Efficacy of terbinafine compared to lanoconazole and luliconazole in the topical treatment of dermatophytosis in a guinea pig model

Ghannoum, Mahmoud A.; Long, Lisa; Kim, H. G.; Cirino, A.J.; Miller, Anthony R.; Mallefet, Pascal

doi:10.3109/13693780903373811

Cited by 30 publications

(21 citation statements)

References 13 publications

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“…In vitro studies with a limited number of isolates have also reported potent activity of this agent against dermatophytes and other causative agents of dermatophytosis, including onychomycosis (8)(9)(10). Results from animal models and small clinical studies have also suggested in vivo efficacy against dermatophytosis (11)(12)(13). Our objective was to measure the in vitro activity of luliconazole against dermatophytes isolated at screening from toenails in an ongoing phase 2b/3 study of patients with mild to moderate toenail onychomycosis (www.clinicaltrials.gov, identifier NCT01431820).…”

mentioning

confidence: 99%

Luliconazole Demonstrates Potent In Vitro Activity against Dermatophytes Recovered from Patients with Onychomycosis

Wiederhold

Fothergill

McCarthy

et al. 2014

Antimicrob Agents Chemother

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The in vitro activities of luliconazole, amorolfine, ciclopirox, and terbinafine were determined against 320 dermatophyte isolates from large toenails of onychomycosis patients enrolled into an ongoing phase 2b/3 clinical study. The geometric mean MIC for luliconazole was 0.00022 g/ml against all isolates, compared to 0.0194 to 0.3107 g/ml for the three other agents. The in vitro potency of luliconazole was maintained regardless of the dermatophyte species.O nychomycosis (tinea unguium) is a fungal infection of the nail bed and or plate and is associated with significant morbidity (1). Besides causing cosmetic concerns, this mycosis can result in pain or discomfort, acute bacterial cellulitis associated with spread of infection to the skin, and social stigma (2, 3). The prevalence of onychomycosis is estimated to be between 2 and 14%, with a rate of 13.8% reported in North America (1, 4). Risk factors for infection include increasing age, male gender, dystrophic nails, tinea pedis, and poor peripheral circulation (1, 3, 4). These infections are caused primarily by dermatophytes, including Trichophyton rubrum and T. mentagrophytes, and to a lesser extent by other dermatophytes (e.g., Epidermophyton floccosum), Candida species, and nondermatophytic molds (e.g., Acremonium, Fusarium, and Scopulariopsis species) (5, 6). Luliconazole is a novel imidazole currently under development. Pharmacokinetic and safety results from phase 1 studies in patients with onychomycosis have demonstrated high concentrations of luliconazole within the nail plates of the great toe and have shown that this agent is well tolerated when administered as a 10% solution (7). In vitro studies with a limited number of isolates have also reported potent activity of this agent against dermatophytes and other causative agents of dermatophytosis, including onychomycosis (8-10). Results from animal models and small clinical studies have also suggested in vivo efficacy against dermatophytosis (11-13). Our objective was to measure the in vitro activity of luliconazole against dermatophytes isolated at screening from toenails in an ongoing phase 2b/3 study of patients with mild to moderate toenail onychomycosis (www.clinicaltrials.gov, identifier NCT01431820). In addition, the in vitro activities of amorolfine, ciclopirox, and terbinafine, three products approved and most often used for treatment of onychomycosis in the United States and the European Union, were also determined.Three hundred twenty dermatophytes obtained from patients with confirmed toenail onychomycosis (positive KOH and culture and clinical diagnosis) during screening were used in this study. This included 308 Trichophyton rubrum and 10 T. mentagrophytes isolates and one each of Trichophyton tonsurans and Epidermophyton floccosum. All isolates were clinical strains that had been freshly subcultured and not previously frozen. Stock solutions of amorolfine, ciclopirox, terbinafine, and luliconazole were prepared in dimethyl sulfoxide (DMSO) and further diluted in RPMI 1640 buffered to a...

