Details of the Drug

General Information of Drug (ID: DM9J6C2)

• Drug Name: Tetracaine
• Synonyms: Amethocaine; Anetain; Contralgin; Dicain; Dicaine; Dikain; Fissucain; Intercain; Laudocaine; Medicaine; Meethobalm; Metraspray; Mucaesthin; Niphanoid; Pontocaine; Rexocaine; Tetracaina; Tetracainum; Tetrakain; Uromucaesthin; Tetrakain [Czech]; Amethocaine (TN); Diaethylaminoaethanol ester der p-butylaminobenzoesaeure;Diaethylaminoaethanol ester der p-butylaminobenzoesaeure [German]; Medihaler-Tetracaine; Pontocaine (TN); Tetracaina [INN-Spanish]; Tetracaine [USAN:INN]; Tetracainum [INN-Latin]; Dimethylaminoethyl p-butyl-aminobenzoate; Tetracaine (USP/INN); P-Butylaminobenzoyl-2-dimethylaminoethanol; BENZOIC ACID,4-BUTYLAMINO,2-DIMETHYLAMINOETHYL ESTER PANTOCAIN BASE; P-(Butylamino)benzoic acid, 2-(dimethylamino)ethyl ester; BENZOIC ACID, p-(BUTYLAMINO)-, 2-(DIMETHYLAMINO)ETHYL ESTER; Benzoic acid, 4-(butylamino)-, 2-(dimethylamino)ethyl ester; 2-(Dimethylamino)ethyl 4-(butylamino)benzoate; 2-(Dimethylamino)ethyl p-(butylamino)benzoate; 2-Dimethylaminoethylester kyseliny p-butylaminobenzoove; 2-Dimethylaminoethylester kyseliny p-butylaminobenzoove [Czech]; 2-dimethylaminoethyl 4-(butylamino)benzoate; 4-(Butylamino)benzoic acid 2-(dimethylamino)ethyl ester; 4-[Butylamino]benzoic acid-2-[dimethylamino]ethyl ester

Indication

Disease Entry	ICD 11	Status	REF
Spinal anesthesia	MB40.3	Approved	[1]
Pain	MG30-MG3Z	Phase 2	[2]
Pruritus	EC90	Investigative	[3]

• Therapeutic Class: Anesthetics
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 264.36
  Logarithm of the Partition Coefficient (xlogp); 3.7
  Rotatable Bond Count (rotbonds); 9
  Hydrogen Bond Donor Count (hbonddonor); 1
  Hydrogen Bond Acceptor Count (hbondacc); 4
• ADMET Property: Metabolism: The drug is metabolized via plasma esterases []
• Chemical Identifiers:
  Formula: C15H24N2O2
  IUPAC Name: 2-(dimethylamino)ethyl 4-(butylamino)benzoate
  Canonical SMILES: CCCCNC1=CC=C(C=C1)C(=O)OCCN(C)C
  InChI: InChI=1S/C15H24N2O2/c1-4-5-10-16-14-8-6-13(7-9-14)15(18)19-12-11-17(2)3/h6-9,16H,4-5,10-12H2,1-3H3
  InChIKey: GKCBAIGFKIBETG-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 5411
  ChEBI ID: CHEBI:9468
  CAS Number: 94-24-6
  DrugBank ID: DB09085
  TTD ID: D08HQK
  VARIDT ID: DR00562
  ACDINA ID: D01479
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated sodium channel alpha Nav1.8 (SCN10A)	TT90XZ8	SCNAA_HUMAN	Inhibitor	[4]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
72 kDa type IV collagenase (MMP2)	OT5NIWA2	MMP2_HUMAN	Gene/Protein Processing	[5]
Cyclin-dependent kinase 2 (CDK2)	OTB5DYYZ	CDK2_HUMAN	Post-Translational Modifications	[6]
Cyclin-dependent kinase 4 (CDK4)	OT7EP05T	CDK4_HUMAN	Post-Translational Modifications	[6]
Cyclin-dependent kinase 6 (CDK6)	OTR95N0X	CDK6_HUMAN	Post-Translational Modifications	[6]
G1/S-specific cyclin-D1 (CCND1)	OT8HPTKJ	CCND1_HUMAN	Gene/Protein Processing	[6]
G1/S-specific cyclin-E1 (CCNE1)	OTLD7UID	CCNE1_HUMAN	Gene/Protein Processing	[6]
Heterogeneous nuclear ribonucleoprotein A0 (HNRNPA0)	OTCP792K	ROA0_HUMAN	Gene/Protein Processing	[6]
Heterogeneous nuclear ribonucleoprotein A1 (HNRNPA1)	OTIRPN6B	ROA1_HUMAN	Gene/Protein Processing	[6]
Heterogeneous nuclear ribonucleoproteins C1/C2 (HNRNPC)	OT47AK4C	HNRPC_HUMAN	Gene/Protein Processing	[6]
Histamine H1 receptor (HRH1)	OT8F9FV6	HRH1_HUMAN	Drug Response	[7]

Molecular Expression Atlas of This Drug

• The Studied Disease: Spinal anesthesia
• ICD Disease Classification: MB40.3

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Voltage-gated sodium channel alpha Nav1.8 (SCN10A)	DTT	SCN10A	9.89E-01	-0.16	-0.31

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
methylparaben	E00149	7456	Antimicrobial preservative
Propylparaben sodium	E00567	23679044	Antimicrobial preservative
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Stearic acid	E00079	5281	Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Eucalyptol	E00063	2758	Flavoring agent
Lauric diethanolamide	E00176	8430	Surfactant; Viscosity-controlling agent
Trolamine	E00151	7618	Alkalizing agent; Emulsifying agent
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Water	E00035	962	Solvent
Diazolidinyl urea	E00354	62277	Antimicrobial preservative

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Tetracaine 1% cream	1%	Cream	Topical

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] Evaluation of a novel topical anesthetic agent for cutaneous laser resurfacing: a randomized comparison study. Dermatol Surg. 2002 Nov;28(11):1004-6; discussion 1006.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [3] Tetracaine FDA Label
• [4] Heterologous expression and functional analysis of rat Nav1.8 (SNS) voltage-gated sodium channels in the dorsal root ganglion neuroblastoma cell line ND7-23. Neuropharmacology. 2004 Mar;46(3):425-38.
• [5] Tetracaine downregulates matrix metalloproteinase activity and inhibits invasiveness of strongly metastatic MDA-MB-231 human breast cancer cells. Chem Biol Interact. 2023 Nov 1;385:110730. doi: 10.1016/j.cbi.2023.110730. Epub 2023 Oct 7.
• [6] Tetracaine hydrochloride induces cell cycle arrest in melanoma by downregulating hnRNPA1. Toxicol Appl Pharmacol. 2022 Jan 1;434:115810. doi: 10.1016/j.taap.2021.115810. Epub 2021 Nov 23.
• [7] H(1)R mediates local anesthetic-induced vascular permeability in angioedema. Toxicol Appl Pharmacol. 2020 Apr 1;392:114921. doi: 10.1016/j.taap.2020.114921. Epub 2020 Feb 12.