Repositioning Candidate Details
| Candidate ID: | R0638 |
| Source ID: | DB04883 |
| Source Type: | investigational |
| Compound Type: | small molecule |
| Compound Name: | Darusentan |
| Synonyms: | Darusentan |
| Molecular Formula: | C22H22N2O6 |
| SMILES: | COC1=CC(OC)=NC(O[C@H](C(O)=O)C(OC)(C2=CC=CC=C2)C2=CC=CC=C2)=N1 |
| Structure: |
|
| DrugBank Description: | Darusentan is a selective endothelin ETA receptor antagonist. It is being evaluated as a treatment for congestive heart failure and hypertension. |
| CAS Number: | 171714-84-4 |
| Molecular Weight: | 410.4199 |
| DrugBank Indication: | For the treatment of congestive heart failure and hypertension. |
| DrugBank Pharmacology: | Darusentan is a selective endothelin ETA receptor antagonist. |
| DrugBank MoA: | The mode of action by which the endothelin receptor antagonists cause a decrease of the BP is not yet totally elucidated; however, peripheral vasodilatation due to blockade of the vasoconstrictor effects of endothelin is the most likely explanation. A reduction of cardiac contractility is considered unlikely. Several studies have been published that investigated the effects of either selective or nonselective endothelin receptor blockade in patients with heart failure. In these studies, application of endothelin antagonists, while decreasing both systemic and pulmonary BP increased cardiac index and did not alter cardiac contractility or heart rate. |
| Targets: | Endothelin-1 receptor |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I12 | 10763 | Hypertension | An artery disease characterized by chronic elevated blood pressure in the arteries. https://en.wikipedia.org/wiki/Hypertension, https://www.ncbi.nlm.nih.gov/pubmed/24352797 | disease of anatomical entity/ cardiovascular system disease/vascular disease/ artery disease | Details |