Proparacaine

Summary

Proparacaine (CHEMBL1196) is an approved small molecule (ATC S01HA04); indicated across 1 condition.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: S01HA04
• Indications: 1 condition
• Clinical trials: 16
• Chemistry: 294.39 Da · C16H26N2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1196
Name	Proparacaine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4935
ATC	S01HA04
Molecular formula	C16H26N2O3
Molecular weight	294.39
InChIKey	KCLANYCVBBTKTO-UHFFFAOYSA-N

SMILES: CCCOC1=C(C=C(C=C1)C(=O)OCCN(CC)CC)N

IUPAC name: 2-(diethylamino)ethyl 3-amino-4-propoxybenzoate

Also known as: Proparacaine, Proximetacaina, Proxymetacaine, SID11112907, proparacaine, SID124882712, SID174006303, PROPARACAINE, PROXYMETACAINE, Proparacaine HCl

Parent form; salt/anhydrous children: CHEMBL1200464

Patent coverage: 3,498 distinct patent families (12,973 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 12,963 (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: 11 (assay-derived). Sample: Amine oxidase [flavin-containing] A, Sodium channel alpha subunits; brain (Types I, II, III), Voltage-gated inwardly rectifying potassium channel KCNH2, Histamine H3 receptor, Sigma non-opioid intracellular receptor 1, Cytochrome P450 2D6, Cytochrome P450 1A2, Cytochrome P450 3A4, Cytochrome P450 2C19, Prostaglandin G/H synthase 1.

Bioactivity

ChEMBL activities: 15 potent at pChembl ≥ 5 of 16 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SIGMAR1	7	Ki	100	nM	CHEMBL_ACT_7737155
SIGMAR1	6.62	IC50	238	nM	CHEMBL_ACT_7737154
Q63921	6.12	AC50	750	nM	CHEMBL_ACT_25174585
CYP3A4	5.9	Potency	1259	nM	CHEMBL_ACT_5001968
CYP3A4	5.9	Potency	1259	nM	CHEMBL_ACT_5070538
CYP3A4	5.9	AC50	1259	nM	CHEMBL_ACT_6009613
HRH3	5.89	AC50	1300	nM	CHEMBL_ACT_25200743
MAOA	5.75	IC50	1777	nM	CHEMBL_ACT_7735048
SCN1A	5.72	IC50	1900	nM	CHEMBL_ACT_382326
P15917	5.5	Potency	3162	nM	CHEMBL_ACT_4633713
CYP2C19	5.4	Potency	3981	nM	CHEMBL_ACT_4015254
CYP1A2	5.3	AC50	5012	nM	CHEMBL_ACT_6016063
CYP2D6	5.2	Potency	6310	nM	CHEMBL_ACT_4974084
CYP2D6	5.2	AC50	6310	nM	CHEMBL_ACT_6041716
KCNH2	5.19	AC50	6400	nM	CHEMBL_ACT_25118141

Target pathways

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

Indications & clinical

Indications

1 indication (0 at ChEMBL trial phase 4).

The 1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 16.

Phase distribution

Phase	Trials
Not specified	9
PHASE4	5
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05663684	PHASE4	RECRUITING	Does Topical Ophthalmic Proparacaine 0.5% Prior to Probing and Irrigation Decrease Pain?
NCT07456826	PHASE4	ENROLLING_BY_INVITATION	Study Evaluating the Efficacy and Safety of Chloroprocaine HCl Ophthalmic Gel 3% vs Proparacaine Ophthalmic Solution 0.5% Plus Subconjunctival Lidocaine in Patients Undergoing Intravitreal Injections
NCT04229771	PHASE4	TERMINATED	Does Topical Ophthalmic Anesthetic Prior to Probing and Irrigation Decrease Pain?
NCT04283331	PHASE4	UNKNOWN	Anesthetic Impregnated Bandage Soft Contact Lens (BSCL) in Pain Management After Photorefractive Keratectomy (PRK)
NCT06636708	PHASE4	COMPLETED	Efficacy of Nanodropper-mediated Topical Anesthetic
NCT01027611	PHASE3	COMPLETED	Patient Assessment of Topical Anesthetic Effectiveness for Intravitreal Injections
NCT05325853	PHASE3	COMPLETED	A Study of Safety and the Local Anesthetic Effect of AG-920 Ophthalmic Solution in a Pediatric Population
NCT00769392	Not specified	COMPLETED	Pilot Study: A Randomized Trial Of Anesthetic Agents For Intravitreal Injection
NCT01266824	Not specified	TERMINATED	Proparacaine and Mydriatic Eye Drops
NCT01640171	Not specified	COMPLETED	Anesthesia Preference for Intravitreal Injection: Topical or Subconjunctival
NCT02528123	Not specified	COMPLETED	VisuMax Femtosecond Laser Small Incision Lenticule Extraction for the Correction of High Myopia
NCT02609997	Not specified	COMPLETED	Comparison of In-the-bag Stability Between Single-piece and Three-piece Intraocular Lens
NCT02613013	Not specified	UNKNOWN	Laser Peripheral Iridotomy Plus Laser Peripheral Iridoplasty for Primary Angle Closure
NCT02925832	Not specified	COMPLETED	Comparing Ropivacaine and Bupivacaine in DTFNB Anesthesia in Patients Undergoing Phacoemulsification
NCT02951351	Not specified	COMPLETED	Topical Proparacaine Eye Drops to Improve the Experience of Patients Undergoing Intravitreal Injections
NCT02973581	Not specified	COMPLETED	SPI-directed Analgesia for Vitreoretinal Surgeries

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).