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	153.14	40.16	30	1937	2153	63484902
Bronchopulmonary aspergillosis allergic	146.07	40.16	29	1938	2229	63484826
Lung opacity	142	40.16	30	1937	3138	63483917
Blood calcium increased	109.72	40.16	30	1937	9320	63477735
Aspiration	105.30	40.16	30	1937	10821	63476234
Rales	100.64	40.16	30	1937	12667	63474388
Sputum discoloured	97.29	40.16	31	1936	16316	63470739
Bronchiectasis	93.55	40.16	30	1937	16112	63470943
Blood test abnormal	90.38	40.16	29	1938	15600	63471455
Obstructive airways disorder	86.23	40.16	30	1937	20669	63466386
Haemoptysis	76.64	40.16	30	1937	28696	63458359
Liver function test increased	76.19	40.16	31	1936	32780	63454275
Transaminases increased	74.08	40.16	30	1937	31337	63455718
Pulmonary fibrosis	67.19	40.16	30	1937	39779	63447276
Hypoxia	55.60	40.16	30	1937	59762	63427293
Blood creatinine increased	47.34	40.16	31	1936	87813	63399242
Gastrooesophageal reflux disease	47.32	40.16	32	1935	95607	63391448
Upper respiratory tract infection	46.78	40.16	30	1937	82017	63405038
Euglycaemic diabetic ketoacidosis	44.05	40.16	12	1955	3662	63483393
Wheezing	42.61	40.16	30	1937	95565	63391490
Metabolic alkalosis	41.41	40.16	11	1956	3050	63484005

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	49.46	35.40	10	902	1001	34955018

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	176.44	37.03	36	2694	2869	79738789
Bronchopulmonary aspergillosis allergic	168.72	37.03	35	2695	3026	79738632
Lung opacity	155.73	37.03	36	2694	5138	79736520
Blood calcium increased	130.77	37.03	36	2694	10364	79731294
Sputum discoloured	108.51	37.03	37	2693	21706	79719952
Rales	107.56	37.03	36	2694	19965	79721693
Aspiration	107.28	37.03	36	2694	20122	79721536
Blood test abnormal	103.72	37.03	34	2696	17676	79723982
Bronchiectasis	103.58	37.03	36	2694	22350	79719308
Obstructive airways disorder	91.64	37.03	36	2694	31423	79710235
Liver function test increased	90.11	37.03	38	2692	39735	79701923
Pulmonary fibrosis	83.09	37.03	37	2693	44075	79697583
Transaminases increased	74.41	37.03	36	2694	51707	79689951
Haemoptysis	71.71	37.03	36	2694	55963	79685695
Upper respiratory tract infection	60.32	37.03	38	2692	91130	79650528
Gastrooesophageal reflux disease	55.67	37.03	38	2692	104208	79637450
Wheezing	51.81	37.03	38	2692	116626	79625032
Hypoxia	51.28	37.03	36	2694	103207	79638451
Lower respiratory tract infection	48.35	37.03	38	2692	129182	79612476
Asthma	42.68	37.03	36	2694	135059	79606599
Blood creatinine increased	42.30	37.03	38	2692	155019	79586639
Pulmonary mass	41.10	37.03	20	2710	29014	79712644
Nail discolouration	40.42	37.03	11	2719	3020	79738638
Pleural effusion	38.44	37.03	35	2695	145227	79596431

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	11654139	Oct. 2, 2034	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	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
DB09040	DRUGBANK_ID
1539753	RXNORM
221737	MMSL
30345	MMSL
015550	NDDF
703880007	SNOMEDCT_US
703881006	SNOMEDCT_US
C3273754	UMLSCUI
9349	INN_ID
489181	PUBCHEM_CID
J82SB7FXWB	UNII

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