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
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 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	60.26	37.28	10	322	794	29573401

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
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:

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

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