rinaldi MG, Graybill JR. In vitro activities of posaconazole, itraconazole, voriconazole, amphotericin B, and fluconazole against 37 clinical isolates of zygomycetes. Antimicrob Agents Chemother 2002;46:1581-2.
9. Barchiesi F, Arzeni D, Camiletti V, Simonetti O, Cellini A, Offidani AM, et al. In vitro activity of posaconazole against clinical isolates of dermatophytes. J Clin Microbiol 2001;39:4208-9.
10. Nucci M, Akiti T, Barreiros G, Silveira F, Revankar SG, Sutton DA, et al. Nosocomial fungemia due to Exophiala jeanselmei var. jeanselmei and a Rhinocladiella species: Newly described causes of bloodstream infection. J Clin Microbiol 2001;39:514-8.
11. Xia L, Liu L, Fu D. A novel broad-spectrum triazole antifungal, pasaconazozle. Chin J New Drugs 2007;16:1226-31.
12. Barchiesi F, Schimizzi AM, Najvar LK, Bocanegra R, Caselli F, Di Cesare S, et al. Interactions of posaconazole and flucytosine against Cryptococcus neoformans. Antimicrob Agents Chemother 2001;45:1355-9.
13. Groll AH, Walsh TJ. Antifungal efficacy and pharmacodynamics of posaconazole in experimental models of invasive fungal infections. Mycoses 2006;49:S7-16.
14. Petraitiene R, Petraitis V, Groll AH, Sein T, Piscitelli S, Candelario M, et al. Antifungal activity and pharmacokinetics of posaconazole (SCH 56592) in treatment and prevention of experimental invasive pulmonary aspergillosis: Correlation with galactomannan antigenemia. Antimicrob Agents Chemother 2001;45:857-69.
16. Sun QN, Najvar LK, Bocanegra R, Loebenberg D, Graybill JR. In vivo activity of posaconazole against Mucor spp. in an immunosuppressedmouse model. Antimicrob Agents Chemother 2002;46:2310-2.
17. Dannaoui E, Meis JF, Loebenberg D, Verweij PE. Activity of posaconazole in treatment of experimental disseminated zygomycosis. Antimicrob Agents Chemother 2003;47:3647-50.
18. GonzrtherbsdsTijerina R, Najvar LK, Bocanegra R, Rinaldi MG, Loebenberg D, et al. Activity of posaconazole against Pseudallescheria boydii: In vitro and in vivo assays. Antimicrob Agents Chemother 2003;47:1436-8.
19. Graybill JR, Najvar LK, Johnson E, Bocanegra R, Loebenberg D. Posaconazole therapy of disseminated phaeohyphomycosis in a murine model. Antimicrob Agents Chemother 2004;48:2288-91.
20. Perea S, Gonzalez G, Fothergill AW, Sutton DA, Rinaldi MG. In vitro activities of terbinafine in combination with fluconazole, itraconazole, voriconazole, and posaconazole against clinical isolates of Candida glabrata with decreased susceptibility to azoles. J Clin Microbiol 2002;40:1831-3.
21. Oliveira ER, Fothergill AW, Kirkpatrick WR, Coco BJ, Patterson TF, Redding SW. In vitro interaction of posaconazole and caspofungin against clinical isolates of Candida glabrata. Antimicrob Agents Chemother 2005;49:3544-5.
22. Cacciapuoti A, Gurnani M, Halpern J, Norris C, Patel R, Loebenberg D. Interaction between posaconazole and amphotericin B in concomitant treatment against Candida albicans in vivo. Antimicrob Agents Chemother 2005;49:638-42.
23. Barchiesi F, Spreghini E, Schimizzi AM, Maracci M, Giannini D, Carle F, et al. Posaconazole and amphotericin B combination therapy against Cryptococcus neoformans infection. Antimicrob Agents Chemother 2004;48:3312-6.
24. Saoulidis S, Simitsopoulou M, Dalakiouridou M, Walsh TJ, Wheat LJ, Papaioannidou P, et al. Antifungal activity of posaconazole and granulocyte colony-stimulating factor in the treatment of disseminated zygomycosis (mucormycosis) in a neutropaenic murine model. Mycoses 2011;54:e486-92.