Efinaconazole in Onychomycosis.
Journal
American journal of clinical dermatology
ISSN: 1179-1888
Titre abrégé: Am J Clin Dermatol
Pays: New Zealand
ID NLM: 100895290
Informations de publication
Date de publication:
Mar 2022
Mar 2022
Historique:
accepted:
14
11
2021
pubmed:
14
12
2021
medline:
15
3
2022
entrez:
13
12
2021
Statut:
ppublish
Résumé
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.
Identifiants
pubmed: 34902110
doi: 10.1007/s40257-021-00660-1
pii: 10.1007/s40257-021-00660-1
doi:
Substances chimiques
Antifungal Agents
0
Triazoles
0
efinaconazole
J82SB7FXWB
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
207-218Informations de copyright
© 2021. The Author(s), under exclusive licence to Springer Nature Switzerland AG.
Références
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.
Westerberg DP, Voyack MJ. Onychomycosis: current trends in diagnosis and treatment. Am Fam Physician. 2013;88(11):762–70.
pubmed: 24364524
Penlac
Penlac
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.
doi: 10.1067/mjd.2000.109072
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.
doi: 10.1016/j.jaad.2020.06.1004
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.
doi: 10.1016/j.jaad.2015.04.010
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.
pubmed: 25607708
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.
doi: 10.1016/j.jaad.2012.10.013
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.
pubmed: 25007364
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.
doi: 10.1067/mjd.2000.109071
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.
doi: 10.2165/00003495-199549010-00008
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).
Lauharanta J. Comparative efficacy and safety of amorolfine nail lacquer 2% versus 5% once weekly. Clin Exp Dermatol. 1992;17:41–3.
doi: 10.1111/j.1365-2230.1992.tb00277.x
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.
doi: 10.1111/j.1468-3083.2012.04529.x
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.
pubmed: 25607707
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.
doi: 10.1128/AAC.00111-14
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.
doi: 10.1111/myc.12528
Product monograph of JUBLIA
Highlights of prescribing information, JUBLIA
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.
doi: 10.1128/AAC.02056-12
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.
doi: 10.3390/jof3020020
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.
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.
pubmed: 25607788
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: 26267730
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: 24307921
pmcid: 3848648
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.
doi: 10.1111/1346-8138.14935
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.
Rich P. Efinaconazole topical solution, 10%: the benefits of treating onychomycosis early. J Drugs Dermatol. 2015.
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: 26562270
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.
doi: 10.1111/ijd.15739
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.
pubmed: 25607552
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: 26705439
pmcid: 4689496
Rodriguez DA. Efinaconazole topical solution, 10%, for the treatment of mild and moderate toenail onychomycosis. J Clin Aesthet Dermatol. 2015;8(6):24.
pubmed: 26155324
pmcid: 4479366
Gupta AK, Korotzer A. Topical treatment of onychomycosis and clinically meaningful outcomes. J Drugs Dermatol. 2016;15(10):1260–6.
pubmed: 27741345
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: 27354888
pmcid: 4896821
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: 25489379
pmcid: 4255695
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.
doi: 10.1159/000514361
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).
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.
doi: 10.1111/pde.12986
Gupta AK, Venkataraman M, Shear NH, Piguet V. Onychomycosis in children—review on treatment and management strategies. J Dermatolog Treat. 2020;26:1–12.
doi: 10.1080/09546634.2020.1810607
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: 34636509
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.
doi: 10.1111/1346-8138.16035
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.
Gupta AK, Cernea M. How effective is efinaconazole in the management of onychomycosis? Expert Opin Pharmacother. 2016;17(4):611–8.
doi: 10.1517/14656566.2016.1146687
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.
doi: 10.1016/j.reprotox.2014.12.007