Bilastine
drug drugOn this page
Also known as BilastinaIlaxtenSID170466329
Summary
Bilastine (CHEMBL1742423) is an approved small molecule (ATC R06AX29) targeting HRH1; indicated across 7 conditions including eye allergy and allergic disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AX29 (+1 more)
- Targets: 1 (HRH1)
- Indications: 7 conditions
- Clinical trials: 21
- Chemistry: 463.6 Da · C28H37N3O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1742423 |
| Name | Bilastine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 185460 |
| ATC | R06AX29, S01GX13 |
| Molecular formula | C28H37N3O3 |
| Molecular weight | 463.6 |
| InChIKey | ACCMWZWAEFYUGZ-UHFFFAOYSA-N |
SMILES: CCOCCN1C2=CC=CC=C2N=C1C3CCN(CC3)CCC4=CC=C(C=C4)C(C)(C)C(=O)O
IUPAC name: 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
Also known as: Bilastina, Bilastine, Ilaxten, SID170466329, BILASTINE
Patent coverage: 77 distinct patent families (164 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 117 (71%) 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 | 7.19 | 0% | P35367 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
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
2 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| eye allergy | 4 | MONDO:0005551 | EFO:0005751 |
| allergic disease | 4 | MONDO:0005271 | MONDO:0005271 |
5 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| seasonal allergic rhinitis | 3 | MONDO:0005324 | EFO:0003956 |
| urticaria | 3 | MONDO:0005492 | EFO:0005531 |
| perennial allergic rhinitis | 3 | MONDO:0024332 | EFO:1001417 |
| atopic conjunctivitis | 3 | MONDO:0005642 | EFO:0007141 |
| cold urticaria | 2 | MONDO:0022799 | EFO:1001881 |
Clinical trials
Total trials: 21.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 7 |
| PHASE4 | 5 |
| PHASE2 | 4 |
| PHASE1 | 3 |
| PHASE2/PHASE3 | 1 |
| PHASE1/PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01940393 | PHASE4 | COMPLETED | Evaluation of the Inhibitory Effect of 5 Anti-Histamines in Urticaria |
| NCT02513290 | PHASE4 | COMPLETED | Quality of Life in Patients With Allergic Rhinitis: Clinical Trial With Bilastine or Loratadine |
| NCT02557269 | PHASE4 | UNKNOWN | 4S - Seasonal Symptoms Suppression Study |
| NCT02576041 | PHASE4 | COMPLETED | Effects of Bilastine on F1 Simulator Driving Performance in Patients Affected by Allergic Rhinitis and/or Urticaria |
| NCT02761252 | PHASE4 | COMPLETED | Efficacy of Co-administration of Bilastine and Montelukast in Patients With SARC and Asthma |
| NCT00421109 | PHASE3 | COMPLETED | Efficacy Study for the Symptomatic Treatment of Chronic Idiopathic Urticaria |
| NCT00504933 | PHASE3 | COMPLETED | Efficacy Study for the Symptomatic Treatment of Seasonal Allergic Rhinitis |
| NCT01108783 | PHASE3 | COMPLETED | A Phase III Efficacy Study of the Symptomatic Treatment of Seasonal Allergic Rhinitis With Bilastine |
| NCT01127620 | PHASE3 | COMPLETED | Efficacy Study for the Symptomatic Treatment of Perennial Allergic Rhinitis With a 1 Year Safety Extension |
| NCT01271075 | PHASE2/PHASE3 | COMPLETED | Bilastine Updosing - Characterization of Underlying Mechanisms |
| NCT01400828 | PHASE3 | COMPLETED | Investigate the Safety/Tolerability and Efficacy of Bilastine 20mg in Korean Patients With Seasonal Allergic Rhinitis |
| NCT02213367 | PHASE3 | COMPLETED | Bilastine Updosing in Chronic Spontaneous Urticaria |
| NCT04810390 | PHASE3 | COMPLETED | Study to Assess the Safety, Tolerability and Efficacy of Bilastine Ophthalmic Solution 0.6% in Children |
| NCT00420082 | PHASE2 | COMPLETED | A Randomized, Double-Blind, 4-way Crossover Study to Evaluate the Efficacy of Bilastine in the Vienna Challenge Chamber |
| NCT00574210 | PHASE2 | COMPLETED | PK/PD and Steady State Efficacy Study of Bilastine Compared With Placebo Given Orally in the Treatment of the Symptoms of SAR in an EEC Model (5-arm) |
| NCT00574379 | PHASE2 | COMPLETED | Efficacy, Safety and PK of Once or Twice Daily Bilastine (10 or 20 mg) Compared With Placebo in the Symptomatic Treatment of SAR |
| NCT01081574 | PHASE1/PHASE2 | COMPLETED | Pharmacokinetic Study of Bilastine in Children From 2 to < 12 Years of Age With Either Allergic Rhinoconjunctivitis (AR) or Chronic Urticaria (CU) |
| NCT03231969 | PHASE2 | COMPLETED | A Single-Center, Phase 2 Study Evaluating Bilastine Ophthalmic Solution in the CAC® Model |
| NCT00419783 | PHASE1 | COMPLETED | A Randomized, Multiple Dose, Double Blind, 5-way Crossover Study of the Electrocardiographic (ECG) Effects of Bilastine |
| NCT01124123 | PHASE1 | COMPLETED | Oral Bioavailability of Bilastine |
| NCT07042828 | PHASE1 | COMPLETED | To Compare and Evaluate the Oral Bioavailability of Bilastine 20 mg Orally Dispersible Tablet With That of Bilaxten (Bilastine) 20 mg Orally Dispersible Tablet in Healthy, Adult, Human Subjects Under Fasting Conditions |
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.
296 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: eye allergy, allergic disease
- In clinical trials for: seasonal allergic rhinitis, urticaria, perennial allergic rhinitis, atopic conjunctivitis, cold urticaria
- 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