All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
antihistaminics	1027	80012-43-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: alesion epinastine (+/-)-Epinastine epinastine hydrochloride epinastine HCl	direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell, indicated for the prevention of itching associated with allergic conjunctivitis Molecular weight: 249.32 Formula: C16H15N3 CLOGP: 2.15 LIPINSKI: 0 HAC: 3 HDO: 1 TPSA: 41.62 ALOGS: -3.18 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.15 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
Oct. 16, 2003	FDA	ALLERGAN
Sept. 20, 2019	PMDA	Santen Pharmaceutical Co., Ltd.

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
Treatment failure	158.74	26.54	80	1368	170312	56120307
Platelet count decreased	35.46	26.54	26	1422	106357	56184262
Hepatic function abnormal	34.15	26.54	17	1431	34541	56256078

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
Treatment failure	94.34	29.22	43	1408	40749	31655144
Hepatic function abnormal	69.48	29.22	35	1416	41187	31654706
Drug eruption	29.27	29.22	15	1436	18172	31677721

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
Hepatic function abnormal	91.00	23.44	47	2727	67949	70857721
Platelet count decreased	42.45	23.44	43	2731	178179	70747491
Drug eruption	40.74	23.44	23	2751	39473	70886197
Pyrexia	36.68	23.44	76	2698	606876	70318794
Interstitial lung disease	33.96	23.44	30	2744	104655	70821015
Decreased appetite	28.25	23.44	46	2728	304734	70620936
Alopecia areata	25.94	23.44	7	2767	1629	70924041
Neutrophil count decreased	25.22	23.44	23	2751	83533	70842137

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R06AX24	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
ATC	S01GX10	SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics
FDA MoA	N0000000122	Adrenergic Agonists
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
FDA EPC	N0000175519	Histamine-1 Receptor Inhibitor
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
FDA PE	N0000175628	Decreased Histamine Release
FDA EPC	N0000175883	Adrenergic Receptor Agonist
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:37956	antihistamines
CHEBI has role	CHEBI:50857	anti-allergic drugs
CHEBI has role	CHEBI:66981	ophthalmology drugs

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

Disease	Relation	SNOMED_ID	DOID
Allergic conjunctivitis	indication	473460002	DOID:11204
Ocular Itching	indication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.94	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	8.90		WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4		WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN					WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN					WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN					WOMBAT-PK
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN					WOMBAT-PK
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	5.37		CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	5.96		CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN					WOMBAT-PK
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	4.53		CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		IC50	8.80		CHEMBL

External reference:

ID	Source
4021466	VUID
N0000148850	NUI
D01713	KEGG_DRUG
108929-04-0	SECONDARY_CAS_RN
4021466	VANDF
C0078442	UMLSCUI
CHEBI:51032	CHEBI
CHEMBL1106	ChEMBL_ID
CHEMBL1200491	ChEMBL_ID
DB00751	DRUGBANK_ID
C053090	MESH_SUPPLEMENTAL_RECORD_UI
3241	PUBCHEM_CID
7176	IUPHAR_LIGAND_ID
5953	INN_ID
Q13WX941EF	UNII
236961	RXNORM
17645	MMSL
181234	MMSL
007311	NDDF
007312	NDDF
407068009	SNOMEDCT_US
407069001	SNOMEDCT_US
427671005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Epinastine	HUMAN PRESCRIPTION DRUG LABEL	1	17478-911	SOLUTION/ DROPS	0.50 mg	OPHTHALMIC	ANDA	22 sections
Epinastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51991-836	SOLUTION/ DROPS	0.50 mg	OPHTHALMIC	ANDA	26 sections
EPINASTINE HYDROCHLORIDE	Human Prescription Drug Label	1	62756-329	SOLUTION	0.50 mg	OPHTHALMIC	ANDA	22 sections
EPINASTINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	70069-008	SOLUTION/ DROPS	0.50 mg	OPHTHALMIC	ANDA	20 sections