Trimetazidine
C01E - Other cardiac preparations
ATC C01EB15
Small molecule
Natural product
JFDA label: Vastarel MR
Indications
Approved
- Cardiovascular Diseases — cardiovascular disease
Off-label
- Cardiomyopathy, Hypertrophic
- Cardiotoxicity
- Diabetic Nephropathies
- Hypertension, Pulmonary
- Non-alcoholic Fatty Liver Disease
Pregnancy & Lactation
Chemistry & Properties
| Formula | C14H22N2O3 |
|---|
| Molecular weight | 266.34 g/mol |
|---|
| IUPAC name | 1-[(2,3,4-trimethoxyphenyl)methyl]piperazine |
|---|
| CAS | 5011-34-7 |
|---|
| PubChem CID | 21109 |
|---|
| InChIKey | UHWVSEOVJBQKBE-UHFFFAOYSA-N |
|---|
| logP | 1.12 (XLogP 1.0) |
|---|
| Polar surface area | 42.96 Ų |
|---|
| H-bond acceptors / donors | 5 / 1 |
|---|
| Drug-likeness (QED) | 0.86 |
|---|
| Lipinski violations | 0 |
|---|
SMILES
COc1ccc(CN2CCNCC2)c(OC)c1OCBiology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 10.0% |
|---|
| Half-life | 1.191 h |
|---|
| Volume of distribution | 2.234 L/kg |
|---|
| Protein binding | 20.6% |
|---|
| BBB penetrant | No |
|---|
Enzyme interactions
| Enzyme | Role | Detail |
|---|
| CYP1A2 | Inhibitor |
— |
| CYP1A2 | Substrate |
— |
| CYP2C19 | Substrate |
— |
| CYP3A4 | Substrate |
— |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Registered Products (3)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|
| Energ MR
|
Tablet 35 mg |
60 tab |
Pharma International Company/ Jordan |
6.560 |
| Tprizat 35mg MR
|
Tablet 35 mg |
60 tab |
UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN |
6.570 |
| Vastarel MR
|
Tablet 35 mg |
60 tab |
The Jordan Drugstore Co |
8.280 |