Mizolastine
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Also known as MizolastinaMizollenSID50125752SID144206216SID170465604MIZOLASTINE (MIZOLLEN)
Summary
Mizolastine (CHEMBL94454) is an approved small molecule (ATC R06AX25) targeting HRH1; indicated across 1 condition including allergic disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AX25
- Targets: 1 (HRH1)
- Indications: 1 condition
- Clinical trials: 1
- Chemistry: 432.5 Da · C24H25FN6O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL94454 |
| Name | Mizolastine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 65906 |
| ATC | R06AX25 |
| Molecular formula | C24H25FN6O |
| Molecular weight | 432.5 |
| InChIKey | PVLJETXTTWAYEW-UHFFFAOYSA-N |
SMILES: CN(C1CCN(CC1)C2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)F)C5=NC=CC(=O)N5
IUPAC name: 2-[[1-[1-[(4-fluorophenyl)methyl]benzimidazol-2-yl]piperidin-4-yl]-methylamino]-1H-pyrimidin-6-one
Also known as: Mizolastina, Mizolastine, Mizollen, mizolastine, SID50125752, SID144206216, MIZOLASTINE, SID170465604, MIZOLASTINE (MIZOLLEN), Mizolastine (Mizollen)
Patent coverage: 2,202 distinct patent families (8,820 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 8,752 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| HRH1 | H1 receptor | Antagonist | 7.33 | 0% | P35367 |
Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Muscarinic acetylcholine receptor M1, Histamine H1 receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, 3’,5’-cyclic-AMP phosphodiesterase 4D.
Bioactivity
ChEMBL activities: 13 potent at pChembl ≥ 5 of 16 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HRH1 | 8.57 | Ki | 2.7 | nM | CHEMBL_ACT_2719632 |
| CHRM1 | 7.96 | AC50 | 11 | nM | CHEMBL_ACT_25136002 |
| KCNH2 | 6.46 | IC50 | 350 | nM | CHEMBL_ACT_345125 |
| KCNH2 | 6.45 | IC50 | 354.8 | nM | CHEMBL_ACT_1429841 |
| KCNH2 | 6.45 | IC50 | 354.8 | nM | CHEMBL_ACT_2645519 |
| KCNH2 | 6.36 | IC50 | 436.5 | nM | CHEMBL_ACT_1042007 |
| KCNH2 | 6.36 | IC50 | 436.5 | nM | CHEMBL_ACT_1523680 |
| KCNH2 | 6.36 | IC50 | 436.5 | nM | CHEMBL_ACT_2358294 |
| KCNH2 | 6.36 | IC50 | 441 | nM | CHEMBL_ACT_2720052 |
| KCNH2 | 6.36 | IC50 | 436.5 | nM | CHEMBL_ACT_5218981 |
| KCNH2 | 5.48 | AC50 | 3340 | nM | CHEMBL_ACT_25118629 |
| PDE3A | 5.21 | AC50 | 6100 | nM | CHEMBL_ACT_25191236 |
| KCNH2 | 5.14 | Ki | 7258 | nM | CHEMBL_ACT_2719681 |
Target pathways
Aggregated over 1 target gene(s): HRH1.
