Skip to main content
SpringerLink
Log in

Efinaconazole in Onychomycosis

  • Review Article
  • Published:
American Journal of Clinical Dermatology Aims and scope Submit manuscript

Abstract

Onychomycosis is a fungal nail infection that causes nail discoloration, nail plate thickening, and onycholysis. Efinaconazole 10% topical solution is an FDA-approved treatment for onychomycosis patients aged 6 years and above. The drug functions as an antifungal by disrupting ergosterol synthesis in the fungal cell membrane. It exhibits higher in vitro activity against dermatophytes than other available antifungals such as ciclopirox and itraconazole, and the activity is comparable to amorolfine and terbinafine. Efinaconazole also provides enhanced nail penetration compared with other topical antifungals due to low surface tension, poor water solubility, and low keratin affinity. The pharmacokinetic studies suggest that the efinaconazole topical delivery to the nail bed is not markedly affected by the presence of disease. There is a subset of onychomycosis patients who are more likely to respond to efinaconazole 10% solution: female patients, those with lower BMI, mild onychomycosis, a short disease duration, no infected non-target toenails (large toenail disease only), and when concomitant tinea pedis is treated. Experts recommend efinaconazole 10% topical solution as the first line for mild-to-moderate onychomycosis, pediatric onychomycosis, those with liver or kidney disease, and as maintenance therapy to prevent relapse. The side effects of topical efinaconazole are minimal: most commonly ingrown toenails, dermatitis, vesicles, and pain at the application site. Altogether, phase I and phase III clinical trials, and post-hoc analyses indicate that efinaconazole 10% topical solution is a safe and effective treatment for adult and pediatric onychomycosis, with a satisfactory mycological and clinical cure.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6

Similar content being viewed by others

References

  1. Vlahovic TC, Gupta AK. Efinaconazole topical solution (10%) for the treatment of onychomycosis in adult and pediatric patients. Expert Rev Anti Infect Ther. 2021;30:1–13.

    Google Scholar 

  2. Westerberg DP, Voyack MJ. Onychomycosis: current trends in diagnosis and treatment. Am Fam Physician. 2013;88(11):762–70.

    PubMed  Google Scholar 

  3. Penlac® Nail Lacquer (ciclopirox) Topical Solution, 8%. 2004. https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21022s004lbl.pdf. Accessed 06 Aug 2021.

  4. Penlac® (ciclopirox topical 8% w/w solution) product monograph. 2021. https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21022s004lbl.pdf. Accessed 16 Sep 2021.

  5. Bohn M, Kraemer KT. Dermatopharmacology of ciclopirox nail lacquer topical solution 8% in the treatment of onychomycosis. J Am Acad Dermatol. 2000;43(4):S57–69.

    Article  CAS  Google Scholar 

  6. Eichenfield LF, Elewski B, Sugarman JL, Rosen T, Vlahovic TC, Gupta AK, et al. Efinaconazole 10% topical solution for the treatment of onychomycosis in pediatric patients: open-label phase 4 study. J Am Acad Dermatol. 2021;84(4):1140–2.

    Article  CAS  Google Scholar 

  7. Elewski BE, Aly R, Baldwin SL, Soto RFG, Rich P, Weisfeld M, et al. Efficacy and safety of tavaborole topical solution, 5%, a novel boron-based antifungal agent, for the treatment of toenail onychomycosis: results from 2 randomized phase-III studies. J Am Acad Dermatol. 2015;73(1):62–9.

    Article  CAS  Google Scholar 

  8. Elewski BE, Pollak RA, Pillai R, Olin JT. Access of efinaconazole topical solution, 10%, to the infection site by spreading through the subungual space. J Drugs Dermatol. 2014;13(11):1394–8.

    CAS  PubMed  Google Scholar 

  9. Elewski BE, Rich P, Pollak R, Pariser DM, Watanabe S, Senda H, et al. Efinaconazole 10% solution in the treatment of toenail onychomycosis: two phase III multicenter, randomized, double-blind studies. J Am Acad Dermatol. 2013;68(4):600–8.

