Mizolastine
This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Identification
- Name
- Mizolastine
- Accession Number
- DB12523
- Description
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
Structure for Mizolastine (DB12523)
- Weight
- Average: 432.503
Monoisotopic: 432.207387612 - Chemical Formula
- C24H25FN6O
- Synonyms
- Mizolastina
- Mizolastine
- Mizolastinum
- External IDs
- CCRIS 8410
- SL 85.0324
Pharmacology
- Indication
- Not Available
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
- Not Available
- Affected organisms
- Not Available
- Pathways
Pathway Category Mizolastine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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.
Drug Interaction Unlock Additional DataAcebutolol The risk or severity of QTc prolongation can be increased when Acebutolol is combined with Mizolastine. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Mizolastine. Acrivastine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Mizolastine. Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Mizolastine. Ajmaline The risk or severity of QTc prolongation can be increased when Ajmaline is combined with Mizolastine. Alfuzosin The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Mizolastine. Alimemazine The risk or severity of QTc prolongation can be increased when Alimemazine is combined with Mizolastine. Almotriptan The metabolism of Almotriptan can be decreased when combined with Mizolastine. Alogliptin The metabolism of Alogliptin can be decreased when combined with Mizolastine. Amantadine The risk or severity of QTc prolongation can be increased when Amantadine is combined with Mizolastine. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
Products
- International/Other Brands
- Mizollen
Categories
- ATC Codes
- R06AX25 — Mizolastine
- Drug Categories
- Antihistamines for Systemic Use
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Heterocyclic Compounds, Fused-Ring
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Histamine H1 Antagonists, Non-Sedating
- Moderate Risk QTc-Prolonging Agents
- Neurotransmitter Agents
- QTc Prolonging Agents
- 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
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
- EMC Package Leaflet: Mizollen (mizolastine) modified-release tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0240233
- PubChem Compound
- 65906
- PubChem Substance
- 347828752
- ChemSpider
- 59315
- BindingDB
- 22877
- 61455
- ChEBI
- 31857
- ChEMBL
- CHEMBL94454
- ZINC
- ZINC000013831810
- PharmGKB
- PA166129535
- Wikipedia
- Mizolastine
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Completed Treatment Healthy Volunteers 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, coated Oral 10 MG Tablet, delayed release Oral 10 MG - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0893 mg/mL ALOGPS logP 3.51 ALOGPS logP 3.73 ChemAxon logS -3.7 ALOGPS pKa (Strongest Acidic) 8.08 ChemAxon pKa (Strongest Basic) 5.63 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 5 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 65.76 Å2 ChemAxon Rotatable Bond Count 5 ChemAxon Refractivity 122.28 m3·mol-1 ChemAxon Polarizability 46.07 Å3 ChemAxon Number of Rings 5 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-0a4i-0011900000-375df4a855e43dfec509 MS/MS Spectrum - , positive LC-MS/MS splash10-056s-1924000000-3222d3ee56cb73f00360 MS/MS Spectrum - , positive LC-MS/MS splash10-001i-0721900000-53e1c9b1a9ae2a2a816d
Enzymes
- 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
- 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. [PubMed:10597902]
- Interactions of the H1 antihistamines [Link]
Drug created on October 20, 2016 16:42 / Updated on October 21, 2020 11:50
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