Prilocaine

Summary

Prilocaine (CHEMBL1194) is an approved small-molecule local anaesthetic (ATC N01BB04); indicated across 8 conditions including skin disorder and premature ejaculation.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N01BB04 (+1 more)
• Indications: 8 conditions
• Clinical trials: 44
• Chemistry: 220.31 Da · C13H20N2O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1194
Name	Prilocaine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4906
ChEBI	CHEBI:8404
ATC	N01BB04, N01BB54
Molecular formula	C13H20N2O
Molecular weight	220.31
InChIKey	MVFGUOIZUNYYSO-UHFFFAOYSA-N

SMILES: CCCNC(C)C(=O)NC1=CC=CC=C1C

IUPAC name: N-(2-methylphenyl)-2-(propylamino)propanamide

ChEBI definition: An amino acid amide in which N-propyl-DL-alanine and 2-methylaniline have combined to form the amide bond; used as a local anaesthetic.

Pharmacological roles (ChEBI): local anaesthetic, anticonvulsant.

Also known as: ASTRA-1512, ASTRA-1515, NSC-40027, Prilocaina, Prilocaine, Prilocaine component of emla, Prilocaine component of fortacin, Prilocaine component of oraqix, Propitocaine, PRILOCAINE, SID90341069, PRILOCAINE HYDROCHLORIDE

Parent form; salt/anhydrous children: CHEMBL1200586

Patent coverage: 4,330 distinct patent families (15,137 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 15,136 (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: 3 (assay-derived). Sample: Progesterone receptor, Sodium channel alpha subunits; brain (Types I, II, III), Glutamate receptor ionotropic, NMDA 1.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PGR	5.41	AC50	3900	nM	CHEMBL_ACT_25222270

Target pathways

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

Indications & clinical

Indications

8 indications (1 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
skin disorder	2	MONDO:0005093	EFO:0000701
premature ejaculation	2	MONDO:0001780	EFO:0803321
squamous cell carcinoma	1	MONDO:0005096	EFO:0000707
actinic keratosis	1	MONDO:0005173	EFO:0002496

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

Clinical trials

Total trials: 44.