    Article  CAS  Google Scholar 

  10. Gupta AK, Elewski BE, Sugarman JL, Ieda C, Kawabata H, Kang R, et al. The efficacy and safety of efinaconazole 10% solution for treatment of mild to moderate onychomycosis: a pooled analysis of two phase 3 randomized trials. J Drugs Dermatol. 2014;13(7):815–20.

    CAS  PubMed  Google Scholar 

  11. Gupta AK, Fleckman P, Baran R. Ciclopirox nail lacquer topical solution 8% in the treatment of toenail onychomycosis. J Am Acad Dermatol. 2000;43(4):S70–80.

    Article  CAS  Google Scholar 

  12. Haria M, Bryson HM. Amorolfine. A review of its pharmacological properties and therapeutic potential in the treatment of onychomycosis and other superficial fungal infections. Drugs. 1995;49(1):103–20.

    Article  CAS  Google Scholar 

  13. Hold K, Bullington R, Jones T, Beutner K. In vivo nail residence time of AN2690, a novel broad-spectrum antifungal agent in development for the topical treatment of onychomycosis: P1816. J Am Acad Dermatol. 2007;56(2).

  14. Lauharanta J. Comparative efficacy and safety of amorolfine nail lacquer 2% versus 5% once weekly. Clin Exp Dermatol. 1992;17:41–3.

    Article  Google Scholar 

  15. Monti D, Herranz U, Dal Bo L, Subissi A. Nail penetration and predicted mycological efficacy of an innovative hydrosoluble ciclopirox nail lacquer vs. a standard amorolfine lacquer in healthy subjects. J Eur Acad Dermatol Venereol. 2013;27(2):e153–8.

    Article  CAS  Google Scholar 

  16. Sakamoto M, Sugimoto N, Kawabata H, Yamakawa E, Kodera N, Pillai R, et al. Transungual delivery of efinaconazole: its deposition in the nail of onychomycosis patients and in vitro fungicidal activity in human nails. J Drugs Dermatol. 2014;13(11):1388–92.

    CAS  PubMed  Google Scholar 

  17. Sugiura K, Sugimoto N, Hosaka S, Katafuchi-Nagashima M, Arakawa Y, Tatsumi Y, et al. The low keratin affinity of efinaconazole contributes to its nail penetration and fungicidal activity in topical onychomycosis treatment. Antimicrob Agents Chemother. 2014;58(7):3837–42.

    Article  Google Scholar 

  18. Gasser J, Pagani E, Vittadello F, Nobile C, Zampieri P, Eisendle K. Frequency, type and treatment of fungal pathogens in toenail onychomycosis in the central Alpine region of South Tyrol, northern Italy—a 10-year retrospective study from 2004 to 2013. Mycoses. 2016;59(12):760–4.

    Article  Google Scholar 

  19. Product monograph of JUBLIA® (efinaconazole), topical solution, 10% w/w (Bausch Health, Canada Inc.). 2020. https://pdf.hres.ca/dpd_pm/00054721.PDF. Accessed 01 Sep 2021.

  20. Highlights of prescribing information, JUBLIA® (efinaconazole) topical solution (FDA label). 2020. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/203567s009lbl.pdf. Accessed 01 Sep 2021.

  21. Jo Siu WJ, Tatsumi Y, Senda H, Pillai R, Nakamura T, Sone D, et al. Comparison of in vitro antifungal activities of efinaconazole and currently available antifungal agents against a variety of pathogenic fungi associated with onychomycosis. Antimicrob Agents Chemother. 2013;57(4):1610–6.

    Article  Google Scholar 

  22. Tupaki-Sreepurna A, Jishnu BT, Thanneru V, Sharma S, Gopi A, Sundaram M, et al. An assessment of in vitro antifungal activities of efinaconazole and itraconazole against common non-dermatophyte fungi causing onychomycosis. J Fungi (Basel). 2017;3(2):20.

