Ravuconazole (CAS 182760-06-1) is an orally available, third-generation triazole antifungal agent that demonstrates potent and broad-spectrum antifungal activity. It functions as a highly selective inhibitor of fungal cytochrome P450-dependent 14α-demethylase (CYP51), the key enzyme responsible for the conversion of lanosterol to ergosterol. By blocking ergosterol biosynthesis, Ravuconazole disrupts fungal cell membrane integrity, leading to cell lysis and fungal death. It is also known by the synonyms BMS-207147 and ER-30346.
Pharmacological Profile & Clinical Studies:
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Potent & Broad-Spectrum Activity: Ravuconazole exhibits strong in vitro and in vivo activity against a wide range of clinically significant fungal pathogens, including Candida spp. (including fluconazole-resistant strains), Cryptococcus neoformans, Aspergillus fumigatus, and various dermatophytes. Its in vitro activity against yeasts is approximately 2 to 4 times more potent than Itraconazole and up to 40 times more potent than Fluconazole. Ravuconazole has also demonstrated excellent activity against Fusarium solani and Pseudallescheria boydii, with MICs in the sub-microgram range.
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Superior Pharmacokinetic Profile: Ravuconazole possesses a remarkably long terminal half-life of approximately 100 hours in humans, supporting the potential for once-weekly or intermittent dosing regimens. It exhibits near-linear pharmacokinetics with high oral bioavailability. The water-soluble prodrug, Fosravuconazole (E1224), is rapidly and completely converted to the active Ravuconazole in vivo, achieving nearly 100% oral bioavailability, which significantly enhances its clinical utility.
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Clinical Efficacy: The clinical potential of Ravuconazole has been extensively investigated in Phase II and Phase III trials. In a Phase III study for the treatment of esophageal candidiasis in HIV patients, Ravuconazole demonstrated an 86% clinical cure rate, outperforming Fluconazole (78%). A separate Phase III trial evaluated Fosravuconazole (100 mg daily, equivalent to Ravuconazole, for 12 weeks) for onychomycosis (fungal nail infection), achieving a complete cure rate of 59.4% and a marked clinical improvement rate of 83.1% at 48 weeks post-treatment initiation. Ravuconazole has also shown in vitro activity against emerging pathogens such as Candida auris, with MIC90 values of 0.12–0.5 mg/L, positioning it as a promising candidate for multidrug-resistant fungal infections.
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Safety, Tolerability & Drug Interactions: Ravuconazole has been demonstrated to be well-tolerated in clinical studies, with the most common adverse events being mild-to-moderate laboratory abnormalities and gastrointestinal symptoms (nausea, diarrhea, abdominal discomfort). Importantly, no significant hepatotoxicity or nephrotoxicity has been associated with Ravuconazole therapy. Unlike several other azoles, Ravuconazole exhibits a low potential for drug-drug interactions due to its minimal inhibition of major CYP450 isoforms (CYP2C9, CYP2C19, CYP2D6, and CYP3A4), with food intake showing no significant effect on its absorption. Its tolerability profile appears superior to that of Itraconazole, with lower rates of hepatobiliary disorders and gastrointestinal adverse events.
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Product Applications:
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Pharmaceutical R&D: As a high-quality active pharmaceutical ingredient (API) for antifungal drug development, or as a reference standard for pharmaceutical analysis
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Quality Control: For quality control (QC) applications, analytical method development and validation (AMV), and impurity profiling studies
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Regulatory Submissions: Serves as a reference standard for impurity identification in ANDA and DMF regulatory filings
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Lifecycle Management: Suitable for use in forced degradation studies, stability indicating method development, and formulation optimization research
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Packaging: ___ (e.g.: 1g, 5g, 10g per package, as per customer's request)
Storage: Store in a cool, dry, well-ventilated area, away from direct sunlight and moisture. Recommended storage temperature: 2-8°C (Refrigerator) for long-term storage.
