Olopatadine
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Also known as AL-4943AOlopatadinaOpatanolOlopatadine hydrochlorideÊOlopatadine hydrochlorideÂOlopatadine hydrochloride (Opatanol)
Summary
Olopatadine (CHEMBL1189432) is an approved small molecule (ATC R01AC08); indicated across 6 conditions including eye allergy and atopic conjunctivitis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R01AC08 (+1 more)
- Indications: 6 conditions
- Clinical trials: 49
- Chemistry: 337.4 Da · C21H23NO3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1189432 |
| Name | Olopatadine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 5281071 |
| ATC | R01AC08, S01GX09 |
| Molecular formula | C21H23NO3 |
| Molecular weight | 337.4 |
| InChIKey | JBIMVDZLSHOPLA-LSCVHKIXSA-N |
SMILES: CN(C)CC/C=C\1/C2=CC=CC=C2COC3=C1C=C(C=C3)CC(=O)O
IUPAC name: 2-[(11Z)-11-[3-(dimethylamino)propylidene]-6H-benzo[c][1]benzoxepin-2-yl]acetic acid
Also known as: AL-4943A, Olopatadina, Olopatadine, Opatanol, olopatadine, OLOPATADINE, Olopatadine hydrochlorideÊ, Olopatadine hydrochlorideÂ, Olopatadine hydrochloride (Opatanol)
Parent form; salt/anhydrous children: CHEMBL1719
Patent coverage: 2,590 distinct patent families (9,682 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 9,580 (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
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Histamine H1 receptor.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HRH1 | 8.5 | Kd | 3.16 | nM | CHEMBL_ACT_29118595 |
| HRH1 | 8.3 | Ki | 5.01 | nM | CHEMBL_ACT_29118529 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
6 indications (2 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 |
| atopic conjunctivitis | 3 | MONDO:0005642 | EFO:0007141 |
| 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: 49.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 23 |
| PHASE3 | 16 |
| PHASE2 | 5 |
| Not specified | 3 |
| PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00655109 | PHASE4 | COMPLETED | A Comparison of Olopatadine and Fluticasone in Patients With Allergic Conjunctivitis |
| NCT00691665 | PHASE4 | COMPLETED | Comparison of Olopatadine 0.6% and Fluticasone Proprionate 50mcg Nasal Sprays in a Two Week Seasonal Allergic Rhinitis Trial |
| NCT00772304 | PHASE4 | COMPLETED | Evaluation of the Sensory Attributes of Olopatadine 0.6% and Azelastine 137mcg Nasal Sprays in Patients w/Allergic Rhinitis |
| NCT00789555 | PHASE4 | COMPLETED | Safety of PATANASE Nasal Spray in Patients With Perennial Allergic Rhinitis |
| NCT00818805 | PHASE4 | COMPLETED | Efficacy Investigation Study of Olopatadine Hydrochloride Ophthalmic Solution Using OHIO Chamber in Patients With Seasonal Allergic Rhinitis (SAR) |
| NCT00845195 | PHASE4 | COMPLETED | Comparison of Seasonal Allergic Rhinitis Treatment With 2 Antihistamines Used in Combination With Intranasal Corticosteroid |
| NCT00979615 | PHASE4 | COMPLETED | Safety and Efficacy of Olopatadine 0.6% and Azelastine 137 Mcg in Vasomotor Rhinitis |
| NCT01007253 | PHASE4 | COMPLETED | Effect of Veramyst and Olopatadine 0.2% Opthalmic Solution on Allergy Symptoms |
| NCT01109485 | PHASE4 | COMPLETED | Clinical Evaluation of 0.1% Olopatadine Hydrochloride Ophthalmic Solution in Pediatric Patients |
| NCT01119287 | PHASE4 | COMPLETED | Assessing the Efficacy of Maxidex® and Patanol® for the Treatment of Allergic Conjunctivitis |
| NCT01159769 | PHASE4 | COMPLETED | Patient Perceptions and Quality of Life Associated With the Use of Olapatadine 0.2% for the Treatment of Allergic Conjunctivitis |
| NCT01272089 | PHASE4 | COMPLETED | A Study of Patient Perception and Quality of Life Associated With the Use of Olopatadine 0.2% in Subjects With Allergic Conjunctivitis |
| NCT01282138 | PHASE4 | COMPLETED | Assessment of Alcon’s Ocular Image Quantification System |