    Article  Google Scholar 

  23. Nachrichtendienst V. Almirall and Kaken Pharmaceutical enter into a license and distribution agreement for European rights to the topical formulation of efinaconazole. 2021. https://www.prnewswire.com/de/pressemitteilungen/almirall-and-kaken-pharmaceutical-enter-into-a-license-and-distribution-agreement-for-european-rights-to-the-topical-formulation-of-efinaconazole-850637563.html. Accessed 22 Sep 2021.

  24. Kircik LH. Enhancing transungual delivery and spreading of efinaconazole under the nail plate through a unique formulation approach. J Drugs Dermatol. 2014;13(12):1457–61.

    CAS  PubMed  Google Scholar 

  25. Gupta AK, Pillai R. The presence of an air gap between the nail plate and nail bed in onychomycosis patients: treatment implications for topical therapy. J Drugs Dermatol. 2015;14(8):859–63.

    PubMed  Google Scholar 

  26. Del Rosso JQ, Reece B, Smith K, Miller T. Efinaconazole 10% solution: a new topical treatment for onychomycosis: contact sensitization and skin irritation potential. J Clin Aesthet Dermatol. 2013;6(3):20.

    PubMed  PubMed Central  Google Scholar 

  27. Iozumi K, Abe M, Ito Y, Uesugi T, Onoduka T, Kato I, et al. Efficacy of long-term treatment with efinaconazole 10% solution in patients with onychomycosis, including severe cases: a multicenter, single-arm study. J Dermatol. 2019;46(8):641–51.

    Article  CAS  Google Scholar 

  28. Gupta AK, Cooper EA. Long-term efficacy and safety of once-daily Efinaconazole 10% topical solution (Jublia) for dermatophyte toenail onychomycosis: an interim analysis. Skin Ther Lett. 2021;26(1):5–10.

    Google Scholar 

  29. Rich P. Efinaconazole topical solution, 10%: the benefits of treating onychomycosis early. J Drugs Dermatol. 2015.

  30. Rosen T. Evaluation of gender as a clinically relevant outcome variable in the treatment of onychomycosis with efinaconazole topical solution 10%. Cutis. 2015;96(3):197–201.

    PubMed  Google Scholar 

  31. Gupta AK, Venkataraman M, Anbalagan N, Guenin EP. One size does not fit all: the need for individualized treatment based on factors that may affect the therapeutic outcome of efinaconazole 10% solution for the treatment of toenail onychomycosis. Int J Dermatol. 2021;60:1296–302.

    Article  CAS  Google Scholar 

  32. Vlahovic TC, Joseph WS. Efinaconazole topical, 10% for the treatment of toenail onychomycosis in patients with diabetes. J Drugs Dermatol. 2014;13(10):1186–90.

    CAS  PubMed  Google Scholar 

  33. Elewski BE, Tosti A. Risk factors and comorbidities for onychomycosis: implications for treatment with topical therapy. J Clin Aesthet Dermatol. 2015;8(11):38.

    PubMed  PubMed Central  Google Scholar 

  34. Rodriguez DA. Efinaconazole topical solution, 10%, for the treatment of mild and moderate toenail onychomycosis. J Clin Aesthet Dermatol. 2015;8(6):24.

    PubMed  PubMed Central  Google Scholar 

  35. Gupta AK, Korotzer A. Topical treatment of onychomycosis and clinically meaningful outcomes. J Drugs Dermatol. 2016;15(10):1260–6.

    PubMed  Google Scholar 

  36. Del Rosso JQ. Onychomycosis of toenails and post-hoc analyses with Efinaconazole 10% solution once-daily treatment: impact of disease severity and other concomitant associated factors on selection of therapy and therapeutic outcomes. J Clin Aesthet Dermatol. 2016;9(2):42–7.

