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
Evaluation of efficacy and sedative profiles of H(1) antihistamines by large-scale surveillance using the visual analogue scale (VAS).	2008-09	18566547
Probing ligand binding modes of human cytochrome P450 2J2 by homology modeling, molecular dynamics simulation, and flexible molecular docking.	2008-05-01	18004755
Rupatadine in allergic rhinitis and chronic urticaria.	2008-04	18339040
Granular parakeratosis presenting with facial keratotic papules.	2008-01-12	18187827
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.	2007-12	18201596
Acquired cold urticaria symptoms can be safely prevented by ebastine.	2007-12	17900265
Human enteric microsomal CYP4F enzymes O-demethylate the antiparasitic prodrug pafuramidine.	2007-11	17709372
[Ebastine-induced hepatotoxicity].	2007-10	17949619
Ebastine improves nasal symptoms and airflow and affects response to decongestion test in patients with persistent allergic rhinitis: a pilot study.	2007-09-22	17883885
Selective, competitive and mechanism-based inhibitors of human cytochrome P450 2J2.	2007-08-15	17470359
[Peripheral anticholinergic syndrome].	2007-06-05	17542247
[New generation antihistamines as monotherapy or in combination. What is the relevance for daily clinical routine for allergic rhinoconjunctivitis].	2007-06	17566806
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.	2007-05	17697901
Palmoplantar pityriasis rosea: two case reports.	2007-03	17309476
Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy.	2007	17902729
[Ebastine (kestine 20) in therapy of allergic rhinitis].	2007	17768822
A comparison of ebastine 10 mg fast-dissolving tablet with oral desloratadine and placebo in inhibiting the cutaneous reaction to histamine in healthy adults.	2007	17563125
Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.	2007	17518511
Rupatadine: a review of its use in the management of allergic disorders.	2007	17335300
Long QT syndrome in a patient with allergic rhinoconjunctivitis and auto-immune diabetes: focus on the choice of anti-H1 drugs.	2006-12	17274518
Inter-individual variation of cytochrome P4502J2 expression and catalytic activities in liver microsomes from Japanese and Caucasian populations.	2006-12	17162467
CYP4F enzymes are the major enzymes in human liver microsomes that catalyze the O-demethylation of the antiparasitic prodrug DB289 [2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime].	2006-12	16997912
Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: major roles for CYP2J2 and CYP3A.	2006-11	16896065
Rupatadine: pharmacological profile and its use in the treatment of allergic disorders.	2006-10	17020424
The effect of CYP2J2, CYP3A4, CYP3A5 and the MDR1 polymorphisms and gender on the urinary excretion of the metabolites of the H-receptor antihistamine ebastine: a pilot study.	2006-08	16842392
Acceptance survey of a fast dissolving tablet pharmaceutical formulation in allergic patients. Satisfaction and expectancies.	2006-06-06	16750120
[Comparison of clinical efficacy and cost-quality of antihistamines in early treatment for Japanese cedar pollinosis].	2006-05	16883093
Stimulating effects of H1-antagonists.	2006	16842173
Management of persistent allergic rhinitis: evidence-based treatment with levocetirizine.	2005-12	18360569
Meta-analysis of the efficacy of ebastine 20 mg compared to loratadine 10 mg and placebo in the symptomatic treatment of seasonal allergic rhinitis.	2005-12	16224195
Collection of medical drug information in pharmacies: Drug Event Monitoring (DEM) in Japan.	2005-07	15997212
[Cardiac arrest following treatment with non-cardiologic QT-interval-increasing medications].	2005-05-02	15929273
Antihistamines and driving ability: evidence from on-the-road driving studies during normal traffic.	2005-03	15801256
Safety of ebastine.	2005-03	15801255
Co-administration of ketoconazole with H1-antagonists ebastine and loratadine in healthy subjects: pharmacokinetic and pharmacodynamic effects.	2005-03	15752381
Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity.	2005-02	15861034
Pharmacological management of allergic rhinitis in the elderly: safety issues with oral antihistamines.	2005	15839718
Simultaneous determination of ebastine and its three metabolites in plasma using liquid chromatography-tandem mass spectrometry.	2004-12-25	15556518
Human CYP4F12 genetic polymorphism: identification and functional characterization of seven variant allozymes.	2004-12-15	15548388
Microbial oxidation of terfenadine and ebastine into fexofenadine and carebastine.	2004-11-01	15454238
A review of the second-generation antihistamine ebastine for the treatment of allergic disorders.	2004-08	15264995
Rupatadine 10 mg and ebastine 10 mg in seasonal allergic rhinitis: a comparison study.	2004-07	15180765
Expression of CYP4F12 in gastrointestinal and urogenital epithelia.	2004-04	15078342
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.	2004-04	15031611
Antihistamines and driving ability: evidence from on-the-road driving studies during normal traffic.	2004-03	15049392
Anti-inflammatory activity of H1-receptor antagonists: review of recent experimental research.	2004-01	14741075
A randomized, double-blind, placebo-controlled study comparing the efficacy and safety of ebastine (20 mg and 10 mg) to loratadine 10 mg once daily in the treatment of seasonal allergic rhinitis.	2004	15160443
Cetirizine: a review of its use in allergic disorders.	2004	14977391
Pharmacokinetics and safety of ebastine in patients with impaired hepatic function compared with healthy volunteers: a phase I open-label study.	2004	14748620
[Effect of H1 histamine receptor antagonists on T cell functions].	2003-11	14685035

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

Download

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