Repositioning Candidate Details
| Candidate ID: | R0150 |
| Source ID: | DB00528 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Lercanidipine |
| Synonyms: | |
| Molecular Formula: | C36H41N3O6 |
| SMILES: | COC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OC(C)(C)CN(C)CCC(C1=CC=CC=C1)C1=CC=CC=C1 |
| Structure: |
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| DrugBank Description: | Lercanidipine is a calcium channel blocker of the dihydropyridine class. It is sold under various commercial names including Zanidip. |
| CAS Number: | 100427-26-7 |
| Molecular Weight: | 611.7272 |
| DrugBank Indication: | For the treatment of Hypertension, management of angina pectoris and Raynaud's syndrome |
| DrugBank Pharmacology: | Lercanidipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Lercanidipine is similar to other peripheral vasodilators. Lercanidipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. |
| DrugBank MoA: | By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Lercanidipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. |
| Targets: | Voltage-dependent calcium channel gamma-1 subunit |
| Inclusion Criteria: |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name | |
|---|---|---|---|---|---|---|---|
| T01 | Insulin receptor | INSR | AGONIST; INHIBITOR | Target is a single protein chain | P06213 | INSR_HUMAN | Details |
| T03 | Angiotensin-converting enzyme | ACE | INHIBITOR | Target is a single protein chain | P12821 | ACE_HUMAN | Details |
| T04 | Peroxisome proliferator-activated receptor gamma | PPARG | AGONIST; MODULATOR; PARTIAL AGONIST; ANTAGONIST | Target is a single protein chain | P37231 | PPARG_HUMAN | Details |
| T06 | Sulfonylurea receptor 1 | ABCC8 | Target is a single protein chain | Q09428 | ABCC8_HUMAN | Details | |
| T15 | Steryl-sulfatase | STS | INHIBITOR | Hydrolase | P08842 | STS_HUMAN | Details |
| T47 | Sialin | SLC17A5 | Target is a single protein chain | Q9NRA2 | SLC17A5_HUMAN | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I02 | 1184 | nephrotic syndrome | "A nephrosis characterized by marked increase in glomerular protein permeability resulting in marked elevation of urine protein levels, hypoalbuminemia, hyperlipidemia, and hypercoagulability." [url:https\://en.wikipedia.org/wiki/Nephrotic_syndrome, url:https\://www.niddk.nih.gov/health-information/kidney-disease/nephrotic-syndrome-adults] | Details | |
| I07 | 9352 | type 2 diabetes mellitus | "A diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin." [url:http\://en.wikipedia.org/wiki/Diabetes, url:http\://en.wikipedia.org/wiki/Diabetes_mellitus_type_2] | Details |