ebastine

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.61 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	4.961		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	1.496		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	0.286	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	14.894	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	0.140	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	0.330	%	High	1
herg	hERG pIC50	5.744	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	8.650	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	54.325	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	0.190	%	High	1
kinase-safety-class	ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,JAK2,JAK3,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK	55
kinase-selectivity-class	AXL,EPHB4,GRK2,PDK4	4
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	0.196		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	86.298		High	1
mppb	Mouse plasma protein binding (% unbound)	0.210		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	0.698		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	0.370	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	116.413	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	0.500	%	High	1
rppb	Rat plasma protein binding (% unbound)	0.160	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	0.385	uM	High	1

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
COVID-19	189.81	17.77	147	8856	168696	90450748
Urticaria	111.74	17.77	146	8857	312588	90306856
Angioedema	91.86	17.77	65	8938	64811	90554633
Endocrine ophthalmopathy	90.06	17.77	21	8982	1053	90618391
Toxic shock syndrome	74.94	17.77	18	8985	1026	90618418
Nasal ulcer	71.13	17.77	21	8982	2645	90616799
Gallbladder polyp	71.03	17.77	17	8986	954	90618490
Drug reaction with eosinophilia and systemic symptoms	67.93	17.77	46	8957	42712	90576732
Allergy test positive	64.82	17.77	15	8988	727	90618717
Eyelid disorder	61.61	17.77	18	8985	2185	90617259
Chronic spontaneous urticaria	55.92	17.77	16	8987	1804	90617640
Mean cell haemoglobin increased	55.34	17.77	19	8984	3886	90615558
Temperature intolerance	46.24	17.77	23	8980	12007	90607437
Swelling of eyelid	45.62	17.77	18	8985	5436	90614008
Systemic infection	40.78	17.77	16	8987	4759	90614685
Synovial cyst	38.01	17.77	20	8983	11732	90607712
Skin disorder	36.91	17.77	30	8973	36676	90582768
Pruritus	36.19	17.77	127	8876	541398	90078046
Mechanical urticaria	36.16	17.77	9	8994	595	90618849
Feeding disorder	35.59	17.77	22	8981	17490	90601954
Dyslipidaemia	34.97	17.77	18	8985	10089	90609355
Blood immunoglobulin E increased	34.90	17.77	14	8989	4411	90615033
Eczema	32.95	17.77	33	8970	52837	90566607
Vitamin D decreased	32.10	17.77	18	8985	11961	90607483
Eye infection	31.77	17.77	19	8984	14235	90605209
Urticarial vasculitis	31.27	17.77	9	8994	1036	90618408
Oesophagitis	30.88	17.77	20	8983	17229	90602215
Erythema	29.27	17.77	68	8935	229178	90390266
Arthrodesis	28.96	17.77	11	8992	3001	90616443
Pelvic pain	27.97	17.77	18	8985	15339	90604105
Death	27.30	17.77	6	8997	456545	90162899
Lymphangiectasia	27.29	17.77	5	8998	74	90619370
Oral herpes	26.75	17.77	24	8979	33500	90585944
Middle insomnia	26.54	17.77	18	8985	16733	90602711
Drug ineffective	25.65	17.77	63	8940	1384235	89235209
Neisseria infection	25.33	17.77	5	8998	112	90619332
Mixed liver injury	24.72	17.77	13	8990	7610	90611834
Acarodermatitis	24.64	17.77	8	8995	1378	90618066
Abdominal pain upper	23.90	17.77	80	8923	332594	90286850
Skin laceration	23.51	17.77	20	8983	26015	90593429
Tendinous contracture	23.41	17.77	5	8998	167	90619277
Intentional overdose	23.37	17.77	37	8966	93797	90525647
Hepatic enzyme increased	23.12	17.77	4	8999	360732	90258712
Hypervigilance	22.84	17.77	6	8997	492	90618952
Injection site oedema	22.75	17.77	8	8995	1755	90617689
Ear swelling	22.18	17.77	8	8995	1889	90617555
Antisocial behaviour	21.81	17.77	6	8997	586	90618858
Skin plaque	21.46	17.77	13	8990	9962	90609482
Rheumatoid arthritis	21.20	17.77	5	8998	362609	90256835
Axillary pain	20.61	17.77	8	8995	2313	90617131
Toxic skin eruption	20.46	17.77	15	8988	15759	90603685
Derealisation	20.17	17.77	7	8996	1478	90617966
Autoimmune myositis	19.84	17.77	5	8998	348	90619096
Tenosynovitis stenosans	19.58	17.77	9	8994	3944	90615500
Rash maculo-papular	19.23	17.77	22	8981	40911	90578533
Sprue-like enteropathy	18.99	17.77	6	8997	947	90618497
Cerebral haematoma	18.88	17.77	9	8994	4280	90615164
Face and mouth X-ray abnormal	18.42	17.77	3	9000	21	90619423
Rhinorrhoea	18.21	17.77	32	8971	88284	90531160

