Naftifine Hydrochloride is the hydrochloride salt form of naftifine, an allylamine derivate with synthetic broad-spectrum antifungal activity. Although the exact mechanism through which naftifine hydrochloride exerts its effect is unknown, it appears to selectively inhibit the enzyme squalene 2, 3-epoxidase, thereby inhibiting the biosynthesis of sterol. This results in a decreased amount of sterols, especially ergosterol which is the primary fungal membrane sterol, and a corresponding accumulation of squalene in fungal cells. Naftifine hydrochloride (Naftifine HCl) can be fungicidal as well as fungistatic to yeasts depending on the concentration and the organisms involved.

Naftifine对多种真菌表现出了有趣的体外活性谱，包括对皮肤癣菌（38株；最小抑制浓度（MIC）范围0.1到0.2 mg/mL）、曲霉（6株；MIC范围0.8到12.5 mg/mL）、Sporothrix schenckii（2株；MICs为0.8和1.5 mg/mL）以及属于念珠菌属的酵母菌（77株；MIC范围1.5至大于100 mg/mL）[1]。对于C. albicans Δ63，在Sabouraud培养基中（初始pH 6.5）的MIC为100 mg/L。Naftifine（50 mg/L）能在整个细胞及C. albicans的细胞提取物中抑制超过99%的固醇生物合成。Naftifine的主要作用似乎是阻断真菌的角鲨烯环氧化作用[2]。

Naftifine HCl 2%霜剂在4周治疗后的临床治愈率和临床成功率分别为33%和84%，而在治疗第2周，Naftifine HCl 2%对象的有效反应率均低于第4周，但显著高于第2周接受载体处理的对照组。Naftifine通过干扰真菌的麦角固醇合成并在真菌细胞内积累角鲨烯而发挥作用。此外，Naftifine还展示出抗炎特性，比如减少超氧化物的产生和减轻多形核白细胞的趋化性/内皮黏附。Naftifine对多种条件显示出良好的疗效和安全性，是一种既提供抗真菌作用又能缓解炎症征状的有用治疗方法。使用Naftifine时记录的不良事件少，最常见的是应用部位出现轻微且短暂的燃烧感、刺痛感或瘙痒。