Benoxinate
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Also known as ConjucainDorsacainMonofree oxybuprocaineOxibuprocainaOxybucaineOxybuprocaineSID11112575SID56320722BENOXINATE HYDROCHLORIDE
Summary
Benoxinate (CHEMBL1200) is an approved small-molecule local anaesthetic (ATC D04AB03); indicated across 1 condition.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: D04AB03 (+1 more)
- Indications: 1 condition
- Clinical trials: 7
- Chemistry: 308.4 Da · C17H28N2O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1200 |
| Name | Benoxinate |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 4633 |
| ChEBI | CHEBI:309594 |
| ATC | D04AB03, S01HA02 |
| Molecular formula | C17H28N2O3 |
| Molecular weight | 308.4 |
| InChIKey | CMHHMUWAYWTMGS-UHFFFAOYSA-N |
SMILES: CCCCOC1=C(C=CC(=C1)C(=O)OCCN(CC)CC)N
IUPAC name: 2-(diethylamino)ethyl 4-amino-3-butoxybenzoate
ChEBI definition: A benzoate ester in which 4-amino-3-butoxybenzoic acid and 2-(diethylamino)ethanol have combined to form the ester bond; an ester-based local anaesthetic (ester “caine”) used especially in ophthalmology and otolaryngology.
Pharmacological roles (ChEBI): local anaesthetic, topical anaesthetic, drug allergen.
Also known as: Conjucain, Dorsacain, Monofree oxybuprocaine, Oxibuprocaina, Oxybucaine, Oxybuprocaine, SID11112575, SID56320722, Benoxinate, BENOXINATE, OXYBUPROCAINE, BENOXINATE HYDROCHLORIDE
Parent form; salt/anhydrous children: CHEMBL1200654
Patent coverage: 1,996 distinct patent families (6,712 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 6,711 (100%) 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: 12 (assay-derived). Sample: 4’-phosphopantetheinyl transferase ffp, Thyrotropin receptor, Sodium channel alpha subunits; brain (Types I, II, III), Sodium-dependent noradrenaline transporter, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2, Histamine H3 receptor, Cytochrome P450 2D6, Cytochrome P450 1A2, Prostaglandin G/H synthase 1.
Bioactivity
ChEMBL activities: 11 potent at pChembl ≥ 5 of 15 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P15917 | 6.8 | Potency | 158.5 | nM | CHEMBL_ACT_4635120 |
| CYP1A2 | 6.4 | AC50 | 398.1 | nM | CHEMBL_ACT_6047208 |
| Q63921 | 5.85 | AC50 | 1400 | nM | CHEMBL_ACT_25174961 |
| SCN1A | 5.54 | IC50 | 2900 | nM | CHEMBL_ACT_345626 |
| HRH3 | 5.25 | AC50 | 5600 | nM | CHEMBL_ACT_25201054 |
| CYP2D6 | 5.2 | Potency | 6310 | nM | CHEMBL_ACT_4949877 |
| CYP2D6 | 5.2 | AC50 | 6310 | nM | CHEMBL_ACT_6006666 |
| SLC6A3 | 5.09 | AC50 | 8200 | nM | CHEMBL_ACT_25124525 |
| SLC6A2 | 5.08 | AC50 | 8400 | nM | CHEMBL_ACT_25145569 |
| HIF1A | 5 | Potency | 10000 | nM | CHEMBL_ACT_4129033 |
| HIF1A | 5 | Potency | 10000 | nM | CHEMBL_ACT_4520855 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
1 indication (1 at ChEMBL trial phase 4).
The 1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.
Clinical trials
Total trials: 7.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 3 |
| Not specified | 2 |
| PHASE4 | 1 |
| PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05666362 | PHASE4 | COMPLETED | Hemodynamic Response to Pain During Retinopathy Of Prematurity Screening |
| NCT05926258 | PHASE3 | COMPLETED | Efficacy and Safety of Chloroprocaine 3% Gel and Oxybuprocaine 0.4% Eye Drops Anesthesia in Pediatric Population |
| NCT06461975 | PHASE3 | COMPLETED | Effect of Benoxinate Hydrochloride Eye Drops on The Premature Infant Pain Profile Score During Retinopathy of Prematurity Screening |
| NCT07230548 | PHASE3 | COMPLETED | Effect of Four Different Diagnostic Eye Drops on Tear Film Thickness |
| NCT03933280 | PHASE2 | COMPLETED | Conscious Sedation for Cataract Operations Under Topical Anaesthesia |
| NCT02528123 | Not specified | COMPLETED | VisuMax Femtosecond Laser Small Incision Lenticule Extraction for the Correction of High Myopia |
| NCT04193774 | Not specified | COMPLETED | Optimization of Sampling and Processing of Samples for Molecular Microbial Research on Ocular Surface Samples |
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).
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.