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
Bronchopulmonary aspergillosis allergic 75.63 44.03 14 981 1177 50602952
Lung opacity 74.52 44.03 15 980 1958 50602171
Total lung capacity decreased 74.50 44.03 14 981 1277 50602852
Blood calcium increased 54.17 44.03 15 980 7704 50596425
Aspiration 51.46 44.03 15 980 9249 50594880
Bronchiectasis 49.91 44.03 15 980 10268 50593861
Euglycaemic diabetic ketoacidosis 47.31 44.03 11 984 2808 50601321
Rales 46.04 44.03 14 981 9964 50594165
Sputum discoloured 46.01 44.03 15 980 13380 50590749
Blood test abnormal 44.30 44.03 14 981 11305 50592824

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 60.26 37.28 10 322 794 29573401

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
Bronchopulmonary aspergillosis allergic 71.89 39.54 14 1201 1608 64495909
Total lung capacity decreased 71.06 39.54 14 1201 1708 64495809
Lung opacity 67.91 39.54 15 1200 3184 64494333
Blood calcium increased 53.28 39.54 15 1200 8527 64488990
Nail discolouration 49.09 39.54 11 1204 2489 64495028
Bronchiectasis 45.82 39.54 15 1200 14125 64483392
Dermatitis contact 43.65 39.54 13 1202 8987 64488530
Aspiration 43.21 39.54 15 1200 16870 64480647
Blood test abnormal 43.03 39.54 14 1201 12929 64484588
Sputum discoloured 42.39 39.54 15 1200 17841 64479676
Liver function test increased 41.02 39.54 17 1198 30953 64466564
Rales 40.79 39.54 14 1201 15215 64482302
Euglycaemic diabetic ketoacidosis 40.65 39.54 11 1204 5399 64492118

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
489181 PUBCHEM_CID
1539753 RXNORM
221737 MMSL
30345 MMSL
015550 NDDF
703880007 SNOMEDCT_US
703881006 SNOMEDCT_US
C3273754 UMLSCUI

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