Trimetazidine

Summary

Trimetazidine (CHEMBL203266) is an approved small molecule (ATC C01EB15); indicated across 9 conditions including cardiovascular disorder and hypertrophic cardiomyopathy.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C01EB15
• Indications: 9 conditions
• Clinical trials: 28
• Chemistry: 266.34 Da · C14H22N2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL203266
Name	Trimetazidine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	21109
ATC	C01EB15
Molecular formula	C14H22N2O3
Molecular weight	266.34
InChIKey	UHWVSEOVJBQKBE-UHFFFAOYSA-N

SMILES: COC1=C(C(=C(C=C1)CN2CCNCC2)OC)OC

IUPAC name: 1-[(2,3,4-trimethoxyphenyl)methyl]piperazine

Also known as: Dilatan, Trimetazidina, Trimetazidine, Vastarel, Vastarel mr, SID11112605, SID56423815, TRIMETAZIDINE, TRIMETAZIDINE DIHYDROCHLORIDE, trimetazidine

Parent form; salt/anhydrous children: CHEMBL3561076

Patent coverage: 1,181 distinct patent families (3,418 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 3,380 (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: 7 (assay-derived). Sample: Ferritin light chain, Muscarinic acetylcholine receptor M2, Sodium-dependent serotonin transporter, Delta-type opioid receptor, Kappa-type opioid receptor, Carnitine O-palmitoyltransferase 1, muscle isoform, Cytochrome P450 1A2.

Bioactivity

ChEMBL activities: 5 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
Q63704	5.89	IC50	1300	nM	CHEMBL_ACT_12204980
Q63704	5.89	IC50	1300	nM	CHEMBL_ACT_25908831
OPRK1	5	AC50	9900	nM	CHEMBL_ACT_25129916
P02791	5	Potency	10000	nM	CHEMBL_ACT_4477783
CYP1A2	5	AC50	10000	nM	CHEMBL_ACT_6016484

Target pathways

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

Indications & clinical

Indications

9 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
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
hypertrophic cardiomyopathy	2	MONDO:0005045	EFO:0000538
pulmonary arterial hypertension	2	MONDO:0015924	EFO:0001361
diabetic kidney disease	2	MONDO:0005016	EFO:0000401
metabolic dysfunction-associated steatotic liver disease	2	MONDO:0013209	EFO:0003095
heart failure	1	MONDO:0005252	EFO:0003144
peripheral neuropathy	1	MONDO:0005244	EFO:0003100

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

Clinical trials

Total trials: 28.

Phase distribution

Phase	Trials
PHASE4	9
PHASE2	8
Not specified	4
PHASE2/PHASE3	2
PHASE3	2
PHASE1	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00282360	PHASE4	COMPLETED	Effect of Metabolic Therapy in Patients With Chronic Ischemic Heart Disease
NCT02107144	PHASE4	COMPLETED	The ImPact of Trimetazidine on MicrOcirculation After Stenting for Stable Coronary Artery Disease
NCT03072082	PHASE4	UNKNOWN	Curative Effect Evaluation of Danlou Tablet on Coronary Artery Disease Not Amenable to Revascularization
NCT03072121	PHASE4	UNKNOWN	Curative Effect Evaluation of Shexiang Baoxin Pill on Coronary Artery Disease Not Amenable to Revascularization
NCT03809273	PHASE4	COMPLETED	Effects of Yangxinshi Pills on the Exercise Tolerance Compared With Trimetazidine in Patients After PCI
NCT03887013	PHASE4	UNKNOWN	Cardiac Metabolic Modulator Treatment for Improvement of Diastolic Function in Patients With Coronary Heart Disease
NCT04661709	PHASE4	UNKNOWN	Efficacy and Safety of Wen Xin Granules for the Treatment of Unstable Angina Pectoris
NCT05540184	PHASE4	UNKNOWN	Allopurinol and Trimetazidine as a Preventive of Acute Kidney Injury in PCI Patients
NCT05633563	PHASE4	COMPLETED	The Effect of Trimetazidine on Mitochondrial Function, Myocardial Performance, and Invasive Hemodynamics in Patients Diagnosed With Wild-Type Transthyretin Cardiac Amyloidosis
NCT03273387	PHASE2/PHASE3	COMPLETED	The Role of Trimetazidine on Right Ventricle Function in Pulmonary Arterial Hypertension
NCT03715582	PHASE3	UNKNOWN	Trimetazidine in Myocardial Injury After Percutaneous Coronary Intervention in Patients With Angina and Diabetes
NCT04939857	PHASE2/PHASE3	UNKNOWN	Effect of Trimetazidine on Radiotherapy-induced Heart Damage.
NCT06656442	PHASE3	COMPLETED	The Effect of Trimetazidine on the Clinical Outcome of Acute Ischemic Stroke Patients
NCT01696370	PHASE2	UNKNOWN	Trimetazidine Therapy in Hypertrophic Cardiomyopathy
NCT02102672	PHASE2	UNKNOWN	Trimetazidine in Pulmonary Artery Hypertension
NCT03603249	PHASE2	COMPLETED	Trimetazidine as an Adjunct to Enhance Clopidogrel Response.
NCT04760821	PHASE2	UNKNOWN	Prevention of Acute Myocardial Injury by Trimetazidine in Patients Hospitalized for COVID-19
NCT04788745	PHASE2	COMPLETED	Targeting Metabolic Flexibility in Amyotrophic Lateral Sclerosis (ALS)
NCT05147194	PHASE2	UNKNOWN	The Effects of TMZ on Diabetic Nephropathy
NCT05556005	PHASE2	UNKNOWN	Efficacy of Trimetazidine in Diabetic Patients
NCT06140953	PHASE2	COMPLETED	Benefits of Trimetazidine in MASLD Patients
NCT06459193	PHASE1/PHASE2	COMPLETED	Trimetazidine Efficacy in Attenuating Paclitaxel-Induced Peripheral Neuropathy
NCT03333499	PHASE1	UNKNOWN	the Effects of YangXinShi (YXS) on the Quality of Life and Exercise Tolerance in Patients With Chronic Heart Failure
NCT03737448	PHASE1	SUSPENDED	TRimetazidine for acUte on Chronic Liver Failure STudy
NCT02826616	Not specified	UNKNOWN	Effect of Trimetazidine During the Primary PCI on Cardiac Function in Patients With ST-elevation Myocardial Infarction
NCT03504202	Not specified	UNKNOWN	Effect of Trimetazidine on the Improvement of Coronary Microvascular Dysfunction in Patients With INOCA(Ischemia and no Obstructive Coronary Artery Disease)
NCT04511520	Not specified	COMPLETED	Efficacy of Personalized Exercise Program and Trimetazidine in Rehabilitation of Patients After RFA of AF
NCT07074834	Not specified	COMPLETED	Metoprolol and Trimetazidine for Coronary Heart Disease With Angina

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).