Azelastine
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Also known as AzelastinaNSC-758971rac-AzelastineAzelastineAstelinOptivar
Summary
Azelastine (CHEMBL639) is an approved small-molecule H1-receptor antagonist (ATC R01AC03) targeting HRH1; indicated across 6 conditions including eye allergy and allergic disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R01AC03 (+2 more)
- Targets: 1 (HRH1)
- Indications: 6 conditions
- Clinical trials: 27
- Chemistry: 381.9 Da · C22H24ClN3O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL639 |
| Name | Azelastine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 2267 |
| ChEBI | CHEBI:2950 |
| ATC | R01AC03, R06AX19, S01GX07 |
| Molecular formula | C22H24ClN3O |
| Molecular weight | 381.9 |
| InChIKey | MBUVEWMHONZEQD-UHFFFAOYSA-N |
SMILES: CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl
IUPAC name: 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one
ChEBI definition: A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.
Pharmacological roles (ChEBI): H1-receptor antagonist, anti-allergic agent, anti-asthmatic drug, bronchodilator agent, platelet aggregation inhibitor, EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor.
Also known as: Azelastina, Azelastine, NSC-758971, rac-Azelastine, azelastine, AZELASTINE, Azelastine; Astelin, Optivar
Parent form; salt/anhydrous children: CHEMBL1200809
Patent coverage: 4,301 distinct patent families (16,805 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 16,664 (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 | 8.9 | 0% | P35367 |
Broader ChEMBL bioactivity targets: 28 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Neuronal acetylcholine receptor subunit alpha-4, 5-hydroxytryptamine receptor 3A, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Muscarinic acetylcholine receptor M2, Beta-1 adrenergic receptor, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter.
Bioactivity
ChEMBL activities: 47 potent at pChembl ≥ 5 of 57 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HRH1 | 9.7 | Kd | 0.2 | nM | CHEMBL_ACT_12037515 |
| HRH1 | 9.7 | Kd | 0.2 | nM | CHEMBL_ACT_16812248 |
| HRH1 | 9.7 | Kd | 0.2 | nM | CHEMBL_ACT_18221313 |
| HRH1 | 9.7 | Kd | 0.2 | nM | CHEMBL_ACT_25101033 |
| HRH1 | 9.7 | Kd | 0.2 | nM | CHEMBL_ACT_6175539 |
| HRH1 | 8.92 | Ki | 1.2 | nM | CHEMBL_ACT_12037516 |
| HRH1 | 8.92 | Ki | 1.2 | nM | CHEMBL_ACT_16812132 |
| HRH1 | 8.9 | Ki | 1.26 | nM | CHEMBL_ACT_25101076 |
| HRH1 | 8.9 | Ki | 1.26 | nM | CHEMBL_ACT_6175677 |
| HTR2B | 7.7 | Ki | 19.95 | nM | CHEMBL_ACT_18221379 |
| HRH1 | 7.62 | AC50 | 24 | nM | CHEMBL_ACT_25212184 |
| ADRA1B | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_12037464 |
| ADRA1A | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_12037496 |
| ADRA1A | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_16812166 |
| ADRA1B | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_16812183 |
| P43140 | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_18221383 |
| ADRA1A | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_25101088 |
| ADRA1B | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_25101100 |
| ADRA1B | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_6175568 |
| ADRA1A | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_6175604 |
| KCNH2 | 7 | IC50 | 100 | nM | CHEMBL_ACT_12037489 |
| KCNH2 | 7 | IC50 | 100 | nM | CHEMBL_ACT_16812217 |
| KCNH2 | 7 | IC50 | 100 | nM | CHEMBL_ACT_18221256 |
| KCNH2 | 7 | IC50 | 100 | nM | CHEMBL_ACT_25101123 |
| KCNH2 | 7 | IC50 | 100 | nM | CHEMBL_ACT_25101147 |
| KCNH2 | 7 | IC50 | 100 | nM | CHEMBL_ACT_6175529 |
| HRH3 | 6.83 | Ki | 147.9 | nM | CHEMBL_ACT_12037424 |
| HRH3 | 6.83 | Ki | 147.9 | nM | CHEMBL_ACT_16812149 |
| HRH3 | 6.8 | Ki | 158.5 | nM | CHEMBL_ACT_6175636 |
| P0DTC2 | 6.59 | Kd | 258 | nM | CHEMBL_ACT_29077440 |
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
6 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| eye allergy | 4 | MONDO:0005551 | EFO:0005751 |
| allergic disease | 4 | MONDO:0005271 | MONDO:0005271 |
| seasonal allergic rhinitis | 3 | MONDO:0005324 | EFO:0003956 |
| allergic rhinitis | 3 | MONDO:0011786 | EFO:0005854 |
| perennial allergic rhinitis | 3 | MONDO:0024332 | EFO:1001417 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 27.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 10 |
| PHASE3 | 9 |
| PHASE2 | 4 |
| PHASE1 | 3 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05626621 | PHASE4 | RECRUITING | Efficacy of Azelastine and Mometasone Irrigation in Comparison to Nasal Sprays in Patients With Chronic Rhinitis |
| NCT00561717 | PHASE4 | COMPLETED | A Randomized, Placebo Controlled Study to Determine the Efficacy and Speed of a Nasal Spray in Allergen Induced Seasonal Allergic Rhinitis |
