ArticleAntimicrobial agents and chemotherapy2014
The low keratin affinity of efinaconazole contributes to its nail penetration and fungicidal activity in topical onychomycosis treatment.
Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 88 citations in OpenAlex.
- Trial
- Efficacy of long-term treatment with efinaconazole 10% solution in patients with onychomycosis, including severe cases: A multicenter, single-arm study.The Journal of dermatology · 2019Trial
- Antifungal efficacy of a novel nitric oxide releasing solution in the presence of keratin.Frontiers in cellular and infection microbiology · 2026Article
- Onychomycosis in Diabetics: A Common Infection with Potentially Serious Complications.Life (Basel, Switzerland) · 2025Review
- Lipid-based nanoformulations in onychomycosis therapy: addressing challenges of current therapies and advancing treatment.RSC advances · 2025Review
- Safety and Efficacy of a 48-Month Efinaconazole 10% Solution Treatment/Maintenance Regimen: 24-Month Daily Use Followed by 24-Month Intermittent Use.Infectious disease reports · 2025Article
- Concealing Meets Healing in the Treatment of Toenail Onychomycosis: A Review of Concurrent Nail Polish Use with Topical Efinaconazole 10% Solution.The Journal of clinical and aesthetic dermatology · 2024Review
- Transungual Penetration and Antifungal Activity of Prescription and Over-the-Counter Topical Antifungals: Ex Vivo Comparison.Dermatology and therapy · 2024Article
- Antifungal Selection for the Treatment of Onychomycosis: Patient Considerations and Outcomes.Infection and drug resistance · 2024Review
- Azorean Black Tea (Molecules (Basel, Switzerland) · 2023Article
- Design, Development, and Evaluation of Constant Voltage Iontophoresis for the Transungual Delivery of Efinaconazole.Pharmaceutics · 2023Article
- Evaluation of Topical Antifungals Using a New Predictive Animal Model for Efficacy against Severe Tinea Unguium: A Comparison of Efinaconazole and Luliconazole.Mycopathologia · 2022Article
- Clinical effectiveness of efinaconazole 10% solution for treatment of onychomycosis with longitudinal spikes.The Journal of dermatology · 2021Article
- Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations.Molecules (Basel, Switzerland) · 2021Article
- A comparative study between two antifungal agents, Luliconazole and Efinaconazole, of their preventive effects in a Trichophyton-infected guinea pig onychomycosis model.Medical mycology · 2021Article
- Preparation andDrug delivery · 2019Article
- Ciclopirox and Efinaconazole Transungual Permeation, Antifungal Activity, and Proficiency To Induce Resistance in Trichophyton rubrum.Antimicrobial agents and chemotherapy · 2019Article
- Improved Methods for Assessing Therapeutic Potential of Antifungal Agents against Dermatophytes and Their Application in the Development of NP213, a Novel Onychomycosis Therapy Candidate.Antimicrobial agents and chemotherapy · 2019Article
- Polyurethanes as New Excipients in Nail Therapeutics.Pharmaceutics · 2018Article
- Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Onychomycosis is a common fungal nail disease that is difficult to treat topically due to the deep location of the infection under the densely keratinized nail plate. Keratin affinity of topical drugs is an important physicochemical property impacting therapeutic efficacy. To be effective, topical drugs must penetrate the nail bed and retain their antifungal activity within the nail matrix, both of which are adversely affected by keratin binding. We investigated these properties for efinaconazole, a new topical antifungal for onychomycosis, compared with those of the existing topical drugs ciclopirox and amorolfine. The efinaconazole free-drug concentration in keratin suspensions was 14.3%, significantly higher than the concentrations of ciclopirox and amorolfine, which were 0.7% and 1.9%, respectively (P < 0.001). Efinaconazole was released from keratin at a higher proportion than in the reference drugs, with about half of the remaining keratin-bound efinaconazole removed after washing. In single-dose in vitro studies, efinaconazole penetrated full-thickness human nails into the receptor phase and also inhibited the growth of Trichophyton rubrum under the nail. In the presence of keratin, efinaconazole exhibited fungicidal activity against Trichophyton mentagrophytes comparable to that of amorolfine and superior to that of ciclopirox. In a guinea pig onychomycosis model with T. mentagrophytes infection, an efinaconazole solution significantly decreased nail fungal burden compared to that of ciclopirox and amorolfine lacquers (P < 0.01). These results suggest that the high nail permeability of efinaconazole and its potent fungicidal activity in the presence of keratin are related to its low keratin affinity, which may contribute to its efficacy in onychomycosis.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.