ME1111 is a novel, topically active antifungal agent[1-2]. ME1111 effectively inhibits the growth of pathogenic fungi such as dermatophytes, while reaching infection sites through its strong nail-penetrating ability. ME1111 can be utilized in research related to onychomycosis and other fungal infections[3-4].
In vitro, ME1111 (0.06–32μg/mL) was incubated with K562, HepG2, U937, and A431 cells for 72 hours. ME1111 exhibited half-maximal inhibitory concentrations (IC50) ranging from 33 to 47μg/mL against these four human cell lines[5]. ME1111 (0.004–8μg/mL) was also incubated with Trichophyton rubrum strains (MRL 28661, 28663, 28669, 28674, and 28675) and Trichophyton mentagrophytes strains (MRL 27777, 28313, 28360, 28556, and 28641) for 96 hours. ME1111 significantly inhibited the growth of these dermatophytes, with an average IC50 of 0.5μg/mL[6].
In vivo, ME1111 (10% solution) was topically applied once daily for seven consecutive days in a guinea pig model of dermatophyte infection (lesion area: 2.5cm²). ME1111 demonstrated significantly superior clinical and mycological efficacy compared to both the control group (saline treatment) and the positive control group (8% ciclopirox treatment)[7].
References:
[1] Hui X, Jung EC, Zhu H, et al. Antifungal ME1111 in vitro human onychopharmacokinetics. Drug Dev Ind Pharm. 2017 Jan;43(1):22-29.
[2] Takei-Masuda N, Nagira Y, Kubota-Ishida N, et al. Antidermatophyte activity and PK/PD of ME1111 in a guinea pig model of tinea corporis. J Antibiot (Tokyo). 2024 Aug;77(8):533-539.
[3] Khalfe Y, Rosen T. Future Fungal Fighters in Dermatology: Novel Antifungal Drug Pipeline. J Drugs Dermatol. 2022 May 1;21(5):496-501.
[4] Takahata S, Kubota N, Takei-Masuda N, et al. Mechanism of Action of ME1111, a Novel Antifungal Agent for Topical Treatment of Onychomycosis. Antimicrob Agents Chemother. 2015 Nov 23;60(2):873-80.
[5] Tabata Y, Takei-Masuda N, Kubota N, et al. Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis. Antimicrob Agents Chemother. 2015 Dec 7;60(2):1035-9.
[6] Ghannoum M, Chaturvedi V, Diekema D, et al. Multilaboratory Evaluation of In Vitro Antifungal Susceptibility Testing of Dermatophytes for ME1111. J Clin Microbiol. 2016 Mar;54(3):662-5.
[7] Long L, Hager C, Ghannoum M. Evaluation of the Efficacy of ME1111 in the Topical Treatment of Dermatophytosis in a Guinea Pig Model. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2343-5.
ME1111是一种新型的、具有局部治疗活性的抗真菌药物[1-2]。ME1111可有效抑制皮肤癣菌等致病真菌的生长，同时通过良好的指甲穿透性以到达感染部位。ME1111可用于甲癣和相关真菌感染的相关研究[3-4]。
在体外，ME1111（0.06–32μg/mL）孵育K562、HepG2、U937、A431细胞72小时，ME1111细胞对四种人类细胞系的半数抑制浓度（IC50）为33至47μg/mL[5]。ME1111（0.004–8μg/mL）孵育Trichophyton. rubrum（MRL 28661，28663，28669，28674和28675），Trichophyton. mentagrophytes（MRL 27777，28313，28360，28556和28641）96小时，ME1111可显著抑制这些皮肤癣菌的生长，平均IC50为0.5μg/mL[6]。
在体内，ME1111（10%溶液）每天一次局部用药连续七天，处理豚鼠背部皮肤癣菌感染模型（伤口面积为2.5cm2）。ME1111在临床和真菌学疗效上均显著优于对照组（生理盐水处理）和阳性对照组（8%环吡酮处理）[7]。