Top Reactome pathways
2 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Histamine receptors | 1 | HRH1 |
| G alpha (q) signalling events | 1 | HRH1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| inflammatory response | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 1 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 1 |
| chemical synaptic transmission | 1 |
| memory | 1 |
| visual learning | 1 |
| regulation of vascular permeability | 1 |
| positive regulation of vasoconstriction | 1 |
| regulation of synaptic plasticity | 1 |
| cellular response to histamine | 1 |
| signal transduction | 1 |
| phospholipase C-activating serotonin receptor signaling pathway | 1 |
Indications & clinical
Indications
1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| allergic disease | 4 | MONDO:0005271 | MONDO:0005271 |
Clinical trials
Total trials: 1.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01928316 | PHASE1 | COMPLETED | A Bioequivalence Study of Domestic (Made in China) and Imported Mizolastine Tablets in Healthy Volunteers |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
295 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ACLIDINIUM BROMIDE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| PALIPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| PRAMIPEXOLE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | HRH1 |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ACRIVASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMISULPRIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMSACRINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ANTAZOLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| ASENAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| ATOMOXETINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AZATADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | HRH1 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | HRH1 |
| BENZTROPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | HRH1 |
| BETAMETHASONE PHOSPHORIC ACID | ChEMBL | Phase 4 (approved) | HRH1 |
| BIPERIDEN | ChEMBL | Phase 4 (approved) | HRH1 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| BROMPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| BROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUCLIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUPROPION | ChEMBL | Phase 4 (approved) | HRH1 |
| BUSPIRONE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUTRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CABERGOLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | HRH1 |
| CAPTOPRIL | ChEMBL | Phase 4 (approved) | HRH1 |
| CARBINOXAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CETIRIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORDIAZEPOXIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPHENTERMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | HRH1 |
| CINACALCET | ChEMBL | Phase 4 (approved) | HRH1 |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| CITALOPRAM | ChEMBL | Phase 4 (approved) | HRH1 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOFAZIMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLOBENZAPRINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DESIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DEXBROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DEXCHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DIBENZEPIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DICYCLOMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DIETHYLPROPION | ChEMBL | Phase 4 (approved) | HRH1 |
| DIMENHYDRINATE | ChEMBL | Phase 4 (approved) | HRH1 |
| DIPHEMANIL | ChEMBL | Phase 4 (approved) | HRH1 |
| DIPHENHYDRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | HRH1 |
| DOTHIEPIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DOXEPIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DROPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| DULOXETINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DYCLONINE | ChEMBL | Phase 4 (approved) | HRH1 |
| EBASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| EPALRESTAT | ChEMBL | Phase 4 (approved) | HRH1 |
| ESCITALOPRAM | ChEMBL | Phase 4 (approved) | HRH1 |
| FENTANYL | ChEMBL | Phase 4 (approved) | HRH1 |
| FEXOFENADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| FLUDROCORTISONE | ChEMBL | Phase 4 (approved) | HRH1 |
| FLUOXETINE | ChEMBL | Phase 4 (approved) | HRH1 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | HRH1 |
| GLYCOPYRRONIUM BROMIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| HISTAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| HYDROXOCOBALAMIN | ChEMBL | Phase 4 (approved) | HRH1 |
| HYDROXYZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| IDARUBICIN | ChEMBL | Phase 4 (approved) | HRH1 |
| ILOPERIDONE | ChEMBL | Phase 4 (approved) | HRH1 |
| IMIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | HRH1 |
| IPRINDOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| KETANSERIN | ChEMBL | Phase 4 (approved) | HRH1 |
| KETOTIFEN | ChEMBL | Phase 4 (approved) | HRH1 |
| LASOFOXIFENE | ChEMBL | Phase 4 (approved) | HRH1 |
| LEVOCETIRIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| LOFEPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| LORATADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| LORCASERIN | ChEMBL | Phase 4 (approved) | HRH1 |
Related Atlas pages
- Genes: HRH1
- Indicated for: allergic disease
- Drugs: Aclidinium Bromide, Desloratadine, Dihydroergotamine, Paliperidone, Pramipexole, Abemaciclib, Acetophenazine, Acrivastine, Amiodarone, Amisulpride, Amitriptyline, Amoxapine, Amsacrine, Antazoline, Apomorphine, Aripiprazole, Asenapine, Astemizole, Atomoxetine, Azatadine, Azelastine, Benfluorex, Benperidol, Benzbromarone, Benztropine, Bepridil, Betamethasone Phosphoric Acid, Biperiden, Brexpiprazole, Bromperidol, Brompheniramine, Buclizine, Bupropion, Buspirone, Butriptyline, Cabergoline, Candesartan Cilexetil, Captopril, Carbinoxamine, Cariprazine, Cetirizine, Chlordiazepoxide, Chlorpheniramine, Chlorphentermine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Cisapride, Citalopram, Clemastine, Clofazimine, Clomipramine, Clotrimazole, Clozapine, Cyclizine, Cyclobenzaprine, Cyproheptadine, Daunorubicin, Desipramine, Dexbrompheniramine, Dibenzepin, Dicyclomine, Diethylpropion, Dimenhydrinate, Diphemanil, Diphenhydramine, Domperidone, Dothiepin, Doxepin, Droperidol, Duloxetine, Dyclonine, Ebastine, Epalrestat, Fentanyl, Fexofenadine, Fludrocortisone, Fluoxetine, Fluphenazine, Fluspirilene, Glycopyrronium Bromide, Haloperidol, Histamine, Hydroxocobalamin, Hydroxyzine, Idarubicin, Iloperidone, Imipramine, Indocyanine Green Acid Form, Iprindole, Ketanserin, Ketotifen, Lasofoxifene, Lofepramine, Loratadine, Lorcaserin