Bepotastine
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Also known as BepotastinaBetotastineBepotastine Besilate
Summary
Bepotastine (CHEMBL1201758) is an approved small-molecule H1-receptor antagonist; indicated across 4 conditions including atopic conjunctivitis and perennial allergic rhinitis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- Indications: 4 conditions
- Clinical trials: 10
- Chemistry: 388.9 Da · C21H25ClN2O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1201758 |
| Name | Bepotastine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 164522 |
| ChEBI | CHEBI:71204 |
| Molecular formula | C21H25ClN2O3 |
| Molecular weight | 388.9 |
| InChIKey | YWGDOWXRIALTES-NRFANRHFSA-N |
SMILES: C1CN(CCC1O[C@@H](C2=CC=C(C=C2)Cl)C3=CC=CC=N3)CCCC(=O)O
IUPAC name: 4-[4-[(S)-(4-chlorophenyl)-pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid
ChEBI definition: An ether that is (S)-(4-chlorophenyl)(pyridin-2-yl)methanol in which the hydroxyl hydrogen is substituted by a 1-(3-carboxypropyl)piperidin-4-yl group. A topical, selective and non-sedating histamine (H1) receptor antagonist used (as its benzenesulfonate salt) for treatment of itching associated with allergic conjunctivitis.
Pharmacological roles (ChEBI): H1-receptor antagonist, anti-allergic agent.
Also known as: Bepotastina, Bepotastine, Betotastine, BEPOTASTINE, Bepotastine Besilate, bepotastine
Parent form; salt/anhydrous children: CHEMBL1201759
Patent coverage: 828 distinct patent families (2,911 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,885 (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
No target linkage available.
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
4 indications (0 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 |
|---|---|---|---|
| atopic conjunctivitis | 3 | MONDO:0005642 | EFO:0007141 |
| perennial allergic rhinitis | 3 | MONDO:0024332 | EFO:1001417 |
| dermatitis | 3 | MONDO:0002406 | MONDO:0002406 |
| seasonal allergic rhinitis | 2 | MONDO:0005324 | EFO:0003956 |
Clinical trials
Total trials: 10.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 4 |
| PHASE3 | 3 |
| PHASE2/PHASE3 | 1 |
| PHASE2 | 1 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01337557 | PHASE4 | UNKNOWN | Use of BEPREVE (Bepotastine Besilate Ophthalmic Solution) 1.5% for Allergic Conjunctivitis and Contact Lenses |
| NCT01443442 | PHASE4 | COMPLETED | Bepreve vs. Alrex in Subjects With Moderate to Severe Allergic Conjunctivitis |
| NCT04776096 | PHASE4 | COMPLETED | Efficacy and Toxicity of Bepotastine 1,5% PF vs Olopatadine 0,2% With BAK on Allergic Conjunctivitis Treatment |
| NCT04877678 | PHASE4 | COMPLETED | Effects of Second-generation Antihistamine Bepotastine on Cough Outcomes in Cough Patients With Allergic Rhinitis |
| NCT00424398 | PHASE2/PHASE3 | COMPLETED | Evaluation of the Onset and Duration of Action of Bepotastine Besilate Ophthalmic Solution in Acute Allergic Conjunctivitis |
| NCT01840605 | PHASE3 | COMPLETED | A Confirmatory Study of TAU-284 in Pediatric Patients With Atopic Dermatitis |
| NCT01861522 | PHASE3 | COMPLETED | The Confirmatory Study of TAU-284 in Pediatric Patients With Perennial Allergic Rhinitis |
| NCT01900054 | PHASE3 | COMPLETED | A Long-Term Study of TAU-284 in Pediatric Patients With Perennial Allergic Rhinitis |
| NCT01753739 | PHASE2 | COMPLETED | Bepotastine Besilate Nasal Sprays in the Treatment of Seasonal Allergic Rhinitis (SAR) |
| NCT04693429 | PHASE1 | COMPLETED | Clinical Study for the Evaluation of Safety and Tolerability of PRO-172 Ophthalmic Solution+ |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).