efinaconazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
systemic antifungal agents, miconazole derivatives 4874 164650-44-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • efinaconazole
  • jublia
  • KP-103
Efinaconazole is an azole antifungal. Efinaconazole inhibits fungal lanosterol 14α-demethylase involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes.
  • Molecular weight: 348.40
  • Formula: C18H22F2N4O
  • CLOGP: 2.42
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 54.18
  • ALOGS: -2.76
  • ROTB: 5

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 6, 2014 FDA DOW PHARM
July 4, 2014 PMDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Total lung capacity decreased 90.82 41.14 17 1125 1472 56289453
Bronchopulmonary aspergillosis allergic 84.97 41.14 16 1126 1430 56289495
Lung opacity 83.14 41.14 17 1125 2324 56288601
Blood calcium increased 62.04 41.14 17 1125 8137 56282788
Aspiration 59.26 41.14 17 1125 9604 56281321
Rales 57.26 41.14 17 1125 10823 56280102
Sputum discoloured 56.74 41.14 18 1124 14274 56276651
Bronchiectasis 56.36 41.14 17 1125 11417 56279508
Blood test abnormal 50.32 41.14 16 1126 12768 56278157
Obstructive airways disorder 49.46 41.14 17 1125 17265 56273660
Euglycaemic diabetic ketoacidosis 45.61 41.14 11 1131 3178 56287747
Liver function test increased 44.83 41.14 18 1124 28115 56262810
Nail discolouration 42.95 41.14 10 1132 2486 56288439
Haemoptysis 42.34 41.14 17 1125 26543 56264382
Metabolic alkalosis 41.63 41.14 10 1132 2841 56288084

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Nail discolouration 59.44 36.43 10 347 859 31696128

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Total lung capacity decreased 86.89 39.06 17 1353 1952 70925122
Bronchopulmonary aspergillosis allergic 80.80 39.06 16 1354 1953 70925121
Lung opacity 76.14 39.06 17 1353 3696 70923378
Blood calcium increased 61.20 39.06 17 1353 8976 70918098
Sputum discoloured 52.69 39.06 18 1352 18833 70908241
Bronchiectasis 51.44 39.06 17 1353 16080 70910994
Rales 50.40 39.06 17 1353 17118 70909956
Aspiration 49.88 39.06 17 1353 17658 70909416
Blood test abnormal 49.00 39.06 16 1354 14574 70912500
Nail discolouration 47.94 39.06 11 1359 2695 70924379
Liver function test increased 45.80 39.06 19 1351 33828 70893246
Obstructive airways disorder 43.40 39.06 17 1353 26096 70900978
Dermatitis contact 42.30 39.06 13 1357 9736 70917338
Euglycaemic diabetic ketoacidosis 39.23 39.06 11 1359 5996 70921078

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC D01AC19 DERMATOLOGICALS
ANTIFUNGALS FOR DERMATOLOGICAL USE
ANTIFUNGALS FOR TOPICAL USE
Imidazole and triazole derivatives
FDA CS M0002083 Azoles
FDA EPC N0000175487 Azole Antifungal
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000935 Antifungal Agents
CHEBI has role CHEBI:77884 sterol 14alpha-demethylase inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Onychomycosis due to Trichophyton mentagrophytes indication 23549005
Onychomycosis due to dermatophyte indication 402134005
Onychomycosis of toenails indication 403059006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.3 acidic
pKa2 7.37 Basic
pKa3 1.38 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 7214506 Feb. 22, 2026 ANTIMYCOTIC USES, SPECIFICALLY TREATMENT OF ONYCHOMYCOSIS
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 10512640 Jan. 3, 2028 TOPICAL TREATMENT OF ONYCHOMYCOSIS OF THE TOENAIL(S) DUE TO TRICHOPHYTON RUBRUM AND TRICHOPHYTON MENTAGROPHYTES
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 11213519 Jan. 3, 2028 ANTIMYCOTIC USES, SPECIFICALLY TREATMENT OF ONYCHOMYCOSIS; TOPICAL TREATMENT OF THE TOENAIL(S) DUE TO TRICHOPHYTON RUBRUM AND TRICHOPHYTON MENTAGROPHYTES
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 9566272 Jan. 3, 2028 TOPICAL TREATMENT OF ONYCHOMYCOSIS OF THE TOENAIL(S) DUE TO TRICHOPHYTON RUBRUM AND TRICHOPHYTON MENTAGROPHYTES
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 9877955 Jan. 3, 2028 TOPICAL TREATMENT OF ONYCHOMYCOSIS OF THE TOENAIL(S) DUE TO TRICHOPHYTON RUBRUM AND TRICHOPHYTON MENTAGROPHYTES
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 8039494 July 8, 2030 ANTIMYCOTIC USES, SPECIFICALLY TREATMENT OF ONYCHOMYCOSIS
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 10342875 Oct. 2, 2034 ANTIMYCOTIC USES, SPECIFICALLY TREATMENT OF ONYCHOMYCOSIS; TOPICAL TREATMENT OF THE TOENAIL(S) DUE TO TRICHOPHYTON RUBRUM AND TRICHOPHYTON MENTAGROPHYTES
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 10828293 Oct. 2, 2034 ANTIMYCOTIC USES, SPECIFICALLY TREATMENT OF ONYCHOMYCOSIS; TOPICAL TREATMENT OF THE TOENAIL(S) DUE TO TRICHOPHYTON RUBRUM AND TRICHOPHYTON MENTAGROPHYTES
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 10864274 Oct. 2, 2034 ANTIMYCOTIC USES, SPECIFICALLY TREATMENT OF ONYCHOMYCOSIS; TOPICAL TREATMENT OF THE TOENAIL(S) DUE TO TRICHOPHYTON RUBRUM AND TRICHOPHYTON MENTAGROPHYTES
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL 10478601 April 25, 2035 TOPICAL TREATMENT OF TINEA UNGUIUM BY USING AN APPLICATOR FOR APPLYING A SOLUTION FOR TREATING TINEA UNGUIUM TO AN AFFECTED PART OF A PATIENT

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10% JUBLIA BAUSCH N203567 June 6, 2014 RX SOLUTION TOPICAL April 27, 2023 NEW PATIENT POPULATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Lanosterol 14-alpha demethylase Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
D10021 KEGG_DRUG
4033415 VUID
N0000190763 NUI
4033415 VANDF
CHEBI:82718 CHEBI
CHEMBL2103877 ChEMBL_ID
C431707 MESH_SUPPLEMENTAL_RECORD_UI
9349 INN_ID
DB09040 DRUGBANK_ID
J82SB7FXWB UNII
1539753 RXNORM
221737 MMSL
30345 MMSL
015550 NDDF
703880007 SNOMEDCT_US
703881006 SNOMEDCT_US
C3273754 UMLSCUI
489181 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
JUBLIA HUMAN PRESCRIPTION DRUG LABEL 1 0187-5400 SOLUTION 100 mg TOPICAL NDA 26 sections
JUBLIA HUMAN PRESCRIPTION DRUG LABEL 1 0187-5400 SOLUTION 100 mg TOPICAL NDA 26 sections
JUBLIA HUMAN PRESCRIPTION DRUG LABEL 1 0187-5400 SOLUTION 100 mg TOPICAL NDA 26 sections