Benzonatate

Summary

Benzonatate (CHEMBL1374379) is an approved small-molecule anaesthetic (ATC R05DB01); indicated across 1 condition.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R05DB01
• Indications: 1 condition
• Clinical trials: 2
• Chemistry: 603.7 Da · C30H53NO11

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1374379
Name	Benzonatate
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	7699
ChEBI	CHEBI:3032
ATC	R05DB01
Molecular formula	C30H53NO11
Molecular weight	603.7
InChIKey	MAFMQEKGGFWBAB-UHFFFAOYSA-N

SMILES: CCCCNC1=CC=C(C=C1)C(=O)OCCOCCOCCOCCOCCOCCOCCOCCOCCOC

IUPAC name: 2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl 4-(butylamino)benzoate

ChEBI definition: The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant.

Pharmacological roles (ChEBI): antitussive, anaesthetic.

Also known as: Benzonatate, Benzonatato, NSC-760128, Tessalon, Tessalon perles, SID11112254, SID56463355, BENZONATATE, benzonatate, SID144203949, SID170465391

Patent coverage: 1,268 distinct patent families (5,244 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: 7 (assay-derived). Sample: Alpha-2B adrenergic receptor, Sodium channel protein type 5 subunit alpha, Beta-lactamase, Delta-type opioid receptor, Cytochrome P450 3A4, Cruzipain, Bile salt export pump.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SCN5A	5.8	AC50	1600	nM	CHEMBL_ACT_25158827
CYP3A4	5.2	Potency	6310	nM	CHEMBL_ACT_5006092
CYP3A4	5.2	Potency	6310	nM	CHEMBL_ACT_5074556
CYP3A4	5.2	AC50	6310	nM	CHEMBL_ACT_6036436
P25779	5.1	Potency	7943	nM	CHEMBL_ACT_3978365
ADRA2B	5.05	AC50	9000	nM	CHEMBL_ACT_25143308
P00811	5.05	Potency	8912	nM	CHEMBL_ACT_4658928

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: 2.

Phase distribution

Phase	Trials
PHASE3	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03722914	PHASE3	UNKNOWN	A Study on the Efficacy and Safety of Benzonatate Soft Capsules for Improving Adult Cough Symptoms
NCT02207699	PHASE1	COMPLETED	Evaluation of the Effect of Benzonatate on QT Intervals Following Single Dose Administration of Benzonatate to Healthy Volunteers

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).