NAV

Mizolastine

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Summary

Mizolastine is a second-generation non-sedating antihistamine used to treat symptoms of allergic rhinoconjunctivitis and urticaria.

Generic Name
Mizolastine
DrugBank Accession Number
DB12523
Background

Mizolastine is under investigation in clinical trial NCT01928316 (A Bioequivalence Study of Domestic (Made in China) and Imported Mizolastine Tablets in Healthy Volunteers).

Type
Small Molecule
Groups
Approved, Investigational
Structure
3D
Similar Structures
Weight
Average: 432.503
Monoisotopic: 432.207387612
Chemical Formula
C24H25FN6O
Synonyms
  • Mizolastina
  • Mizolastine
  • Mizolastinum
External IDs
  • CCRIS 8410
  • SL 85.0324
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Pharmacology

Indication

Not Available

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Symptomatic treatment ofPerennial allergic rhinitis (par)••••••••••••••••••• ••••••• •••••••
Symptomatic treatment ofSeasonal allergic rhinitis••••••••••••••••••• ••••••• •••••••
Symptomatic treatment ofUrticaria••••••••••••••••••• ••••••• •••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action
Not Available
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
PathwayCategory
Mizolastine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
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interactions in your software
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Mizolastine.
AdenosineThe risk or severity of QTc prolongation can be increased when Adenosine is combined with Mizolastine.
AjmalineThe risk or severity of QTc prolongation can be increased when Ajmaline is combined with Mizolastine.
AlfuzosinThe risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Mizolastine.
AlimemazineThe risk or severity of QTc prolongation can be increased when Alimemazine is combined with Mizolastine.
Food Interactions
Not Available

Products

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International/Other Brands
Mizollen

Categories

ATC Codes
R06AX25 — Mizolastine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as benzimidazoles. These are organic compounds containing a benzene ring fused to an imidazole ring (five member ring containing a nitrogen atom, 4 carbon atoms, and two double bonds).
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzimidazoles
Sub Class
Not Available
Direct Parent
Benzimidazoles
Alternative Parents
Dialkylarylamines / Hydroxypyrimidines / Fluorobenzenes / Aminopyrimidines and derivatives / Piperidines / N-substituted imidazoles / Aryl fluorides / Aminoimidazoles / Heteroaromatic compounds / Azacyclic compounds
show 4 more
Substituents
Aminoimidazole / Aminopyrimidine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle / Azole / Benzenoid / Benzimidazole / Dialkylarylamine
show 17 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
244O1F90NA
CAS number
108612-45-9
InChI Key
PVLJETXTTWAYEW-UHFFFAOYSA-N
InChI
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)
IUPAC Name
2-[(1-{1-[(4-fluorophenyl)methyl]-1H-1,3-benzodiazol-2-yl}piperidin-4-yl)(methyl)amino]-3,4-dihydropyrimidin-4-one
SMILES
CN(C1CCN(CC1)C1=NC2=C(C=CC=C2)N1CC1=CC=C(F)C=C1)C1=NC=CC(=O)N1

References

General References
  1. EMC Package Leaflet: Mizollen (mizolastine) modified-release tablets [Link]
  2. EMC Summary of Product Characteristics: Mizollen (mizolastine) modified-release tablets for oral use [Link]
Human Metabolome Database
HMDB0240233
PubChem Compound
65906
PubChem Substance
347828752
ChemSpider
59315
BindingDB
22877
RxNav
61455
ChEBI
31857
ChEMBL
CHEMBL94454
ZINC
ZINC000013831810
PharmGKB
PA166129535
Wikipedia
Mizolastine

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Subjects (HS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral
TabletOral10 mg
Tablet, extended releaseOral10 mg
Tablet, film coatedOral10 MG
Tablet, delayed releaseOral10 MG
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0893 mg/mLALOGPS
logP3.51ALOGPS
logP3.73Chemaxon
logS-3.7ALOGPS
pKa (Strongest Acidic)8.08Chemaxon
pKa (Strongest Basic)5.63Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area65.76 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity122.28 m3·mol-1Chemaxon
Polarizability46.07 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-0a4i-0011900000-375df4a855e43dfec509
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-001i-0721900000-53e1c9b1a9ae2a2a816d
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0011900000-375df4a855e43dfec509
MS/MS Spectrum - , positiveLC-MS/MSsplash10-056s-1924000000-3222d3ee56cb73f00360
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-0721900000-53e1c9b1a9ae2a2a816d
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-0000900000-cb7365a0ae4d985c784f
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-0000900000-333a55ab516ac9d5b5b9
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-0000900000-36ea7186247ce8066d99
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-01qj-1009500000-7bb4a2ad2c8890141222
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-055k-0149300000-d44e7292dff7d20b95ba
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-2139300000-89afc900a55c516afea7
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-221.5874941
predicted
DarkChem Lite v0.1.0
[M-H]-218.8513941
predicted
DarkChem Lite v0.1.0
[M-H]-194.78941
predicted
DeepCCS 1.0 (2019)
[M+H]+222.3702941
predicted
DarkChem Lite v0.1.0
[M+H]+218.8164941
predicted
DarkChem Lite v0.1.0
[M+H]+197.14743
predicted
DeepCCS 1.0 (2019)
[M+Na]+221.7293941
predicted
DarkChem Lite v0.1.0
[M+Na]+218.9775941
predicted
DarkChem Lite v0.1.0
[M+Na]+203.90608
predicted
DeepCCS 1.0 (2019)

Enzymes

Details1. Cytochrome P450 2D6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Nicolas JM, Whomsley R, Collart P, Roba J: In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem Biol Interact. 1999 Nov 15;123(1):63-79. [Article]
  2. Interactions of the H1 antihistamines [Link]

Drug created at October 20, 2016 22:42 / Updated at June 02, 2021 20:03