Voriconazole: A New Triazole Antifungal Agent

Abstract
The 1990s witnessed an expansion of the antifungal armamentarium to include 2 new azole agents, fluconazole and itraconazole. These agents changed our approach to treating many fungal infections. However, neither was an ideal agent. Itraconazole was plagued by absorption problems; fluconazole had a limited spectrum of antifungal activity, and resistance was soon noted in immunosuppressed hosts who received long-term treatment. Second-generation triazole agents have been in development for the past decade. The first of these new agents to receive approval from the US Food and Drug Administration (FDA) is voriconazole, a synthetic derivative of fluconazole. Replacement of one of the triazole rings with a fluorinated pyrimidine and the addition of an α-methyl group resulted in expanded activity, compared with that of fluconazole. The development of voriconazole proceeded primarily because of this broadened antifungal spectrum.

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