Oxethazaine

Summary

Oxethazaine (CHEMBL127592) is a phase-3 clinical-stage small molecule (ATC C05AD06); indicated across 1 condition including hemorrhoid.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: C05AD06
• Indications: 1 condition
• Clinical trials: 1
• Chemistry: 467.6 Da · C28H41N3O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL127592
Name	Oxethazaine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	4621
ATC	C05AD06
Molecular formula	C28H41N3O3
Molecular weight	467.6
InChIKey	FTLDJPRFCGDUFH-UHFFFAOYSA-N

SMILES: CC(C)(CC1=CC=CC=C1)N(C)C(=O)CN(CCO)CC(=O)N(C)C(C)(C)CC2=CC=CC=C2

IUPAC name: 2-[2-hydroxyethyl-[2-[methyl-(2-methyl-1-phenylpropan-2-yl)amino]-2-oxoethyl]amino]-N-methyl-N-(2-methyl-1-phenylpropan-2-yl)acetamide

Also known as: NSC-758444, Oxetacaina, Oxetacaine, Oxethazaine, Strocain, WY-806, SID11112275, SID26748773, SID56463559, OXETHAZAINE, SID144203958, SID170465643

Patent coverage: 846 distinct patent families (3,161 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: 10 (assay-derived). Sample: Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Thyrotropin receptor, Menin/Histone-lysine N-methyltransferase MLL, Sodium channel alpha subunits; brain (Types I, II, III), Cytochrome P450 2D6, Polyunsaturated fatty acid lipoxygenase ALOX15, Cytochrome P450 3A4, Cytochrome P450 2C19, Hypoxia-inducible factor 1-alpha.

Bioactivity

ChEMBL activities: 10 potent at pChembl ≥ 5 of 17 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	7.35	Potency	44.7	nM	CHEMBL_ACT_3646520
SCN1A	5.64	IC50	2300	nM	CHEMBL_ACT_349628
ALOX15	5.6	Potency	2512	nM	CHEMBL_ACT_4464508
CYP2D6	5.5	Potency	3162	nM	CHEMBL_ACT_4973933
CYP2D6	5.5	AC50	3162	nM	CHEMBL_ACT_6006426
HIF1A	5.1	Potency	7943	nM	CHEMBL_ACT_4131597
HIF1A	5.1	Potency	7943	nM	CHEMBL_ACT_4519120
CYP3A4	5.1	Potency	7943	nM	CHEMBL_ACT_4997834
CYP3A4	5.1	Potency	7943	nM	CHEMBL_ACT_5066543
CYP3A4	5.1	AC50	7943	nM	CHEMBL_ACT_6049364

Target pathways

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

Indications & clinical

Indications

1 indication (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
hemorrhoid	3	MONDO:0004872	EFO:0009552

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01336530	PHASE3	TERMINATED	Tepilta® Versus Oxetacaine, Antacids and Placebo

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).