Chloroprocaine

Summary

Chloroprocaine (CHEMBL1179047) is an approved small-molecule local anaesthetic (ATC S01HA08); indicated across 3 conditions including cataract.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: S01HA08 (+1 more)
• Indications: 3 conditions
• Clinical trials: 29
• Chemistry: 270.75 Da · C13H19ClN2O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1179047
Name	Chloroprocaine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	8612
ChEBI	CHEBI:3636
ATC	S01HA08, N01BA04
Molecular formula	C13H19ClN2O2
Molecular weight	270.75
InChIKey	VDANGULDQQJODZ-UHFFFAOYSA-N

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

IUPAC name: 2-(diethylamino)ethyl 4-amino-2-chlorobenzoate

ChEBI definition: Procaine in which one of the hydrogens ortho- to the carboxylic acid group is substituted by chlorine. It is used as its monohydrochloride salt as a local anaesthetic, particularly for oral surgery. It has the advantage over lidocaine of constricting blood vessels, so reducing bleeding.

Pharmacological roles (ChEBI): local anaesthetic, peripheral nervous system drug, central nervous system depressant.

Also known as: Chloroprocaine, Cloroprocaina, CHLOROPROCAINE, Chloroprocaine hydrochlorideÊ, Chloroprocaine hydrochlorideÂ, chloroprocaine

Parent form; salt/anhydrous children: CHEMBL944

Patent coverage: 13,747 distinct patent families (52,577 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 52,310 (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: 8 (assay-derived). Sample: Neuronal acetylcholine receptor subunit alpha-4, 5-hydroxytryptamine receptor 3A, Amine oxidase [flavin-containing] A, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 2C, Voltage-gated inwardly rectifying potassium channel KCNH2, Muscarinic acetylcholine receptor M3, Histamine H3 receptor.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HRH3	5.4	AC50	4000	nM	CHEMBL_ACT_25201142
MAOA	5.1	AC50	7900	nM	CHEMBL_ACT_25160363

Target pathways

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

Indications & clinical

Indications

3 indications (0 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
cataract	3	MONDO:0005129	MONDO:0005129

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

Clinical trials

Total trials: 29.

Phase distribution

Phase	Trials
PHASE4	11
Not specified	9
PHASE3	5
PHASE2	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06472232	PHASE4	NOT_YET_RECRUITING	Multicenter Study of Chloroprocaine Versus Ropivacaine for Epidural Labor Analgesia
NCT07239999	PHASE4	NOT_YET_RECRUITING	Comparing Spinal Anesthesia With 1% Chloroprocaine Versus 1% Mepivacaine in Patients Undergoing Outpatient Primary Total Knee Arthroplasty
NCT07348614	PHASE4	NOT_YET_RECRUITING	Flex Appeal: Evaluating the Efficacy of Anesthetic Techniques for Manipulation of Knees Under Anesthesia
NCT07444827	PHASE4	NOT_YET_RECRUITING	Targeted Nerve Injection to the Knee (Nerve to Vastus Medialis): Comparing Two Adductor Canal Block Approaches
NCT02049255	PHASE4	COMPLETED	Comparision of the Use in Marcaine and Chloroprocaine in Rachianesthesia for the Surgical Correction of Inguinal Hernia.
NCT02287870	PHASE4	COMPLETED	Epidural Anesthesia With Chloroprocaine Versus Lidocaine
NCT02862912	PHASE4	COMPLETED	Chloroprocaine Spinal Anesthesia for Cervical Cerclage (CP Spinal)
NCT03038958	PHASE4	COMPLETED	Comparison of Hyperbaric Prilocaine With Chloroprocaine for Intrathecal Anaesthesia in Day Case Knee Arthroscopy
NCT03305575	PHASE4	COMPLETED	Intrathecal Chloroprocaine vs. Bupivacaine for Cervical Cerclage
NCT03805438	PHASE4	COMPLETED	ED90 of 3% Chloroprocaine for Cervical Cerclage
NCT03805503	PHASE4	COMPLETED	Chloroprocaine for Inguinal Herniorrhaphy
NCT02385097	PHASE3	COMPLETED	Chloroprocaine 2% vs Ropivacaine 0.75% in Ultrasound-guided Axillary Nerve Block
NCT02919072	PHASE3	TERMINATED	Chloroprocaine 3% - Epidural Anesthesia in Unplanned Caesarean Section
NCT03260972	PHASE3	WITHDRAWN	Intraabdominal Chloroprocaine During Cesarean Delivery for Pain Control
NCT04685538	PHASE3	COMPLETED	Chloroprocaine 3% Gel Eye Drop as Topical Anestheticsin Phacoemulsification.
NCT05926258	PHASE3	COMPLETED	Efficacy and Safety of Chloroprocaine 3% Gel and Oxybuprocaine 0.4% Eye Drops Anesthesia in Pediatric Population
NCT02481505	PHASE2	COMPLETED	Spinal Anaesthesia With Chloroprocaine HCl 1% for Elective Lower Limb Procedures of Short Duration.
NCT03365752	PHASE2	TERMINATED	Chloroprocaine Spinal for Outpatient Knee Surgery
NCT03918798	PHASE2	COMPLETED	The Efficacy and Safety of Chloroprocaine 1% and 2% in Pediatric Population
NCT03993314	PHASE2	TERMINATED	Optimizing Anesthesia for Post Partum Tubal Ligations
NCT06376058	Not specified	RECRUITING	Chloroprocaine 1% Versus Ropivacaine 0,75% During Cesarean Section
NCT00845962	Not specified	COMPLETED	A Comparison of Bupivacaine and 2-chloroprocaine for Spinal Anesthesia
NCT02067806	Not specified	COMPLETED	Observational Study on 2-chloroprocaine Hydrochloride 1%
NCT02207855	Not specified	COMPLETED	Chloroprocaine for Continuous Epidural Analgesia in Neonates and Infants
NCT02406703	Not specified	COMPLETED	The Impact of Chloroprocaine 3% for Ambulatory Foot Surgery on Perioperative Process Costs
NCT02726620	Not specified	COMPLETED	Decision Support for Intraoperative Low Blood Pressure
NCT02813382	Not specified	COMPLETED	Spinal Anesthesia for Outpatient Abdominal Wall Surgery: Comparison of Bupivacaine, 2-chloroprocaine and Prilocaine
NCT03882489	Not specified	COMPLETED	Estimation of Effective Dose 95 (ED95) of Intrathecal Isobaric 2-chloroprocaine (2-CP) Based on the Height (cm) of a Patient Undergoing Ambulatory Knee Arthroscopy
NCT05365074	Not specified	COMPLETED	Intrathecal Chloroprocaine for Lower Limb Arthroplasty

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).