Phase distribution

Phase	Trials
Not specified	19
PHASE4	16
PHASE1	5
PHASE2/PHASE3	2
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07329582	PHASE4	ACTIVE_NOT_RECRUITING	Hyperbaric Bupivacaine Versus Hyperbaric Prilocaine in Spinal Anaesthesia
NCT07546370	PHASE4	NOT_YET_RECRUITING	The Effectiveness of Topical Prilocaine-Lidocaine Cream Plus Acetaminophen and Naproxen Compared to Lidocaine Injection Plus Acetaminophen and Naproxen to Manage Pain During IntraUterine Device Insertion
NCT00408941	PHASE4	UNKNOWN	EEG and Auditory Evoked Potentials During Local Anesthesia
NCT01309360	PHASE4	COMPLETED	Ultrasound-guided Axillary Plexus Block - Dose Reduction of Prilocaine
NCT01591616	PHASE4	COMPLETED	Pediatric Study to Access Pharmacokinetics and Safety of Oraqix Gel
NCT01880775	PHASE4	COMPLETED	Discharge Conditions of Spinal Anesthesia With Heavy Prilocaine-Fentanyl and Heavy Bupivacaine-Fentanyl
NCT02384915	PHASE4	COMPLETED	Spinal Anesthesia Versus Combined Sciatic-femoral Nerve Block for Outpatient Knee Arthroscopy
NCT02820688	PHASE4	COMPLETED	Concentration-Volume Relationship in Infraclavicular Block
NCT03038958	PHASE4	COMPLETED	Comparison of Hyperbaric Prilocaine With Chloroprocaine for Intrathecal Anaesthesia in Day Case Knee Arthroscopy
NCT03731988	PHASE4	COMPLETED	Efficacy of Ablative Fractional Laser-assisted Photodynamic Therapy According to the Laser Density for Actinic Keratosis
NCT04756050	PHASE4	COMPLETED	Comparison of Different Approaches for Supraclavicular Block and Their Effects on Diaphragm Muscle Function
NCT04784104	PHASE4	UNKNOWN	Comparison of Infraclavicular And Supraclavicular Block
NCT05610007	PHASE4	UNKNOWN	Comparison of Hyperbaric Prilocaine 2% 50 Mg and Hyperbaric Bupivacaine 0.5% 12.5 Mg Against Spinal Anesthesia Recovery Time in Cystoscopy Procedure
NCT05834647	PHASE4	UNKNOWN	Efficacy and Safety of Prilocaine 2% and Lidocaine 5% Hyperbaric Against Spinal Anesthesia in Post Cystoscopy Procedure
NCT06133881	PHASE4	COMPLETED	Effect of Prilocaine on Motor Block During Caesarean Section
NCT07262398	PHASE4	COMPLETED	Unilateral Intrathecal Bupivacaine Versus Prilocaine on Postoperative Spontaneous Voiding
NCT00556478	PHASE2/PHASE3	COMPLETED	Efficacy, Safety and Tolerability of PSD502 (a Topical Anesthetic) in the Treatment Premature Ejaculation
NCT02973048	PHASE3	COMPLETED	Hyperbaric Bupivacaine Versus Hyperbaric Prilocaine 2% for Cesarean Section Under Spinal Anesthesia
NCT04523961	PHASE2/PHASE3	COMPLETED	Comparative Study of Two Topical Anesthetics Prior to Fractional Nonablative Laser Treatment of the Face
NCT06165679	PHASE3	COMPLETED	Effect of Prilocaine vs Bupivacaine on Hemodynamics in Spinal Anesthesia for Geriatric Patients
NCT01073371	PHASE1	COMPLETED	Anesthetic Efficacy of Liposomal Prilocaine in Maxillary Infiltration Anesthesia
NCT02670655	PHASE1	COMPLETED	Efficacy of Iontophoresis-assisted AFL-PDT in Actinic Keratosis
NCT02976727	PHASE1	COMPLETED	Efficacy of Topical Calcipotriol-assisted AFL-PDT in Actinic Keratosis
NCT03325803	PHASE1	COMPLETED	Efficacy in Ablative Fractional Laser Assisted Photodynamic Therapy According to Ablative Depth for Actinic Keratosis
NCT03441841	PHASE1	COMPLETED	Pharmacokinetic Study of Nanoencapsulated Gel of Lidocaine, Prilocaine and Combination of Lidocaine and Prilocaine
NCT00309673	Not specified	UNKNOWN	Local Anesthesia and Tuberculin Skin Test in Infants and Children
NCT01643616	Not specified	COMPLETED	Ultrasound Guided Distal Sciatic Nerve Block - a Comparison With Nerve Stimulator Technique
NCT01963559	Not specified	COMPLETED	Cutaneous Microcirculation and Diabetic Foot
NCT02282280	Not specified	COMPLETED	Clinical Use of Prilocaine Chlorhydrate Among a General Surgical Population
NCT02390310	Not specified	COMPLETED	Simplifying the Shang Ring Technique for Circumcision of Men and Boys
NCT02403687	Not specified	COMPLETED	Prospective Analgesic Compound Efficacy (PACE) Study
NCT02537951	Not specified	COMPLETED	Autofluorescent Flavoprotein Imaging of Intraepidermal Nerve Fibers: a Pilot Study
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
NCT03219086	Not specified	COMPLETED	Spinal Prilocaine for Caesarian Sections
NCT04161586	Not specified	COMPLETED	Prilocaine for Spinal Anesthesia in Ambulatory Setting
NCT05042817	Not specified	COMPLETED	Effect of Intrathecal Morphine on Urinary Bladder Function and Recovery in Patients Having a Cesarean Delivery
NCT05648708	Not specified	COMPLETED	Combined Adductor&Sciatic Nerve Block vs Femoral&Sciatic Nerve Block in Total Knee Replacement Surgery
NCT05688202	Not specified	COMPLETED	Simultaneous Versus Sequential Fractional CO2 Laser and Subcision Combination for Post-acne Atrophic Scars: A Split-face Comparative Study.
NCT05877690	Not specified	UNKNOWN	Selective Spinal Anaesthesia With Hyperbaric Prilocain With 2%Provides Better Perioperative Hemodynamic Stability for Patients With Peripheral Vascular Disease and Cardiac Dysfunction in Lower Limb Surgery

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).