Investigational Drug Details
| Drug ID: | D064 |
| Drug Name: | Ranolazine |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00243 |
| DrugBank Description: | Ranolazine is an acetanilide and piperazine derivative that is used for the treatment of angina.[L3580] It was originally approved by the FDA in 2006.[L5440] |
| PubChem ID: | 56959 |
| CasNo: | 95635-55-5 |
| Repositioning for NAFLD: | Yes |
| SMILES: | COC1=CC=CC=C1OCC(O)CN1CCN(CC(=O)NC2=C(C)C=CC=C2C)CC1 |
| Structure: |
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| InChiKey: | XKLMZUWKNUAPSZ-UHFFFAOYSA-N |
| Molecular Weight: | 427.5365 |
| DrugBank Targets: | Sodium channel protein; Inward rectifier potassium channel; Voltage gated L-type calcium channel; Alpha-1 adrenergic receptors; Beta-1 adrenergic receptor; Fatty acid |
| DrugBank MoA: | The mechanism of action for ranolazine is not fully understood. at therapeutic levels can inhibit the cardiac late sodium 205 current (INa). However, the clinical significance this inhibition to angina symptoms is not confirmed.[L3580] Ranolazine inhibits sodium and potassium ion channel currents.[A174898] The effect of ranolazine on sodium channels is thought to be tissue-specific and dependent on frequency and voltage.[A174913] Ranolazine has been shown to have a small activity towards L-type calcium channels making it a weak direct vasodilator and presents a minimal direct effect on atrioventricular nodal conduction.[A174913] Some other mechanisms have been elucidated in which ranolazine presents antagonistic activity towards the alpha1- and beta1-adrenergic in animal models as well as an inhibitory profile against fatty acid oxidation.[A174898] |
| DrugBank Pharmacology: | Ranolazine exerts both antianginal and ischemic effects. It blocks IKr, the rapid portion of the delayed rectifier potassium current, and prolongs the QTc interval in a dose-related manner. The Ikr is important for cardiac repolarization.[L3580] |
| DrugBank Indication: | Ranolazine is indicated for the treatment of chronic angina. It can be used in conjunction with nitrates, beta-blockers, angiotensin receptor blockers, anti-platelet drugs, calcium channel blockers, lipid-lowering drugs, ACE inhibitors.[L3580] Ranolazine has also been used off-label for the treatment of some arrhythmias such as ventricular tachycardia, however, this use does not have a lot of supporting evidence.[A174940] The use of ranolazine has been researched in the treatment of acute coronary syndrome, microvascular coronary dysfunction, arrhythmia, and glycemic control.[A174898] |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L3268 | NCT00679939 | PHASE4 | COMPLETED | YES | 2008-04-21 | 2018-04-18 | Details |
| L4932 | NCT01089790 | PHASE3 | TERMINATED | NO | 2010-03 | 2011-09-21 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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