EBASTINE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C32H39NO2
Molecular Weight	469.6576
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4

InChI

InChIKey=MJJALKDDGIKVBE-UHFFFAOYSA-N

InChI=1S/C32H39NO2/c1-32(2,3)28-18-16-25(17-19-28)30(34)15-10-22-33-23-20-29(21-24-33)35-31(26-11-6-4-7-12-26)27-13-8-5-9-14-27/h4-9,11-14,16-19,29,31H,10,15,20-24H2,1-3H3

HIDE SMILES / InChI

Molecular Formula	C32H39NO2
Molecular Weight	469.6576
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/19032340

Ebastine is an antihistamine which blocks H1-receptors through its carboxylic acid metabolite. Ebastine is indicated for the treatment of allergic rhinitis and chronic idiopathic urticaria.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H1 receptor 316 Target ID: P35367 Gene ID: 3269.0 Gene Symbol: HRH1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/19032340	Antagonist 2849

Conditions

Condition	Modality	Targets	Highest Phase	Product
Allergic rhinitis 104 Sources: http://www.ncbi.nlm.nih.gov/pubmed/19032340	Primary		Approved 8583	EBATROL Approved Use Unknown
Chronic idiopathic urticaria 11 Sources: http://www.ncbi.nlm.nih.gov/pubmed/19032340	Primary		Approved 8583	EBATROL Approved Use Unknown

C_max

Value	Dose	Analyte	Population
53.4 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400093_4490019F1028_1_023_1F.pdf#page=26	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	CAREBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
97.7 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400093_4490019F1028_1_023_1F.pdf#page=26	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	CAREBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.71 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.98 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.31 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.49 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.91 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.58 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.15 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: sex: MALE food status: UNKNOWN
5.97 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
1417 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400093_4490019F1028_1_023_1F.pdf#page=26	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	CAREBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2630 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400093_4490019F1028_1_023_1F.pdf#page=26	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	CAREBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
30.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
28.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: sex: MALE food status: UNKNOWN
25.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
18.1 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400093_4490019F1028_1_023_1F.pdf#page=26	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	CAREBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
17.6 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400093_4490019F1028_1_023_1F.pdf#page=26	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	CAREBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
24.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
24.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
23.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: sex: MALE food status: UNKNOWN
37.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17518511/	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	EBASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.1% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400093_4490019F1028_1_023_1F.pdf#page=29			EBASTINE serum	Homo sapiens
2.3% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400093_4490019F1028_1_023_1F.pdf#page=29			CAREBASTINE plasma	Homo sapiens

Doses

Dose	Population	Adverse events
40 mg 1 times / day single, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: single Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/7907873/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/7907873/	Sources: https://pubmed.ncbi.nlm.nih.gov/7907873/
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/	Other AEs: Headache, Drowsiness... Other AEs: Headache (7.9%) Drowsiness (3%) dry mouth (2.1%) Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/
60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: https://pubmed.ncbi.nlm.nih.gov/28396756/	healthy Health Status: healthy Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/28396756/	Sources: https://pubmed.ncbi.nlm.nih.gov/28396756/

AEs

AE	Significance	Dose	Population
dry mouth	2.1%	20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/
Drowsiness	3%	20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/
Headache	7.9%	20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19032340/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 activator 150 inhibitor 2252	inhibitor 2438	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 rabbit CYP2J2 1 CYP1A2 2153 BSEP 550 MRP2 499 CYP2A6 879 MRP3 246 CYP2E1 1060 CYP2C19 2057 MRP4 290 CYP19A1 429	CYP2E1 729 CYP3A 220 CYP2C 16 CYP3A5 446 CYP2J2 71 CYP4F2 11 CYP2C19 1119 CYP4F12 10 CYP2B6 776 CYP2A6 626 CYP1A2 1197 P-gp 2052 CYP4A11 137

Drug as perpetrator

Target	Modality	Activity	Metabolite
CYP2D6 2546	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1671196#sid=170465995	inconclusive [IC50 10.964 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1671197#sid=170465995	inconclusive [IC50 15.4871 uM]
CYP3A4 2633	activator 342 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645841#sid=170465995	no [EC50 3.0901 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/625245#sid=103266539	no [IC50 >10 uM]
CYP2A6 911	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/625246#sid=103266539	no [IC50 >10 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/625250#sid=103266539	no [IC50 >10 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/625251#sid=103266539	no [IC50 >10 uM]
BSEP 554	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP2 625	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP3 326	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP4 345	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/743139#sid=144205778	no
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11510488/	no	Carebastine 1
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11510488/	no	Desbutyrophenone 1
CYP2C9 2497	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645842#sid=170465995	yes [IC50 13.8029 uM]
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11510488/	yes
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11510488/	yes	Hydroxyebastine 1
rabbit CYP2J2 1	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/14622984/	yes

