Efinaconazole

Efinaconazole, sold under the brand name Jublia among others, is a triazole antifungal medication. It is approved for use in the United States, Canada, and Japan as a 10% topical solution for the treatment of onychomycosis (fungal infection of the nail).^[3][4] Efinaconazole acts as a 14α-demethylase inhibitor.^[5][2]

Efinaconazole

Clinical data
Trade names	Jublia, Clenafin
AHFS/Drugs.com	Monograph
MedlinePlus	a614050
License data	US DailyMed: Efinaconazole US FDA: Efinaconazole
Routes of administration	Topical
ATC code	D01AC19 (WHO)
Legal status
Legal status	CA: ℞-only[1] US: ℞-only[2]
Identifiers
IUPAC name (2R,3R)-2-(2,4-Difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol
CAS Number	164650-44-6
PubChem CID	489181
DrugBank	DB09040
ChemSpider	428538
UNII	J82SB7FXWB
KEGG	D10021
ChEBI	CHEBI:82718
ChEMBL	ChEMBL2103877
CompTox Dashboard (EPA)	DTXSID40167787
ECHA InfoCard	100.245.862
Chemical and physical data
Formula	C18H22F2N4O
Molar mass	348.398 g·mol−1
3D model (JSmol)	Interactive image
SMILES C[C@H]([C@](CN1C=NC=N1)(C2=C(C=C(C=C2)F)F)O)N3CCC(=C)CC3
InChI 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

It is available as a generic medication.^[6][7][8][9]

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]

Efficacy

In two clinical trials 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]

History

In 2014, the U.S. Food and Drug Administration (FDA) approved the New Drug Application (NDA).^[10][11] According to Valeant Pharmaceuticals International Inc CEO J. Michael Pearson they acquired Jublia through their purchase of Dow Pharmaceutical Sciences in 2008.^[11]

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; it was first approved in 2014, in people aged 18 years of age and older.^[12]

Society and culture

Economics

In 2015, the cost of treatment with efinaconazole in the United States was said to be US$2,307 per nail.^[13]

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.^[14]