    PubMed  PubMed Central  Google Scholar 

  37. Tosti A, Elewski BE. Treatment of onychomycosis with efinaconazole 10% topical solution and quality of life. J Clin Aesthet Dermatol. 2014;7(11):25.

    PubMed  PubMed Central  Google Scholar 

  38. Gupta AK, Venkataraman M, Quinlan EM, Gupta MA, Anbalagan N, Lyons R. More than nail deep: the effect of efinaconazole 10% treatment on the quality of life in patients with onychomycosis: a post hoc study. Skin Appendage Disord. 2021;7(4):272–9.

    Article  Google Scholar 

  39. Foley K, Gupta AK, Versteeg S, Mays R, Villanueva E, John D. Topical and device‐based treatments for fungal infections of the toenails. Cochrane Database Syst Rev. 2020;(1).

  40. Totri CR, Feldstein S, Admani S, Friedlander SF, Eichenfield LF. Epidemiologic analysis of onychomycosis in the San Diego pediatric population. Pediatr Dermatol. 2017;34(1):46–9.

    Article  Google Scholar 

  41. Gupta AK, Venkataraman M, Shear NH, Piguet V. Onychomycosis in children—review on treatment and management strategies. J Dermatolog Treat. 2020;26:1–12.

    Article  Google Scholar 

  42. Lipner SR, Joseph WS, Vlahovic TC, Scher RK, Rich P, Ghannoum M, et al. Therapeutic recommendations for the treatment of toenail onychomycosis in the US. J Drugs Dermatol. 2021;20(10):1076–84.

    PubMed  Google Scholar 

  43. Watanabe S, Iozumi K, Abe M, Ito Y, Uesugi T, Onoduka T, et al. Clinical effectiveness of efinaconazole 10% solution for treatment of onychomycosis with longitudinal spikes. J Dermatol. 2021;48(10):1474–81.

    Article  CAS  Google Scholar 

  44. FDA Adverse Event Reporting System (FAERS) Public Dashboard. 2020. https://www.fda.gov/drugs/questions-and-answers-fdas-adverse-event-reporting-system-faers/fda-adverse-event-reporting-system-faers-public-dashboard. Accessed 17 Dec 2020.

  45. Gupta AK, Cernea M. How effective is efinaconazole in the management of onychomycosis? Expert Opin Pharmacother. 2016;17(4):611–8.

    Article  Google Scholar 

  46. Glynn M, Jo W, Minowa K, Sanada H, Nejishima H, Matsuuchi H, et al. Efinaconazole: developmental and reproductive toxicity potential of a novel antifungal azole. Reprod Toxicol. 2015;52:18–25.

    Article  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Mediprobe Research Inc., 645 Windermere Road, London, ON, N5X 2P1, Canada

    Aditya K. Gupta & Mesbah Talukder

  2. Division of Dermatology, Department of Medicine, University of Toronto, Toronto, ON, Canada

    Aditya K. Gupta

Authors
  1. Aditya K. Gupta
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Mesbah Talukder
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Aditya K. Gupta.

Ethics declarations

Funding

None.

Competing Interests

AKG has conducted clinical trials and been a speaker for Bausch Health in Canada; he is a consultant for Ortho Diagnostics (USA). MT has no conflict of interest to declare.

Ethics approval

The authors declare that human ethics approval was not required for this article.

Consent to participate

Not applicable.

Consent for publication

Not applicable.

Availability of data and material

Not applicable.

Code availability

Not applicable.

Author’s contributions

Conception of the manuscript was done by AKG. The work was drafted by MT and substantively revised by AKG and MT.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Gupta, A.K., Talukder, M. Efinaconazole in Onychomycosis. Am J Clin Dermatol 23, 207–218 (2022). https://doi.org/10.1007/s40257-021-00660-1

Download citation

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40257-021-00660-1

Search

Navigation