Efinaconazole

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Efinaconazole
Efinaconazole.svg
Clinical data
Trade names Jublia, Clenafin
AHFS/Drugs.com Monograph
MedlinePlus a614050
License data
Routes of
administration 		Topical
ATC code
Legal status
Legal status
Identifiers
  • (2R,3R)-2-(2,4-Difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.245.862 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C18H22F2N4O
Molar mass 348.398 g·mol−1
3D model (JSmol)
  • C[C@H]([C@](CN1C=NC=N1)(C2=C(C=C(C=C2)F)F)O)N3CCC(=C)CC3
  • InChI=1S/C18H22F2N4O/c1-13-5-7-23(8-6-13)14(2)18(25,10-24-12-21-11-22-24)16-4-3-15(19)9-17(16)20/h3-4,9,11-12,14,25H,1,5-8,10H2,2H3/t14-,18-/m1/s1
  • Key:NFEZZTICAUWDHU-RDTXWAMCSA-N

Efinaconazole, sold under the brand name Jublia and Clenafin among others, is a triazole antifungal compound discovered by Kaken Pharmaceutical, indicated for the treatment of onychomycosis, a fungal infection of the nail. Since it has low binding affinity with keratin, the main component of nails, it has superior nail-penetrating properties. It is approved for use in the United States, Canada, Japan and certain European countries as a 10% topical solution. [3] [4]

Contents

Efinaconazole acts as a 14α-demethylase inhibitor [5] [2] .

Medical uses

Efinaconazole is an azole antifungal indicated in the US for the topical treatment of onychomycosis of the toenails due to Trichophyton rubrum and Trichophyton mentagrophytes . [2] Unlike nail lacquers it does not require debridement.

Efficacy

The safety and efficacy of efinaconazole were established in two multi-centre randomised clinical trials with a total of 1,655 participants. 17.8% (trial 1) and 15.2% (trial 2) of participants using efinaconazole were completely cured (0% clinical involvement of the target toenail, plus negative KOH test and negative culture), compared with 3.3% (trial 1) and 5.5% (trial 2) of participants using a placebo. [2] The "complete cure or almost complete cure" rate (≤5% affected target toenail area involved, and negative KOH and culture) for efinaconazole was 26.4% (trial 1) and 23.4% (trial 2) (compared with 7.0% (trial 1) and 7.5% (trial 2)). [2]

In 2020, the FDA approved a supplemental New Drug Application for efinaconazole topical solution, 10%, which extended the age range included in the product's label to children six years of age and older. [6]

History

Efinaconazole was discovered by Japan dermatology company Kaken Pharmaceutical. In 2014, the U.S. Food and Drug Administration (FDA) approved the New Drug Application (NDA). [7] [8] According to Valeant Pharmaceuticals International Inc CEO J. Michael Pearson they acquired Jublia through their purchase of Dow Pharmaceutical Sciences in 2008. [8] Japan and Korean approvals followed. In 2024, Almirall announced completion of decentralized regulatory approval procedure for Jublia in Europe [9] .

Economics

In 2015, the cost of treatment with efinaconazole in the United States was said to be US$2,307 per nail. [10]

In 2019, a study by the Canadian Agency for Drugs and Technologies in Health found the cost for a 48-week course to be $178 for a big toe, and $89 for an other toe. [11]

A 2025 review of nine online Canadian pharmacies shows that the price for a four-week treatment is about $143 USD. Therefore a 48-week course of treatment is about 12 x $143 = $1716.[ citation needed ]

It is available as a generic medication in the USA. [12] [13] [14] [15]

References

  1. ↑ "Archived copy" (PDF). Archived (PDF) from the original on 10 June 2022. Retrieved 10 June 2022.{{cite web}}: CS1 maint: archived copy as title (link)
  2. 1 2 3 4 5 "Jublia- efinaconazole solution". DailyMed. 30 September 2016. Archived from the original on 30 November 2020. Retrieved 27 April 2020.
  3. ↑ Patel T, Dhillon S (November 2013). "Efinaconazole: first global approval". Drugs. 73 (17): 1977–1983. doi:10.1007/s40265-013-0152-x. PMID   24249649. S2CID   40015633.
  4. ↑ Tschen EH, Bucko AD, Oizumi N, Kawabata H, Olin JT, Pillai R (February 2013). "Efinaconazole solution in the treatment of toenail onychomycosis: a phase 2, multicenter, randomized, double-blind study". J Drugs Dermatol. 12 (2): 186–192. PMID   23377392.
  5. ↑ Tatsumi Y, Nagashima M, Shibanushi T, et al. (May 2013). "Mechanism of action of efinaconazole, a novel triazole antifungal agent". Antimicrob Agents Chemother. 57 (5): 2405–2509. doi:10.1128/aac.02063-12. PMC   3632939 . PMID   23459486.
  6. ↑ "FDA Approves Ortho Dermatologics' Labeling For Jublia (efinaconazole) Topical Solution, 10%, In Patients As Young As Six Years Old". Bausch Health (Press release). Archived from the original on 10 June 2022. Retrieved 10 June 2022.
  7. ↑ "Drug Approval Package: Jublia topical solution (efinaconazole) NDA #203567". U.S. Food and Drug Administration (FDA). 24 December 1999. Archived from the original on 29 May 2020. Retrieved 27 April 2020.
  8. 1 2 "Valeant Pharmaceuticals Announces FDA Approval Of Jublia for the Treatment of Onychomycosis". Valeant Pharmaceuticals (Press release). 9 June 2014. Archived from the original on 8 November 2015. Retrieved 1 November 2015.
  9. ↑ "Almirall announces completion of decentralized regulatory approval procedure for efinaconazole in Europe". Almirall newsroom. Retrieved 3 December 2025.
  10. ↑ Mikailov A, Cohen J, Joyce C, Mostaghimi A (2015). "Cost-effectiveness of Confirmatory Testing Before Treatment of Onychomycosis". JAMA Dermatology. 152 (3): 1–6. doi: 10.1001/jamadermatol.2015.4190 . PMID   26716567.
  11. ↑ "Table 5, CDR Cost Comparison Table for Onychomycosis". www.ncbi.nlm.nih.gov. 8 June 2019. Archived from the original on 10 June 2022. Retrieved 10 June 2022.
  12. ↑ "Efinaconazole: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 21 March 2021. Retrieved 14 February 2021.
  13. ↑ "Efinaconazole: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 21 March 2021. Retrieved 14 February 2021.
  14. ↑ "First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). Archived from the original on 26 January 2021. Retrieved 13 February 2021.
  15. ↑ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 3 March 2023. Archived from the original on 20 February 2020. Retrieved 6 March 2023.
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