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
COVID-19	81.26	22.14	74	3802	115874	42501585
Dental caries	72.33	22.14	24	3852	4848	42612611
Vitamin D deficiency	50.21	22.14	21	3855	8052	42609407
Blood pressure fluctuation	47.74	22.14	30	3846	26878	42590581
Diabetes mellitus inadequate control	45.67	22.14	24	3852	15366	42602093
Drug reaction with eosinophilia and systemic symptoms	42.04	22.14	33	3843	42042	42575417
Blood pressure increased	30.87	22.14	42	3834	101886	42515573
Urticaria	29.53	22.14	35	3841	74001	42543458
Hepatitis	28.53	22.14	22	3854	27278	42590181
Hypocoagulable state	27.81	22.14	8	3868	1005	42616454
Measles	26.03	22.14	6	3870	313	42617146
Rheumatoid arthritis	25.63	22.14	25	3851	42415	42575044
Discoloured vomit	25.29	22.14	7	3869	765	42616694
Capillary permeability increased	25.04	22.14	4	3872	27	42617432
Poisoning deliberate	25.03	22.14	14	3862	10120	42607339
Pneumonia aspiration	23.91	22.14	26	3850	50052	42567407
Foetal macrosomia	23.63	22.14	5	3871	175	42617284
Toxic skin eruption	23.56	22.14	15	3861	13715	42603744
Skin wrinkling	23.56	22.14	6	3870	476	42616983
Pigmentation disorder	22.33	22.14	9	3867	3139	42614320

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
COVID-19	248.91	16.73	216	12813	244844	110331426
Urticaria	135.68	16.73	177	12852	318680	110257590
Drug reaction with eosinophilia and systemic symptoms	96.77	16.73	79	12950	82016	110494254
Angioedema	84.30	16.73	79	12950	98421	110477849
Endocrine ophthalmopathy	81.37	16.73	21	13008	1352	110574918
Nasal ulcer	68.21	16.73	21	13008	2566	110573704
Toxic shock syndrome	65.18	16.73	18	13011	1502	110574768
Allergy test positive	63.98	16.73	16	13013	907	110575363
Gallbladder polyp	58.70	16.73	16	13013	1271	110574999
Eyelid disorder	57.02	16.73	18	13011	2387	110573883
Dental caries	55.39	16.73	28	13001	12745	110563525
Pruritus	55.24	16.73	172	12857	581388	109994882
Chronic spontaneous urticaria	51.79	16.73	16	13013	1977	110574293
Eczema	50.67	16.73	52	12977	72241	110504029
Death	45.53	16.73	13	13016	698856	109877414
Mean cell haemoglobin increased	45.46	16.73	19	13010	5598	110570672
Swelling of eyelid	42.37	16.73	19	13010	6634	110569636
Temperature intolerance	39.35	16.73	23	13006	13927	110562343
Toxic skin eruption	37.81	16.73	29	13000	27486	110548784
Synovial cyst	35.32	16.73	20	13009	11410	110564860
Mechanical urticaria	34.95	16.73	9	13020	574	110575696
Blood immunoglobulin E increased	31.27	16.73	16	13013	7466	110568804
Skin disorder	30.30	16.73	31	12998	42882	110533388
Haematochezia	30.04	16.73	51	12978	115473	110460797
Vitamin D decreased	28.92	16.73	18	13011	12197	110564073
Vitamin D deficiency	28.71	16.73	21	13008	18531	110557739
Eye infection	28.47	16.73	19	13010	14499	110561771
Feeding disorder	28.23	16.73	22	13007	21340	110554930
Arthrodesis	28.23	16.73	11	13018	2707	110573563
Acarodermatitis	27.81	16.73	10	13019	1971	110574299
Blood immunoglobulin M decreased	27.52	16.73	10	13019	2031	110574239
Systemic infection	27.20	16.73	16	13013	9803	110566467
Middle insomnia	26.84	16.73	21	13008	20481	110555789
Urticarial vasculitis	25.98	16.73	8	13021	978	110575292
Diabetes mellitus inadequate control	25.68	16.73	24	13005	29751	110546519
Erythema	25.58	16.73	84	12945	291363	110284907
Oral herpes	25.36	16.73	26	13003	36054	110540216
Injection site oedema	24.69	16.73	9	13020	1845	110574425
Pelvic pain	24.57	16.73	18	13011	15924	110560346
Dyslipidaemia	24.55	16.73	18	13011	15947	110560323
Lymphangiectasia	24.53	16.73	5	13024	111	110576159
SARS-CoV-2 antibody test negative	22.98	16.73	6	13023	404	110575866
Abdominal pain upper	22.49	16.73	91	12938	349020	110227250
Product availability issue	22.23	16.73	13	13016	7877	110568393
Neisseria infection	21.45	16.73	5	13024	210	110576060
Blood pressure increased	21.36	16.73	73	12956	258300	110317970
Capillary permeability increased	20.63	16.73	4	13025	68	110576202
Hypervigilance	20.18	16.73	6	13023	651	110575619
Measles	20.06	16.73	6	13023	665	110575605
Ear swelling	19.93	16.73	8	13021	2128	110574142
Tendinous contracture	19.81	16.73	5	13024	294	110575976
Upper respiratory tract infection	19.63	16.73	46	12983	131282	110444988
Contraindicated product administered	19.44	16.73	3	13026	248264	110328006
Swelling face	19.20	16.73	37	12992	92284	110483986
Hepatic enzyme increased	19.04	16.73	7	13022	320885	110255385
Disease progression	19.00	16.73	3	13026	244031	110332239
Heart rate increased	18.96	16.73	48	12981	143786	110432484
Tenosynovitis stenosans	18.91	16.73	9	13020	3594	110572676
Skin plaque	18.86	16.73	14	13015	12631	110563639
Antisocial behaviour	18.54	16.73	6	13023	862	110575408
Weight decreased	18.51	16.73	106	12923	467951	110108319
Axillary pain	18.45	16.73	8	13021	2578	110573692
Hypocoagulable state	18.37	16.73	8	13021	2607	110573663
Intentional overdose	18.29	16.73	45	12984	132456	110443814
Hepatic cytolysis	18.01	16.73	27	13002	55026	110521244
Somnolence	17.94	16.73	76	12953	297373	110278897
Anaphylactic shock	17.90	16.73	26	13003	51520	110524750
Pigmentation disorder	17.88	16.73	11	13018	7300	110568970
Hepatitis	17.41	16.73	35	12994	90019	110486251
Oesophagitis	17.18	16.73	19	13010	28696	110547574
Vitamin B12 deficiency	16.98	16.73	12	13017	10043	110566227
Face and mouth X-ray abnormal	16.95	16.73	3	13026	30	110576240
Fractured sacrum	16.86	16.73	7	13022	2029	110574241
Blood pressure fluctuation	16.82	16.73	31	12998	74793	110501477
Poisoning deliberate	16.76	16.73	18	13011	26313	110549957

