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Details

Stereochemistry ACHIRAL
Molecular Formula C24H25FN6O
Molecular Weight 432.4933
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MIZOLASTINE

SMILES

CN(C1CCN(CC1)C2=NC3=C(C=CC=C3)N2CC4=CC=C(F)C=C4)C5=NC=CC(=O)N5

InChI

InChIKey=PVLJETXTTWAYEW-UHFFFAOYSA-N
InChI=1S/C24H25FN6O/c1-29(23-26-13-10-22(32)28-23)19-11-14-30(15-12-19)24-27-20-4-2-3-5-21(20)31(24)16-17-6-8-18(25)9-7-17/h2-10,13,19H,11-12,14-16H2,1H3,(H,26,28,32)

HIDE SMILES / InChI
Molecular Formula C24H25FN6O
Molecular Weight 432.4933
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including http://www.medicines.org.uk/emc/medicine/19970/SPC/Mizollen+10+mg+modified-release+tablets

Mizolastine (Mizollen) is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria. It blocks H1 receptors and is commonly fast-acting. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Side effects can include dry mouth and throat

CNS Activity

CNS Non-penetrant
1040
Curator's Comment: Mizolastine did not influence on the central nervous system (CNS) at up to 1,500 times the effective dosage

Originator

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2849
 47.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
Mizollen

Approved Use

Mizolastine is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria.

Launch Date

2003
Primary
Approved
8583
Mizollen

Approved Use

Mizolastine is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria.

Launch Date

2003
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
351.6 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29702735/
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MIZOLASTINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2636.8 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29702735/
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MIZOLASTINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.13 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29702735/
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MIZOLASTINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
75 mg single, oral
Highest studied dose
Dose: 75 mg
Route: oral
Route: single
Dose: 75 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/1354949/
https://pubmed.ncbi.nlm.nih.gov/11510627/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: unknown
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/1354949/
https://pubmed.ncbi.nlm.nih.gov/11510627/
Sources:
https://pubmed.ncbi.nlm.nih.gov/1354949/
https://pubmed.ncbi.nlm.nih.gov/11510627/
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
Disc. AE: Drowsiness, Dizziness...
Other AEs: Headache, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Drowsiness (grade 2, 3.6%)
Dizziness (grade 2, 3.6%)
Other AEs:
Headache
Diarrhea
Nausea
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
10 mg single, oral
Recommended
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/16937762/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16937762/
Other AEs: Anaphylaxis...
Other AEs:
Anaphylaxis
Sources:
https://pubmed.ncbi.nlm.nih.gov/16937762/
AEs

AEs

AESignificanceDosePopulation
Diarrhea
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
Headache
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
Nausea
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
Dizziness grade 2, 3.6%
Disc. AE
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
Drowsiness grade 2, 3.6%
Disc. AE
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/8836336/
Anaphylaxis
10 mg single, oral
Recommended
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/16937762/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16937762/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252
inhibitor
2438
inhibitor
2507

substrate
1388
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2C19
2057

UGT
45

UGT1A6
136

CYP2E1
1060

UGT1A1
246

CYP19A1
429
SULT
12

UGT
219

CYP3A5
446

CYP2A6
626

P-gp
2052
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
2333
 no [IC50 >100 uM]
CYP2C19
2141
 no [IC50 >100 uM]
UGT
70
 no [IC50 >100 uM]
UGT1A1
303
 no [IC50 >100 uM]
UGT1A6
171
 no [IC50 >100 uM]
CYP19A1
430
 no
CYP3A4
2633
 weak [IC50 119 uM]
CYP2C9
2497
 weak [IC50 69 uM]
CYP2D6
2546
 weak
CYP2E1
1146
 weak
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
UGT
219
 major
CYP2A6
626
 minor
CYP2D6
1388
 minor
SULT
12
 minor
CYP3A4
1946
 yes
CYP3A5
446
 yes
P-gp
2052
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
PubMed

PubMed

TitleDatePubMed
Cetirizine and loratadine: minimal risk of QT prolongation.
2010-02
Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine.
2000-11
Antiallergic effects of H1-receptor antagonists.
2000
Efficacy and safety of mizolastine 10 mg in a placebo-controlled comparison with loratadine in chronic idiopathic urticaria: results of the MILOR Study.
1999-01
Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria.
1998-07
In vivo and in vitro interaction of the novel selective histamine H1 receptor antagonist mizolastine with H1 receptors in the rodent.
1995-05
Patents

Patents

JP2008526895A
32
JP2011529894A
1

Sample Use Guides

In Vivo Use Guide
10 mg daily was administered for 14 days during the pollen season
Route of Administration: Oral
In Vitro Use Guide
The highest dose of mizolastine (6 x 10(-6) M), corresponding to 10-fold the peak plasma level after a single oral administration of 10 mg, was able to act on fibroblasts, significantly downregulating the expression of CD54 (p<0.05). Regarding T lymphocyte proliferation, the addition of mizolastine did not induce any significant change; furthermore, mizolastine was ineffective at all of the tested concentrations on both HLA-DR expression and CD4+/CD8+ ratio.
Substance Class Chemical
Created
by admin
on Wed Apr 02 09:56:00 GMT 2025
Edited
by admin
on Wed Apr 02 09:56:00 GMT 2025
Record UNII
244O1F90NA
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MIZOLLEN
Preferred Name English
MIZOLASTINE
INN   JAN   MART.   MI   WHO-DD  
INN  
Official Name English
mizolastine [INN]
Common Name English
MIZOLASTINE [MI]
Common Name English
MIZOLASTINE [MART.]
Common Name English
2-((1-(1-(P-FLUOROBENZYL)-2-BENZIMIDAZOLYL)-4-PIPERIDYL)METHYLAMINO)-4(3H)-PYRIMIDINONE
Common Name English
Mizolastine [WHO-DD]
Common Name English
MIZOLASTINE [JAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29578
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
WHO-ATC R06AX25
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
WHO-VATC QR06AX25
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
Code System Code Type Description
EVMPD
SUB09018MIG
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
DRUG BANK
DB12523
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
FDA UNII
244O1F90NA
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
MERCK INDEX
m7577
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY Merck Index
NCI_THESAURUS
C66171
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
CAS
108612-45-9
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
DRUG CENTRAL
1824
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
PUBCHEM
65906
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
WIKIPEDIA
MIZOLASTINE
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
ChEMBL
CHEMBL94454
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
SMS_ID
100000080903
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
EPA CompTox
DTXSID5046801
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
RXCUI
61455
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY RxNorm
INN
6663
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
MESH
C076170
Created by admin on Wed Apr 02 09:56:00 GMT 2025 , Edited by admin on Wed Apr 02 09:56:00 GMT 2025
PRIMARY
Related Record Type Details
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
HISTAMINE H1 RECEPTOR
TARGET -> INHIBITOR
Kd
Related Record Type Details
Structure of MIZOLASTINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
NIH
NCATS
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