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

Stem definition	Drug id	CAS RN
anti-inflammatory agents, ibufenac derivatives	1899	78281-72-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nepafenac nevanac	penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a nonsteroidal anti-inflammatory drug, amfenac is thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production Molecular weight: 254.29 Formula: C15H14N2O2 CLOGP: 1.38 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 86.18 ALOGS: -4.11 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nepafenac
nevanac

penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a nonsteroidal anti-inflammatory drug, amfenac is thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production

Molecular weight: 254.29
Formula: C15H14N2O2
CLOGP: 1.38
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 86.18
ALOGS: -4.11
ROTB: 4

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.17 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Aug. 19, 2005	FDA	ALCON PHARMS LTD

FDA Adverse Event Reporting System (Female)

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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
Ulcerative keratitis	121.43	34.13	24	1304	2686	63485008
Toxic anterior segment syndrome	112.35	34.13	21	1307	1750	63485944
Visual acuity reduced	100.57	34.13	31	1297	21795	63465899
Corneal epithelium defect	99.38	34.13	15	1313	337	63487357
Corneal opacity	95.10	34.13	16	1312	727	63486967
Product container issue	93.29	34.13	18	1310	1775	63485919
Product quality issue	93.02	34.13	33	1295	35832	63451862
Corneal oedema	90.23	34.13	17	1311	1476	63486218
Eye pain	83.42	34.13	30	1298	33824	63453870
Cataract	81.49	34.13	34	1294	57019	63430675

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FDA Adverse Event Reporting System (Male)

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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
Ulcerative keratitis	91.93	36.54	19	1113	1710	34954089
Corneal oedema	90.54	36.54	18	1114	1333	34954466
Toxic anterior segment syndrome	86.99	36.54	17	1115	1152	34954647
Intraocular pressure increased	61.16	36.54	17	1115	5366	34950433
Endophthalmitis	58.46	36.54	15	1117	3493	34952306
Visual impairment	53.19	36.54	25	1107	35777	34920022
Corneal opacity	52.74	36.54	10	1122	576	34955223
Ocular hyperaemia	52.39	36.54	18	1114	11434	34944365
Cystoid macular oedema	50.75	36.54	10	1122	705	34955094
Vision blurred	44.44	36.54	24	1108	45939	34909860

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FDA Adverse Event Reporting System (Geriatric)

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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
Ulcerative keratitis	172.02	32.85	34	1704	3655	79738995
Corneal oedema	158.24	32.85	30	1708	2590	79740060
Toxic anterior segment syndrome	156.64	32.85	30	1708	2734	79739916
Intraocular pressure increased	115.68	32.85	29	1709	9176	79733474
Endophthalmitis	110.15	32.85	26	1712	6402	79736248
Visual acuity reduced	109.95	32.85	36	1702	29433	79713217
Cataract	90.46	32.85	38	1700	62082	79680568
Corneal epithelium defect	81.20	32.85	14	1724	705	79741945
Corneal opacity	76.31	32.85	14	1724	1006	79741644
Cystoid macular oedema	67.05	32.85	14	1724	1966	79740684

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	S01BC10	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFLAMMATORY AGENTS Antiinflammatory agents, non-steroids
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:35493	anti-pyretic
CHEBI has role	CHEBI:50629	COX-2 inhibitor
CHEBI has role	CHEBI:50630	COX-1 inhibitor
CHEBI has role	CHEBI:50266	Prodrugs
FDA CS	M0001335	Anti-Inflammatory Agents, Non-Steroidal
FDA EPC	N0000175722	Nonsteroidal Anti-inflammatory Drug
FDA MoA	N0000000160	Cyclooxygenase Inhibitors
MeSH PA	D000700	Analgesics

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

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Disease	Relation	SNOMED_ID	DOID
Post-Op Ocular Inflammation	indication
Postoperative Ocular Pain	indication
Keratitis	contraindication	5888003	DOID:4677
Tear film insufficiency	contraindication	46152009
Corneal erosion	contraindication	50792001
Blood coagulation disorder	contraindication	64779008	DOID:1247
Rheumatoid arthritis	contraindication	69896004	DOID:7148
Diabetes mellitus	contraindication	73211009	DOID:9351
Perforation of cornea	contraindication	74895004
Corneal ulcer	contraindication	91514001	DOID:8463

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.34	acidic
pKa2	2.94	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.1%	NEVANAC	HARROW EYE	N021862	Aug. 19, 2005	RX	SUSPENSION/DROPS	OPHTHALMIC	7834059	Jan. 31, 2027	METHOD OF TREATING OCULAR INFLAMMATION

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN	INHIBITOR	IC50	6.82	WOMBAT-PK	KEGG DRUG
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN	INHIBITOR	IC50	6.60	WOMBAT-PK	KEGG DRUG
Cyclooxygenase	Enzyme		PGH1_BOVIN PGH2_BOVIN		IC50	6.70	CHEMBL
Cyclooxygenase	Enzyme		PGH2_RAT PGH1_RAT		IC50	7	CHEMBL

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External reference:

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ID	Source
010980	NDDF
0J9L7J6V8C	UNII
151075	PUBCHEM_CID
196661	MMSL
20485	MMSL
2136	PUBCHEM_CID
28O5C1J38A	UNII
298665	RXNORM
4024931	VUID
4024931	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ILEVRO	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0743	SUSPENSION/ DROPS	3 mg	OPHTHALMIC	NDA	22 sections
ILEVRO	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0743	SUSPENSION/ DROPS	3 mg	OPHTHALMIC	NDA	22 sections
ILEVRO	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0743	SUSPENSION/ DROPS	3 mg	OPHTHALMIC	NDA	22 sections
NEVANAC	HUMAN PRESCRIPTION DRUG LABEL	1	0065-0002	SUSPENSION/ DROPS	1 mg	OPHTHALMIC	NDA	23 sections
NEVANAC	HUMAN PRESCRIPTION DRUG LABEL	1	0065-0002	SUSPENSION/ DROPS	1 mg	OPHTHALMIC	NDA	23 sections
NEVANAC	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0778	SUSPENSION/ DROPS	1 mg	OPHTHALMIC	NDA	23 sections
NEVANAC	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0778	SUSPENSION/ DROPS	1 mg	OPHTHALMIC	NDA	23 sections
Nevanac	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6302	SUSPENSION	1 mg	OPHTHALMIC	NDA	22 sections

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