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confidence: 99%

Luliconazole Demonstrates Potent In Vitro Activity against Dermatophytes Recovered from Patients with Onychomycosis

Wiederhold

Fothergill

McCarthy

et al. 2014

Antimicrob Agents Chemother

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“…Recently, in vitro antifungal susceptibility testing of lanoconazole and luliconazole demonstrated potent efficacy against Trichophyton rubrum and Epidermophyton floccosum (9)(10)(11)(12)(13)(14). In addition, animal studies and small human series suggested that luliconazole and lanoconazole are effective in treating dermatophytosis and onychomycosis (15,16). Only limited data on the in vitro activity of lanoconazole and luliconazole against Aspergillus species are available.…”

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confidence: 99%

Potent Activities of Novel Imidazoles Lanoconazole and Luliconazole against a Collection of Azole-Resistant and -Susceptible Aspergillus fumigatus Strains

Abastabar

Rahimi

Meis

et al. 2016

Antimicrob Agents Chemother

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A collection of azole-susceptible (n ‫؍‬ 141) and azole-resistant (n ‫؍‬ 27) Aspergillus fumigatus isolates was tested against seven antifungal drugs, including the new imidazoles lanoconazole and luliconazole. The luliconazole and lanoconazole MIC 90 values for the azole-susceptible strains were 0.001 g/ml and 0.008 g/ml, and those for the azole-resistant strains were 0.016 g/ml and 0.032 g/ml.

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“…The total score for any treatment group signifies the average clinical score from animals in the same group. 21 …”

Section: Animal Grouping and Dosingmentioning

confidence: 99%

“…An animal infection model of dandruff was performed according to protocol of Tatsumi et al 20 and Ghannoum et al 21 with little modification. Before inoculation, the hairs of both flanks at upper left side and lower right side skin (3 cm ×3 cm) of each rat were removed by electric hair clipper (MOSER, Germany) followed by the application of hair remover cream for complete removal of hairs.…”

Section: In Vivo Efficacy Of Ag Nano Animal Model For Dandruffmentioning

confidence: 99%

Size- and shape-dependent clinical and mycological efficacy of silver nanoparticles on dandruff

Anwar¹,

Yadav²,

Jain³

et al. 2016

IJN

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Dandruff is a prominent scalp problem caused by the growth of fungus Malassezia furfur , potentially cascading into dermal inflammation, itching, and tissue damage. The present work outlines a detailed analysis of the treatment of scalp infection using silver nanomaterials (Ag NMs), and focuses on biocidal activity owing to manipulation of size, shape, and structure. Monodisperse silver spherical nanoparticles (NPs) and nanorods (NRs) were synthesized by chemical routes that were characterized using analytical and spectroscopic techniques. Ag NMs demonstrated enhanced biocidal tendencies compared to market available drugs, itracanozole and ketoconazole, showing greater zones of inhibition. The obtained 20 nm and 50 nm spherical-shaped NPs and 50 nm NRs showed concentration-, size-, and shape-dependent antifungal activity, with 20 nm spherical-shaped NPs exhibiting excellent potency. Minimum inhibitory concentration for 20 nm was lowest at 0.2 mg/mL in comparison to 0.3 mg/mL for NRs. Primary irritation index was 0.33 and 0.16 for 20 nm and 50 nm spherical-shaped NPs, respectively, while 50 nm rod-shaped NMs exhibited negligible redness. An in vivo model for M. furfur infection was generated by passing fungi subcutaneously in rats’ skin. Again, 20 nm particles showed best normalization of skin after 10 days on regular dosing, in comparison with bigger and rod-shaped particles. The statistical clinical score was highest for Ag nanorods, followed by 50 nm Ag NPs-treated animals. It was observed that 20 nm spherical particles exhibited the lowest score (0) compared with others as well as with antifungal drugs. Biochemical analysis performed by checking antioxidant enzymatic activities indicated tissue repair and normalization of enzymes and protein concentration by Ag NPs.

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Efficacy of terbinafine compared to lanoconazole and luliconazole in the topical treatment of dermatophytosis in a guinea pig model

Cited by 30 publications

References 13 publications

Luliconazole Demonstrates Potent In Vitro Activity against Dermatophytes Recovered from Patients with Onychomycosis

Luliconazole Demonstrates Potent In Vitro Activity against Dermatophytes Recovered from Patients with Onychomycosis

Potent Activities of Novel Imidazoles Lanoconazole and Luliconazole against a Collection of Azole-Resistant and -Susceptible Aspergillus fumigatus Strains

Size- and shape-dependent clinical and mycological efficacy of silver nanoparticles on dandruff

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