Investigational Drug Details
| Drug ID: | D174 |
| Drug Name: | Bisoprolol |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00612 |
| DrugBank Description: | Bisoprolol is a cardioselective β1-adrenergic blocking agent used to treat high blood pressure.[A180472,L7219] It is considered a potent drug with a long-half life that can be used once daily to reduce the need for multiple doses of antihypertensive drugs.[A180472] Bisoprolol is generally well tolerated, likely due to its β1-adrenergic receptor selectivity and is a useful alternative to non-selective β-blocker drugs in the treatment of hypertension such as [Carvedilol] and [Labetalol]. It may be used alone or in combination with other drugs to manage hypertension[L7219] and can be useful in patients with chronic obstructive pulmonary disease (COPD) due to its receptor selectivity.[A180562] |
| PubChem ID: | 2405 |
| CasNo: | 66722-44-9 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1 |
| Structure: |
|
| InChiKey: | VHYCDWMUTMEGQY-UHFFFAOYSA-N |
| Molecular Weight: | 325.443 |
| DrugBank Targets: | Beta-1 adrenergic receptor; Beta-2 adrenergic receptor |
| DrugBank MoA: | Though the mechanism of action of bisoprolol has not been fully elucidated in hypertension, it is thought that therapeutic effects are achieved through the antagonism of β-1adrenoceptors to result in lower cardiac output. Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. When β1-receptors (located mainly in the heart)[T640] are activated by adrenergic neurotransmitters such as epinephrine, both the blood pressure and heart rate increase, leading to greater cardiovascular work, increasing the demand for oxygen. Bisoprolol reduces cardiac workload by decreasing contractility and the need for oxygen through competitive inhibition of β1-adrenergic receptors.[A180499,A180502,T640] Bisoprolol is also thought to reduce the output of renin in the kidneys, which normally increases blood pressure. Additionally, some central nervous system effects of bisoprolol may include diminishing sympathetic nervous system output from the brain, decreasing blood pressure and heart rate.[L7219] |
| DrugBank Pharmacology: | Bisoprolol decreases heart rate (chronotropy), decreases contractility (inotropy), and reduces blood pressure.[T640,L7219] The results of various clinical studies indicate that bisoprolol reduces cardiovascular mortality and all-cause mortality in patients with heart failure and decreased cardiac ejection fraction (EF).[A180466,A180505] |
| DrugBank Indication: | Bisoprolol is indicated for the treatment of mild to moderate hypertension.[L7219] It may be used off-label to treat heart failure, atrial fibrillation, and angina pectoris.[A180460,A180463] |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L3128 | NCT04711226 | PHASE2 | WITHDRAWN | NO | 2021-02-19 | 2022-08-10 | Details |
| L7192 | NCT00283777 | PHASE4 | COMPLETED | NO | 1998-08 | 2016-04-08 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Article ID | PMID | Source | Title |
|---|