Repositioning Candidate Details
| Candidate ID: | R0110 |
| Source ID: | DB00308 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Ibutilide |
| Synonyms: | Ibutilide; N-(4-{4-[ethyl(heptyl)amino]-1-hydroxybutyl}phenyl)methanesulfonamide |
| Molecular Formula: | C20H36N2O3S |
| SMILES: | CCCCCCCN(CC)CCCC(O)C1=CC=C(NS(C)(=O)=O)C=C1 |
| Structure: |
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| DrugBank Description: | Ibutilide is a Class III antiarrhythmic agent available in intravenous formulations. It is indicated for the conversion of acute atrial flutter and recent onset atrial fibrillation to normal sinus rhythm (NSR). |
| CAS Number: | 122647-31-8 |
| Molecular Weight: | 384.576 |
| DrugBank Indication: | Indicated for the rapid conversion of atrial fibrillation or atrial flutter of recent onset to sinus rhythm. |
| DrugBank Pharmacology: | Ibutilide prolongs the action potential duration and increases both atrial and ventricular refractoriness in vivo, i.e., class III electrophysiologic effects. Voltage clamp studies indicate that ibutilide, at nanomolar concentrations, delays repolarization by activation of a slow, inward current (predominantly sodium), rather than by blocking outward potassium currents, which is the mechanism by which most other class III antiarrhythmics act. |
| DrugBank MoA: | Ibutilide is a 'pure' class III antiarrhythmic drug, used intravenously against atrial flutter and fibrillation. At a cellular level it exerts two main actions: induction of a persistent Na+ current sensitive to dihydropyridine Ca<sup>2+</sup> channel blockers and potent inhibition of the cardiac rapid delayed rectifier K<sup>+</sup> current, by binding within potassium channel pores. In other words, Ibutilide binds to and alters the activity of hERG potassium channels, delayed inward rectifier potassium (IKr) channels and L-type (dihydropyridine sensitive) calcium channels |
| Targets: | Voltage-dependent L-type calcium channel subunit alpha-1C activator; Voltage-dependent L-type calcium channel subunit beta-1 activator; Potassium voltage-gated channel subfamily H member 2 inhibitor; Voltage-dependent calcium channel subunit alpha-2/delta-1 activator; Voltage-dependent calcium channel gamma-1 subunit activator; Potassium channel subfamily K member 1 inhibitor; Potassium channel subfamily K member 6 inhibitor; Potassium voltage-gated channel subfamily H member 6 inhibitor; Potassium voltage-gated channel subfamily H member 7 inhibitor; ATP-sensitive inward rectifier potassium channel 11 inhibitor |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| 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 |