Efinaconazole 10% solution in the treatment of toenail onychomycosis: Two phase III multicenter, randomized, double-blind studies

Elewski, Boni E.; Rich, Phoebe; Pollak, Richard; Pariser, David M.; Watanabe, Shinichi; Senda, Hisato; Ieda, Chikara; Smith, Kathleen; Pillai, Radhakrishnan; Ramakrishna, Tage; Olin, Jason T.

doi:10.1016/j.jaad.2012.10.013

Cited by 197 publications

(202 citation statements)

References 28 publications

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“…Although both oral (terbinafine and itraconazole) and topical (ciclopirox, amorolfine, efinaconazole, and tavaborole) medications are available for the treatment of fungal nail infection, these agents suffer from a number of disadvantages: (i) oral onychomycosis drugs can cause liver toxicity issues and/or drug-drug interaction concerns (6), making them difficult to prescribe to elderly patients, especially those taking multiple medications, and (ii) the efficacy of topical therapeutics is relatively low, presumably due to poor nail permeability and high keratin binding. Additionally, the recently approved topical drugs efinaconazole (7)(8)(9) and tavaborole (6,10) have problems of low efficacy and local side effects. As a result of the various drawbacks of currently available therapeutics, there is an opportunity for the development of new topical agents with greater efficacy and fewer side effects.…”

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confidence: 99%

Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis

Tabata

Takei-Masuda

Kubota

et al. 2016

Antimicrob Agents Chemother

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Fungal nail infection (onychomycosis) is a prevalent disease in many areas of the world, with a high incidence approaching 23%. Available antifungals to treat the disease suffer from a number of disadvantages, necessitating the discovery of new efficacious and safe antifungals. Here, we evaluate the in vitro antifungal activity and nail penetration ability of ME1111, a novel antifungal agent, along with comparator drugs, including ciclopirox, amorolfine, terbinafine, and itraconazole. ME1111 showed potent antifungal activity against Trichophyton rubrum and Trichophyton mentagrophytes (the major etiologic agents of onychomycosis) strains isolated in Japan and reference fungal strains with an MIC range of 0.12 to 0.5 mg/liter and an MIC 50 and MIC 90 of 0.5 mg/liter for both. Importantly, none of the tested isolates showed an elevated ME1111 MIC. Moreover, the antifungal activity of ME1111 was minimally affected by 5% wool keratin powder in comparison to the other antifungals tested. The ME1111 solution was able to penetrate human nails and inhibit fungal growth in a dose-dependent manner according to the TurChub assay. In contrast, 8% ciclopirox and 5% amorolfine nail lacquers showed no activity under the same conditions. ME1111 demonstrated approximately 60-fold-greater selectivity in inhibition of Trichophyton spp. than of human cell lines. Our findings demonstrate that ME1111 possesses potent antidermatophyte activity, maintains this activity in the presence of keratin, and possesses excellent human nail permeability. These results suggest that ME1111 is a promising topical medication for the treatment of onychomycosis and therefore warrants further clinical evaluation.

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confidence: 99%

Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis

Tabata

Takei-Masuda

Kubota

et al. 2016

Antimicrob Agents Chemother

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“…The newer topical products efinaconazole 10% and tavabarole 5%, were approved for the treatment of onychomycosis of toenails due to Trichophyton rubrum or Trichophton mentagrophytes. 7,8 The efficacy in the phase III trials was better than previously available topical antifungals, but remains below that of oral agents such as terbinafine and itraconazole, [9][10][11][12][13][14][15][16][17][18] Even with oral therapy in onychomycosis, recurrence rates…”

Section: Methodsmentioning

confidence: 99%

Efinaconazole 10% and Tavaborole 5% Penetrate Across Poly-ureaurethane 16%: Results of In Vitro Release Testing and Clinical Implications of Onychodystrophy in Onychomycosis

Adigun¹,

Vlahovic²,

McClellan³

et al. 2017

J of Skin

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“…Efinaconazole is an inhibitor of sterol 14α-demethylase and possess broad spectrum antifungal activity against dermatophytes, yeasts and non-dermatophyte molds. It is approved for use in Canada and the USA as a 10% topical solution for the treatment of onychomycosis [66,67].…”

Section: Newer Topical Solutionsmentioning

confidence: 99%

Is This the Right Drug or the Dose for the Management of Onychomycosis?

Thatai¹,

Sapra²

2017

J Cosmo Trichol

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Efinaconazole 10% solution in the treatment of toenail onychomycosis: Two phase III multicenter, randomized, double-blind studies

Cited by 197 publications

References 28 publications

Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis

Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis

Efinaconazole 10% and Tavaborole 5% Penetrate Across Poly-ureaurethane 16%: Results of In Vitro Release Testing and Clinical Implications of Onychodystrophy in Onychomycosis

Is This the Right Drug or the Dose for the Management of Onychomycosis?

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