Six novel antimycotics.

Abstract

We have reviewed six new antimycotic agents which have potential applications for human cutaneous and mucosal diseases. Information on these six drugs was obtained via an English language search of PubMed through the US National Library of Medicine. The antimycotic agents reviewed include rilopirox, lanoconazole, NND-502, butenafine, eberconazole and voriconazole. Rilopirox is a synthetic pyridone derivative, related to ciclopirox, with a fungicidal action. Rilopirox is a hydrophobic, topical agent with potential application in mucosal candida infections, tinea versicolor and seborrheic dermatitis. Lanoconazole, an imidazole, is a topical agent with potential application in tinea infections and cutaneous candidiasis. The drug has been available for clinical use in Japan since 1994 and once-daily application to affected areas is recommended. In addition to its antifungal effect, animal data suggest that application of lanoconazole 0.5 or 1% cream is associated with accelerated wound healing. NND-502, a stereoselective analog of lanoconazole, is a topical agent with potential application in tinea pedis infection. NND-502 appears to be more effective in inhibiting ergosterol biosynthesis than lanoconazole or bifonazole and clinical trials comparing these agents are awaited. Butenafine is the first member of a new class of antifungals, the benzylamine derivatives, and has been approved for topical use in Japan (since 1992) and the US. Butenafine has a potent fungicidal action and the drug has been shown to be effective in multiple clinical trials in patients with tinea pedis, tinea corporis and tinea cruris. Butenafine has also been reported to exert an anti-inflammatory action after topical application and this may offer potential benefit over other topical antifungal agents. Eberconazole, an imidazole derivative, is a topical antifungal agent that has been shown to be effective in clinical trials in patients with tinea infections. Preliminary data indicate that the eberconazole is effective against some triazole-resistant yeasts such as Candida krusei and Candida glabrata. Voriconazole is an azole antifungal derivative of fluconazole. The drug is available in both oral and parenteral formulations. Oral voriconazole 200mg twice daily has been effective in treating oropharyngeal candidiasis and apergillosis in immunocompromised patients. After 12 weeks' treatment, a similar dosage of the drug elicited a positive response in 69% of nonimmunocompromised patients with invasive aspergillosis.