| NCT00806754 | PHASE4 | COMPLETED | Investigation of the Efficacy and Safety of Concomitant Administration of Ciclesonide Nasal Spray and Azelastine Nasal Spray in Patients (18 Years or Older) With Perennial Allergic Rhinitis (PAR) Not Adequately Controlled on an Intranasal Corticosteroid or Antihistamine Monotherapy (BY9010/M1-490) |
| NCT00845195 | PHASE4 | COMPLETED | Comparison of Seasonal Allergic Rhinitis Treatment With 2 Antihistamines Used in Combination With Intranasal Corticosteroid |
| NCT00845598 | PHASE4 | WITHDRAWN | Azelastine Fluticasone Combination vs. Fluticasone |
| NCT00979615 | PHASE4 | COMPLETED | Safety and Efficacy of Olopatadine 0.6% and Azelastine 137 Mcg in Vasomotor Rhinitis |
| NCT02238353 | PHASE4 | UNKNOWN | AZELASTINE/FLUTICASONE (AZE/FLU) Nasal Spray on Symptom Control, Nasal Mediators and Nasal Hyperresponsiveness in Allergic Rhinitis (AR) |
| NCT03004131 | PHASE4 | COMPLETED | MP-AzeFlu Allergen Chamber - Onset of Action Study |
| NCT04601324 | PHASE4 | WITHDRAWN | Allergic Rhinitis Combination Pharmacotherapy Efficacy Study |
| NCT06800274 | PHASE4 | COMPLETED | Clinical and Biological Evaluation of NAAGA Versus Azelastine Eye Drops in Allergic Subjects With Tear Film Dysfunction |
| NCT01018862 | PHASE3 | COMPLETED | A Study to Evaluate the Safety and Efficacy of a Nasal Spray to Treat Children With Perennial Allergic Rhinitis |
| NCT01368445 | PHASE3 | COMPLETED | A Study to Evaluate the Safety and Efficacy of a Nasal Spray to Treat Seasonal Allergies |
| NCT01915823 | PHASE3 | COMPLETED | Safety and Efficacy Trial of Dymista Nasal Spray in Children Ages 4 to 11 With Seasonal Allergic Rhinitis (SAR) |
| NCT02249663 | PHASE3 | UNKNOWN | Clinical Equivalence of Azelastine Hydrochloride and Fluticasone Propionate, 137/50 mcg Nasal Spray to Dymista™ |
| NCT03599791 | PHASE3 | COMPLETED | DYmista NAsal Spray in CHInese Patients |
| NCT04264637 | PHASE3 | COMPLETED | Study to Find Out How Long it Takes Azelastine Hydrochloride 0.15% Nasal Spray to Relieve Symptoms in Patients Suffering From Allergic Rhinitis |
| NCT05311475 | PHASE3 | COMPLETED | Prospective, Randomized, Multinational, Multicenter, Double-blind, Placebo and Active Controlled Trial in 4 Parallel-groups of Patients Suffering From Seasonal Allergic Rhinitis |
| NCT05590598 | PHASE3 | COMPLETED | Efficacy and Safety of Azelastine +Mometasone , Nasal Spray, 140 mcg + 50 mcg, (Sandoz d.d., Slovenia) and Momat Rino Advance, Nasal Spray, 140 mcg + 50 mcg, (Glenmark, India) Administered as a Monotherapy to Patients With Seasonal Allergic Rhinitis. |
| NCT06212973 | PHASE3 | COMPLETED | A Study to Evaluate the Efficacy and Safety of Epinastine Hydrochloride Eye Drops in the Treatment of Chinese Seasonal Allergic Conjunctivitis Patients |
| NCT00940953 | PHASE2 | COMPLETED | Compare Captisol-Enabled (CE) Budesonide + Azelastine Nasal Solution and Rhinocort Aqua + Astelin in an Environmental Exposure Chamber (EEC) Study of Allergic Rhinitis |
| NCT01382654 | PHASE2 | COMPLETED | Two Formulations and Concentrations of Epinastine Nasal Spray Versus Azelastine Nasal Solution for Allergic Rhinitis |
| NCT02279563 | PHASE2 | UNKNOWN | A Study Comparing the Bioequivalence of Azelastine Hydrochloride and Fluticasone Propionate Nasal Spray (Apotex, Inc.) to That of Dymista™ Nasal Spray (Meda Pharmaceuticals, Inc.) in the Treatment of Seasonal Allergic Rhinitis |
| NCT06051786 | PHASE2 | COMPLETED | A Study to Evaluate the Safety and Effectiveness of a Nasal Spray to Treat Perennial Allergic Rhinitis |
| NCT01190852 | PHASE1 | COMPLETED | Single Dose Pharmacokinetics of Intranasal Azelastine Delivered by a Fixed Combination With Fluticasone in Comparison to Azelastine Nasal Sprays |
| NCT01194622 | PHASE1 | COMPLETED | Single Dose Pharmacokinetics of Intranasal Fluticasone Delivered by a Fixed Combination With Azelastine (MP29 02) in Comparison to Two Different Fluticasone Nasal Sprays |
| NCT05887843 | PHASE1 | TERMINATED | Study to Compare the Pharmacokinetics of Fixed-Dose Combination of Mometasone + Azelastine Nasal Spray to Mometasone and Azelastine Nasal Sprays in Adolescents and Young Adults With Seasonal Allergic Rhinitis |
| NCT04561687 | Not specified | UNKNOWN | Comparison of Montelukast and Azelastine in Treatment of Moderate to Severe Allergic Rhinitis |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
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 60 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 |
| 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 |
Related Atlas pages
- Genes: HRH1
- Diseases: eye allergy, allergic disease, seasonal allergic rhinitis, allergic rhinitis, perennial allergic rhinitis
- Drugs: Aclidinium Bromide, Desloratadine, Dihydroergotamine, Paliperidone, Pramipexole, Abemaciclib, Acetophenazine, Acrivastine, Amiodarone, Amisulpride, Amitriptyline, Amoxapine, Amsacrine, Antazoline, Apomorphine, Aripiprazole, Asenapine, Astemizole, Atomoxetine, Azatadine, 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