Naftifine was invented at the Sandoz Research Institute in Vienna, Austria.

[1] Naftifine has triple action: antifungal, antibacterial, and anti-inflammatory.

Its fungistatic activity is believed to be based on inhibition of the squalene-2,3-epoxidase enzyme, which in turn results in the shortage of ergosterol required for the formation of fungal cell membranes.

With some fungal species, there is also fungicidal activity from a resulting accumulation of squalenes, leading to damage of the fungal cell membranes, including at the endoplasmatic reticulum.

[citation needed] Naftifine is almost completely metabolized in the human body, with a half-life of 2–3 days.