Liranaftate was launched in Japan as a new topical antifungal for the treatment of
dermatophycoses. This compound belonging to the thiocarbamate class of antifungals can
be prepared by condensation of 5,6，7,8-tetrahydro-2-naphthol with the corresponding Npyridylthiocarbamoyl
chloride. It is a potent and specific inhibitor of squalene epoxidase
and consequently a blocker of ergosterol biosynthesis in fungi, without any detectable
effect on mammalian cholesterol biosynthesis in rat liver at therapeutic dose levels.
Liranaftate was found to be significantly more active than the other thiocarbamate
tolnaftate against several dermatophytes, including Trichophyton mentagrophyfes, and
against certain yeasts, such as Crypfococcus neoformans. On the other hand, it was
inactive against a variety of Gram-positive and negative bacteria. When applicated as a 1 or 2% cream during clinical trials, it was well tolerated and no systemic absorption was observed.