| NCT01294969 | PHASE4 | COMPLETED | Patient Perception Study for AL-4943A |
| NCT01470118 | PHASE4 | COMPLETED | A Study to Evaluate the Duration of LASTACAFT® in Acute Allergic Conjunctivitis |
| NCT01697969 | PHASE4 | COMPLETED | Confocal Analysis of Corneal Structures of Symptomatic Allergic Conjunctivitis Patients |
| NCT01732757 | PHASE4 | COMPLETED | A Study to Evaluate the Efficacy of Lastacaft® Compared to Pataday™ and Placebo in Patients With Acute Allergic Conjunctivitis |
| NCT02251613 | PHASE4 | COMPLETED | Effectiveness of Olopatadine HCl Ophthalmic Solution for the Treatment of Allergic Conjunctivitis in Japan |
| NCT03186755 | PHASE4 | UNKNOWN | Clinical Evaluation of Hylo-Dual Versus Patanol in Children With Seasonal Allergic Conjunctivitis |
| NCT04708821 | PHASE4 | COMPLETED | DEXTENZA Therapy for Treatment of Allergic Conjunctivitis |
| NCT04776096 | PHASE4 | COMPLETED | Efficacy and Toxicity of Bepotastine 1,5% PF vs Olopatadine 0,2% With BAK on Allergic Conjunctivitis Treatment |
| NCT05265910 | PHASE4 | COMPLETED | A Study Comparing the Efficacy of Pataday® Once Daily Relief Extra Strength to Claritin® Tablets 24-Hour in Subjects With Allergic Conjunctivitis |
| NCT05314621 | PHASE4 | COMPLETED | A Study Comparing the Efficacy of Pataday® Once Daily Relief Extra Strength to Flonase® Allergy Relief in Subjects With Allergic Conjunctivitis |
| NCT00331500 | PHASE3 | COMPLETED | Olopatadine 0.2% for the Treatment of Allergic Conjunctivitis |
| NCT00550550 | PHASE3 | COMPLETED | Efficacy and Safety of Grass Sublingual Tablet in Children and Adolescents (P05239 AM3)(COMPLETED) |
| NCT00562159 | PHASE3 | COMPLETED | Efficacy and Safety of Grass Sublingual Tablet in Adults (P05238 AM3)(COMPLETED) |
| NCT00578331 | PHASE3 | COMPLETED | Safety Study of Olopatadine Nasal Spray |
| NCT00578929 | PHASE3 | COMPLETED | Safety and Efficacy of Olopatadine HCl Nasal Spray in 6-11 Year Old Patients |
| NCT00987272 | PHASE3 | COMPLETED | Study of Olopatadine HCl Ophthalmic Solutions Compared to Vehicle Using the Conjunctival Allergen Challenge (CAC) Model of Acute Allergic Conjunctivitis in Japanese Subjects |
| NCT01037179 | PHASE3 | COMPLETED | An Open-Label, Long-Term Study With AL-4943A Ophthalmic Solution, 0.2% in Patients With Allergic Conjunctivitis |
| NCT01258309 | PHASE3 | COMPLETED | Safety and Efficacy of Olopatadine Hydrochloride/Ketorolac Tromethamine Ophthalmic Solution Compared With Olopatadine Hydrochloride Ophthalmic Solution in Patients With Seasonal Allergic Conjunctivitis |
| NCT01363700 | PHASE3 | COMPLETED | Study of DE-114 Ophthalmic Solution in Patients With Allergic Conjunctivitis |
| NCT01435460 | PHASE3 | COMPLETED | Alrex® Versus Patanol in the Treatment of Seasonal Allergic Conjunctivitis(SAC) |
| NCT01479374 | PHASE3 | COMPLETED | Efficacy and Safety of AL-4943A Ophthalmic Solution in Patients With Allergic Conjunctivitis Using the Conjunctival Allergen Challenge (CAC) Model |
| NCT01743027 | PHASE3 | COMPLETED | Efficacy and Safety of an Ophthalmic Solution in Patients With Allergic Conjunctivitis |
| NCT02161146 | PHASE3 | COMPLETED | AGN-229666 Ophthalmic Solution in Japanese Patients With Allergic Conjunctivitis |
| NCT02322216 | PHASE3 | COMPLETED | Olopatadine Hydrochloride Ophthalmic Solution Study in Chinese Subjects |
| NCT02478398 | PHASE3 | COMPLETED | Efficacy and Safety Study of RAGWITEK™ (MK-3641) in Children With Ragweed-Induced Rhinoconjunctivitis With or Without Asthma (MK-3641-008) |
| NCT02631551 | PHASE3 | COMPLETED | Efficacy and Safety of Fixed Dose Combination GSP 301 Nasal Spray (NS) in the Treatment of Seasonal Allergic Rhinitis (SAR) |
| NCT00794144 | PHASE2 | COMPLETED | Safety and Pharmacokinetics of Patanase in Pediatric Patients 2 to < 6 Years of Age |
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
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).