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ebastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

Source	Code	Description
ATC	R06AX22	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018494	Histamine Agents
CHEBI has role	CHEBI:53784	antispasmodic drug

Disease	Relation	SNOMED_ID	DOID
Allergic rhinitis	indication	61582004
Chronic idiopathic urticaria	indication	302162004

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	8	WOMBAT-PK	SCIENTIFIC LITERATURE
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.22	DRUG MATRIX
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		IC50	7.21	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.51	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.55	WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	5.82	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.19	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	6.34	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		IC50	7.33	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	7.59	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.70	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.91	DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.99	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.47	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	7.38	DRUG MATRIX
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.54	DRUG MATRIX
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		IC50	5.96	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.55	DRUG MATRIX
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	6.86	DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	7.40	DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	6.62	DRUG MATRIX
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		Ki	5.72	DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	7.11	DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.74	DRUG MATRIX
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	6.34	DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.06	DRUG MATRIX
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN		IC50	5.13	DRUG MATRIX
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		IC50	6.25	DRUG MATRIX
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		IC50	6.09	DRUG MATRIX
Receptor tyrosine-protein kinase erbB-2	Kinase	P04626	ERBB2_HUMAN		IC50	5.98	DRUG MATRIX
Substance-K receptor	GPCR	P21452	NK2R_HUMAN		Ki	6.19	DRUG MATRIX
5'-AMP-activated protein kinase catalytic subunit alpha-2	Kinase	P54646	AAPK2_HUMAN		Ki	7.58	CHEMBL
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	6.94	DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	6.63	DRUG MATRIX
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	5.85	DRUG MATRIX
Membrane-associated progesterone receptor component 1	Membrane receptor		PGRC1_RAT		Ki	5.87	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	5.58	CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		IC50	7.35	CHEMBL

ID	Source
D01478	KEGG_DRUG
C0058895	UMLSCUI
CHEBI:31528	CHEBI
CHEMBL305660	ChEMBL_ID
DB11742	DRUGBANK_ID
C058249	MESH_SUPPLEMENTAL_RECORD_UI
5633	INN_ID
TQD7Q784P1	UNII
3191	PUBCHEM_CID
23796	RXNORM
007136	NDDF
TQD7Q784P1	INXIGHT DRUGS