ERTACZO Cream Ref.[50723] Active ingredients: Sertaconazole

In a multiple-dose pharmacokinetic trial that included 5 male subjects with interdigital tinea pedis (range of diseased area, 42-140 cm²; mean, 93 cm²), ERTACZO cream, 2%, was topically applied every 12 hours for a total of 13 doses to the diseased skin (0.5 g sertaconazole nitrate per 100 cm²). Sertaconazole concentrations in plasma measured by serial blood sampling for 72 hours after the thirteenth dose were below the limit of quantitation (2.5 ng/mL) of the analytical method used.

Mechanism of Action

Sertaconazole, an azole antifungal agent, inhibits fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylase enzyme. This enzyme functions to convert lanosterol to ergosterol. Ergosterol is a key component of fungal cell membranes and lack of this component leads to fungal cell injury by leakage of key constituents in the cytoplasm from the cell.

Activity In Vitro and in Clinical Infections

Sertaconazole nitrate has been shown to be active against isolates of the following microorganisms in clinical infections [see Indications and Usage (1)]:

Trichophyton rubrum
Trichophyton mentagrophytes
Epidermophyton floccosum

In a 2-year rat dermal carcinogenicity study, topical administration of sertaconazole nitrate cream did not increase the number of neoplastic lesions compared to control animals, at sertaconazole nitrate doses of up to 800 mg/kg/day (200 times the MRHD based on a BSA comparison).

No clastogenic potential was observed in a mouse micronucleus test. Sertaconazole nitrate was nonclastogenic in the in vivo mouse sister chromatid exchange assay. There was no evidence that sertaconazole nitrate induced unscheduled DNA synthesis in primary rat hepatocyte cultures.

Rats treated orally with up to 160 mg/kg/day of sertaconazole nitrate (40 times the MRHD based on a BSA comparison), exhibited no toxicity or adverse effects on reproductive performance or fertility in male or female rats.

In two randomized, double-blind clinical trials, subjects 12 years and older with interdigital tinea pedis applied either ERTACZO cream, 2%, or vehicle, twice daily for 4 weeks. Subjects with moccasin-type (plantar) tinea pedis and/or onychomycosis were excluded from the trial. Two weeks after completion of therapy (6 weeks after beginning therapy), subjects were evaluated for signs and symptoms related to interdigital tinea pedis.

Treatment outcomes are summarized in the table below.

^* Complete Cure – Patients who had complete clearing of signs and symptoms and Mycological Cure.
^** Effective Treatment – Patients who had minimal residual signs and symptoms of interdigital tinea pedis and Mycological Cure.
^*** Mycological Cure – Patients who had both negative microscopic KOH preparation and negative fungal culture.

In clinical trials, complete cure in ERTACZO cream, 2%-treated subjects was achieved in 32 of 160 (20%) subjects with Trichophyton rubrum, in 7 of 28 (25%) subjects with Trichophyton mentagrophytes, and in 1 of 13 (15%) subjects with Epidermophyton floccosum.