Repositioning Candidate Details
| Candidate ID: | R0420 |
| Source ID: | DB01136 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Carvedilol |
| Synonyms: | (+-)-1-(Carbazol-4-yloxy)-3-((2-(o-methoxyphenoxy)ethyl)amino)-2-propanol |
| Molecular Formula: | C24H26N2O4 |
| SMILES: | COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=C1C1=CC=CC=C1N2 |
| Structure: |
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| DrugBank Description: | Carvedilol is a racemic mixture where the S(-) enantiomer is a beta adrenoceptor blocker and the R(+) enantiomer is both a beta and alpha-1 adrenoceptor blocker. It is currently used to treat heart failure, left ventricular dysfunction, and hypertension. The dual action of carvedilol is advantageous in combination therapies as moderate doses of 2 drugs have a decreased incidence of adverse effects compared to high dose monotherapy in the treatment of moderate hypertension. Carvedilol was granted FDA approval on 14 September 1995. |
| CAS Number: | 72956-09-3 |
| Molecular Weight: | 406.4742 |
| DrugBank Indication: | Carvedilol is indicated to treat mild to severe heart failure, left ventricular dysfunction after myocardial infarction with ventricular ejection fraction ≤40%, or hypertension. |
| DrugBank Pharmacology: | Carvedilol reduces tachycardia through beta adrenergic antagonism and lowers blood pressure through alpha-1 adrenergic antagonism. It has a long duration of action as it is generally taken once daily and has a broad therapeutic index as patients generally take 10-80mg daily. Patients taking carvedilol should not abruptly stop taking this medication as this may exacerbate coronary artery disease. |
| DrugBank MoA: | Carvedilol inhibits exercise induce tachycardia through its inhibition of beta adrenoceptors. Carvedilol's action on alpha-1 adrenergic receptors relaxes smooth muscle in vasculature, leading to reduced peripheral vascular resistance and an overall reduction in blood pressure. At higher doses, calcium channel blocking and antioxidant activity can also be seen. The antioxidant activity of carvedilol prevents oxidation of low density lipoprotein and its uptake into coronary circulation. |
| Targets: | Beta-1 adrenergic receptor antagonist; Alpha-1A adrenergic receptor antagonist&potentiator; NADH dehydrogenase [ubiquinone] 1 subunit C2 inhibitor; Beta-2 adrenergic receptor antagonist; Vascular endothelial growth factor A other; Natriuretic peptides B other; Gap junction alpha-1 protein other; Potassium voltage-gated channel subfamily H member 2 inhibitor; Vascular cell adhesion protein 1 inhibitor; Alpha-1D adrenergic receptor antagonist; Alpha-1B adrenergic receptor antagonist; Alpha-2C adrenergic receptor antagonist; Alpha-2B adrenergic receptor antagonist; Alpha-2A adrenergic receptor antagonist; E-selectin inhibitor; Hypoxia-inducible factor 1-alpha modulator; Inward rectifier potassium channel 4 inhibitor; Inward rectifier potassium channel 2 inhibitor; Alpha-1 adrenergic receptors inhibitor |
| Inclusion Criteria: | Indication associated |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I08 | 114 | Cardiovascular system disease | A disease of anatomical entity which occurs in the blood, heart, blood vessels or the lymphatic system that passes nutrients (such as amino acids and electrolytes), gases, hormones, blood cells or lymph to and from cells in the body to help fight diseases and help stabilize body temperature and pH to maintain homeostasis. http://en.wikipedia.org/wiki/Circulatory_system | disease of anatomical entity | Details |
| 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 |