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

Stem definition	Drug id	CAS RN
systemic antifungal agents, miconazole derivatives	4874	164650-44-6

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company	Orphan
June 6, 2014	FDA	DOW PHARM
July 4, 2014	PMDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	13.3	acidic
pKa2	7.37	Basic
pKa3	1.38	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10%	JUBLIA	BAUSCH	N203567	June 6, 2014	RX	SOLUTION	TOPICAL	April 27, 2023	NEW PATIENT POPULATION

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Lanosterol 14-alpha demethylase	Enzyme		F2SHH3_TRIRC	INHIBITOR				CHEMBL	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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