Drug as victim

Target	Modality	Activity	Metabolite
CYP4F2 11	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	likely
CYP3A 220	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	major
CYP1A2 1197	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	no
CYP2A6 626	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	no
CYP2B6 776	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	no
CYP2C 16	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	no
CYP2C19 1119	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	no
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	no
CYP2E1 729	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	no
CYP4A11 137	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	no
CYP2J2 71	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16896065/	yes [Km 0.75 uM]	Hydroxyebastine 1
CYP2J2 71	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	yes [Km 1.3 uM]
CYP3A5 446	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16896065/	yes [Km 21.9 uM]	Hydroxyebastine 1
CYP4F12 10	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11752129/	yes [Km 3 uM]
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16896065/	yes [Km 3.85 uM]	Carebastine 1
CYP3A5 446	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16896065/	yes [Km 5.56 uM]
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16896065/	yes [Km 7.63 uM]	Hydroxyebastine 1
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16896065/	yes [Km 7.67 uM]
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11510488/	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubmed.ncbi.nlm.nih.gov/9103502/ \| https://pubchem.ncbi.nlm.nih.gov/bioassay/625171#sid=103266539

PubMed

Title	Date	PubMed
Mechanism responsible for epileptogenic activity by first-generation H1-antagonists in rats.	2000 Dec 22	11134603
Safety of antihistamines in children.	2001	11235817
Problems of heart rate correction in assessment of drug-induced QT interval prolongation.	2001 Apr	11332559
Transport characteristics of ebastine and its metabolites across human intestinal epithelial Caco-2 cell monolayers.	2001 Aug	11510488
Blockade of eosinophil migration and airway hyperresponsiveness by cPLA2-inhibition.	2001 Feb	11175812
Simultaneous determination of the histamine H1-receptor antagonist ebastine and its two metabolites, carebastine and hydroxyebastine, in human plasma using high-performance liquid chromatography.	2001 Jun 5	11419742
Urticaria to cetirizine.	2002	12371532
[Comparative antihistamine and anti-allergic effects of various antihistamine preparations].	2002	11980129
Involvement of CYP2J2 and CYP4F12 in the metabolism of ebastine in human intestinal microsomes.	2002 Jan	11752129
[Effect of H1 histamine receptor antagonists on T cell functions].	2003 Nov	14685035
A study comparing the inhibitory effects of single and repeated oral doses of ebastine and fexofenadine against histamine-induced skin reactivity.	2003 Nov	14646388
Fixed drug eruption due to loratadine.	2003 Sep-Oct	14572420
Pharmacokinetics and safety of ebastine in patients with impaired hepatic function compared with healthy volunteers: a phase I open-label study.	2004	14748620
Efficacy and safety of ebastine 20 mg compared to loratadine 10 mg once daily in the treatment of seasonal allergic rhinitis: a randomized, double-blind, placebo-controlled study.	2004 Apr	15031611
A review of the second-generation antihistamine ebastine for the treatment of allergic disorders.	2004 Aug	15264995
Anti-inflammatory activity of H1-receptor antagonists: review of recent experimental research.	2004 Jan	14741075
Pharmacological management of allergic rhinitis in the elderly: safety issues with oral antihistamines.	2005	15839718
Management of persistent allergic rhinitis: evidence-based treatment with levocetirizine.	2005 Dec	18360569
Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity.	2005 Feb	15861034
Antihistamines and driving ability: evidence from on-the-road driving studies during normal traffic.	2005 Mar	15801256
Safety of ebastine.	2005 Mar	15801255
[Cardiac arrest following treatment with non-cardiologic QT-interval-increasing medications].	2005 May 2	15929273
Comparison of inhibition of cutaneous histamine reaction of ebastine fast-dissolving tablet [20 mg] versus desloratadine capsule [5 mg]: a randomized, double-blind, double-dummy, placebo-controlled, three-period crossover study in healthy, nonatopic adults.	2007 Dec	18201596
[Ebastine-induced hepatotoxicity].	2007 Oct	17949619
Rupatadine in allergic rhinitis and chronic urticaria.	2008 Apr	18339040
Granular parakeratosis presenting with facial keratotic papules.	2008 Jan-Feb	18187827
Probing ligand binding modes of human cytochrome P450 2J2 by homology modeling, molecular dynamics simulation, and flexible molecular docking.	2008 May 1	18004755
Evaluation of efficacy and sedative profiles of H(1) antihistamines by large-scale surveillance using the visual analogue scale (VAS).	2008 Sep	18566547

Patents

Sample Use Guides

In Vivo Use Guide

Once-daily, 10 mg.

Route of Administration: Oral

In Vitro Use Guide

In vitro, ebastine and carebastine were shown to block the release of anti-IgE-induced eicosanoids LTC4/D4 and PGD2. Ebastine inhibited release of the two mediators by 30% at clinically relevant concentrations (IC30 = 2.57–9.6 umol/L).

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:05:44 GMT 2025` Edited by `admin` on `Mon Mar 31 18:05:44 GMT 2025`
Record UNII	TQD7Q784P1
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LAS-W-090

Preferred Name

English

EBASTINE

Official Name

English

RP-64305

Code

English

EBASTINE [EP MONOGRAPH]

Common Name

English

RP 64305

Code

English

EBASTINE [EP IMPURITY]

Common Name

English

Ebastine [WHO-DD]

Common Name

English

EBASTINE [MART.]

Common Name

English

EBASTINE [USAN]

Common Name

English

EBASTINE [JAN]

Common Name

English

ebastine [INN]

Common Name

English

EBASTINE [MI]

Common Name

English

Classification Tree Code System Code

WHO-ATC

R06AX22