Tolperisone

Summary

Tolperisone (CHEMBL1076211) is a phase-3 clinical-stage small molecule (ATC M02AX06); indicated across 4 conditions.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: M02AX06 (+1 more)
• Indications: 4 conditions
• Clinical trials: 4
• Chemistry: 245.36 Da · C16H23NO

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1076211
Name	Tolperisone
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5511
ATC	M02AX06, M03BX04
Molecular formula	C16H23NO
Molecular weight	245.36
InChIKey	FSKFPVLPFLJRQB-UHFFFAOYSA-N

SMILES: CC1=CC=C(C=C1)C(=O)C(C)CN2CCCCC2

IUPAC name: 2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one

Also known as: N-553 FREE BASE, NSC-107321, Tolperisona, Tolperisone, TOLPERISONE, tolperisone, Tolperisone hydrochlorideÊ, Tolperisone hydrochlorideÂ

Parent form; salt/anhydrous children: CHEMBL1395150, CHEMBL2107740

Patent coverage: 723 distinct patent families (2,402 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: 5 (assay-derived). Sample: Alpha-2B adrenergic receptor, Muscarinic acetylcholine receptor M2, D(3) dopamine receptor, Histamine H3 receptor, Sigma non-opioid intracellular receptor 1.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SIGMAR1	8.25	Ki	5.59	nM	CHEMBL_ACT_7823675
SIGMAR1	7.89	IC50	13	nM	CHEMBL_ACT_7823674
ADRA2B	6.34	Ki	456	nM	CHEMBL_ACT_7819465
ADRA2B	6	IC50	1000	nM	CHEMBL_ACT_7819464
DRD3	5.6	AC50	2520	nM	CHEMBL_ACT_25194923
CHRM2	5.43	AC50	3699	nM	CHEMBL_ACT_25196148
HRH3	5.33	AC50	4736	nM	CHEMBL_ACT_25199944

Target pathways

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

Indications & clinical

Indications

4 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE2	3
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00531466	PHASE2	TERMINATED	Safety and Preliminary Effectiveness of AV650 in Patients With Spasticity Due to Spinal Cord Injury
NCT00532532	PHASE2	TERMINATED	Safety and Preliminary Effectiveness of AV650 in Patients With Spasticity Associated With Multiple Sclerosis
NCT03802565	PHASE2	COMPLETED	Tolperisone in Acute Muscle Spasm of the Back
NCT04465266	PHASE1	COMPLETED	A Phase 1 PK Study of Tolperisone in Healthy Subjects

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 4 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

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