Benzocaine

Summary

Benzocaine (CHEMBL278172) is an approved small-molecule topical anaesthetic (ATC D04AB04); indicated across 15 conditions including hemorrhoid and pharyngitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: D04AB04 (+3 more)
• Indications: 15 conditions
• Clinical trials: 21
• Chemistry: 165.19 Da · C9H11NO2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL278172
Name	Benzocaine
Type	Small molecule
Max phase	3
FDA approved	yes
PubChem CID	2337
ChEBI	CHEBI:116735
ATC	D04AB04, C05AD03, N01BA05, R02AD01
Molecular formula	C9H11NO2
Molecular weight	165.19
InChIKey	BLFLLBZGZJTVJG-UHFFFAOYSA-N

SMILES: CCOC(=O)C1=CC=C(C=C1)N

IUPAC name: ethyl 4-aminobenzoate

ChEBI definition: A benzoate ester having 4-aminobenzoic acid as the acid component and ethanol as the alcohol component. A surface anaesthetic, it is used to suppress the gag reflex, and as a lubricant and topical anaesthetic on the larynx, mouth, nasal cavity, respiratory tract, oesophagus, rectum, urinary tract, and vagina.

Pharmacological roles (ChEBI): topical anaesthetic, antipruritic drug, allergen, sensitiser.

Also known as: Aezodent, Americaine, Anaesthesin, Anthisan plus, AR-01, AR01, Baby anbesol, Benzocaina, Benzocaine, Benzocainum, Burneze, Children’s chloraseptic

Patent coverage: 14,115 distinct patent families (43,282 SureChEMBL compound mentions), from 1 matched compound structure(s). 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: 5 (assay-derived). Sample: Nuclear receptor ROR-gamma, Prelamin-A/C, Amine oxidase [flavin-containing] A, Cytochrome P450 1A2, Cytochrome P450 3A4.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 9 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CYP1A2	5.7	AC50	1995	nM	CHEMBL_ACT_6047195
P51450	5.15	Potency	7080	nM	CHEMBL_ACT_4789986
LMNA	5.1	Potency	7943	nM	CHEMBL_ACT_3623847

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

5 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
hemorrhoid	4	MONDO:0004872	EFO:0009552
pharyngitis	4	MONDO:0002258	MONDO:0002258
sunburn	4	MONDO:0005326	EFO:0003958
burn	4	MONDO:0043519	EFO:0009516
premature ejaculation	4	MONDO:0001780	EFO:0803321

3 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
otitis media	3	MONDO:0005441	MONDO:0024330
asthma	2	MONDO:0004979	MONDO:0004979
obesity disorder	1	MONDO:0011122	EFO:0001073

7 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 21.

Phase distribution

Phase	Trials
PHASE4	7
PHASE3	6
PHASE2	3
Not specified	3
PHASE1/PHASE2	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00474175	PHASE4	COMPLETED	Benzocaine Gel Toothache Dose-Response Study
NCT00716443	PHASE4	TERMINATED	Evaluate Efficacy, Safety & Subject Satisfaction of Pain Management With Pliaglis® Cream for Dermal Filler Injections
NCT00846690	PHASE4	UNKNOWN	Comparative Efficacy of 20% Benzocaine Versus TAC Alternate Gel
NCT01925469	PHASE4	COMPLETED	Benzocaine Versus Placebo Spray for Pain Relief at Hysterosalpingogram
NCT01951820	PHASE4	COMPLETED	Comparison of Two Topical Anesthetics: Benzocaine Versus Pliaglis
NCT06165432	PHASE4	COMPLETED	Pre Injection Use of Cryoanesthesia Versus Topical Anesthetic Gel in Reducing Pain Perception During Palatal Injections
NCT06951191	PHASE4	TERMINATED	Intrauterine Device Insertion Pain Management
NCT00148499	PHASE3	COMPLETED	Efficacy and Tolerability of Ambroxol Lozenge 20 mf in Relieving Pain of Sore Throat in Pat. With Acute/Viralpharyngitis
NCT01429701	PHASE3	COMPLETED	Effectiveness of Polymyxin B Sulphate + Prednisolone + Benzocaine + Clioquinol in Acute and Sub-acute Dermatitis Eczematous
NCT02044341	PHASE3	COMPLETED	Phase 3 Study to Compare the Efficacy and Safety of AR01 to a Placebo Solution for Relief of Pain in Acute Otitis Media
NCT02074007	PHASE3	TERMINATED	Study to Compare Efficacy and Safety of AR01 to a Placebo Solution for Relief of Pain in Acute Otitis Media (AR01007)
NCT03432923	PHASE3	COMPLETED	A Study to Determine the Efficacy and Safety of a Benzocaine Lozenge for Treatment of Sore Throat.
NCT07242157	PHASE3	COMPLETED	Effects of Topical Lidocaine and Benzocaine on Pain Level and Injection Satisfaction
NCT01274247	PHASE1/PHASE2	TERMINATED	Use of Topical Benzocaine for Analgesia in Lingual Frenotomy of the Newborn
NCT01588535	PHASE2	COMPLETED	Study of FAECC Scale (Modified FLACC) to Evaluate Ear Pain in Children With Acute Otitis Media
NCT02092454	PHASE2	COMPLETED	Study to Assess the Safety and Efficacy of Benzocaine for Pain Relief in Children Presenting With Acute Otitis Media
NCT03790540	PHASE2	COMPLETED	Pain Assessment During Mandibular Nerve Block Injection With the Aid of Dental Vibe Tool in Pediatric Dental Patients
NCT02537314	PHASE1	COMPLETED	Role of the Foregut in Nutrient Metabolism in Lean and Obese Humans
NCT06691269	Not specified	RECRUITING	Photobiomodulation and Tooth Analgesia
NCT07558720	Not specified	ACTIVE_NOT_RECRUITING	Effect of Diode Laser and 20% Benzocaine Anesthetic Gel on Pain Reduction Following Tooth Separation With Elastomeric Separators in Fixed Orthodontic Patients: A Randomized Trial in Karachi-Pakistan
NCT02726620	Not specified	COMPLETED	Decision Support for Intraoperative Low Blood Pressure

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).