Dronedarone
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Also known as DronedaronaSR-33589SR33589SID144206559SID170465064Dronedarone HCl (Multaq)
Summary
Dronedarone (CHEMBL184412) is an approved small-molecule anti-arrhythmia drug (ATC C01BD07) targeting KCNA5; indicated across 4 conditions including atrial fibrillation and congestive heart failure.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: C01BD07
- Targets: 1 (KCNA5)
- Indications: 4 conditions
- Clinical trials: 27
- Chemistry: 556.8 Da · C31H44N2O5S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL184412 |
| Name | Dronedarone |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 208898 |
| ChEBI | CHEBI:50659 |
| ATC | C01BD07 |
| Molecular formula | C31H44N2O5S |
| Molecular weight | 556.8 |
| InChIKey | ZQTNQVWKHCQYLQ-UHFFFAOYSA-N |
SMILES: CCCCC1=C(C2=C(O1)C=CC(=C2)NS(=O)(=O)C)C(=O)C3=CC=C(C=C3)OCCCN(CCCC)CCCC
IUPAC name: N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-1-benzofuran-5-yl]methanesulfonamide
ChEBI definition: A member of the class of 1-benzofurans used for the treatment of cardiac arrhythmias.
Pharmacological roles (ChEBI): anti-arrhythmia drug.
Other ChEBI roles (chemical / environmental): environmental contaminant, xenobiotic.
Also known as: Dronedarona, Dronedarone, SR-33589, SR33589, SID144206559, SID170465064, dronedarone, DRONEDARONE, Dronedarone HCl (Multaq)
Parent form; salt/anhydrous children: CHEMBL1201729
Patent coverage: 1,056 distinct patent families (3,608 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,604 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| KCNA5 | Kv1.5 | Inhibition | 5.63 | 0.2% | P22460 |
Broader ChEMBL bioactivity targets: 20 (assay-derived). Sample: Alpha-2A adrenergic receptor, D(1A) dopamine receptor, Estrogen receptor, Thromboxane A2 receptor, Progesterone receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter.
Bioactivity
ChEMBL activities: 17 potent at pChembl ≥ 5 of 21 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| KCNH2 | 6.5 | IC50 | 316.2 | nM | CHEMBL_ACT_5218995 |
| O35505 | 6.4 | IC50 | 400 | nM | CHEMBL_ACT_15777525 |
| DRD3 | 6.19 | AC50 | 641.8 | nM | CHEMBL_ACT_25194244 |
| PGR | 6.19 | AC50 | 639.7 | nM | CHEMBL_ACT_25204004 |
| ADORA3 | 5.81 | AC50 | 1537 | nM | CHEMBL_ACT_25198487 |
| SLC6A3 | 5.76 | AC50 | 1731 | nM | CHEMBL_ACT_25124672 |
| HTR1A | 5.76 | AC50 | 1721 | nM | CHEMBL_ACT_25164737 |
| CHRM2 | 5.62 | AC50 | 2386 | nM | CHEMBL_ACT_25195449 |
| KCNH2 | 5.52 | IC50 | 3000 | nM | CHEMBL_ACT_1449636 |
| OPRM1 | 5.51 | AC50 | 3094 | nM | CHEMBL_ACT_25157888 |
| SLC6A4 | 5.48 | AC50 | 3312 | nM | CHEMBL_ACT_25151040 |
| SLC6A2 | 5.4 | AC50 | 3984 | nM | CHEMBL_ACT_25145713 |
| ESR1 | 5.33 | AC50 | 4736 | nM | CHEMBL_ACT_25138571 |
| DRD1 | 5.27 | AC50 | 5400 | nM | CHEMBL_ACT_25114923 |
| ADRA1A | 5.23 | AC50 | 5924 | nM | CHEMBL_ACT_25218605 |
| Q8R4B8 | 5.17 | IC50 | 6840 | nM | CHEMBL_ACT_23165786 |
| CHRM1 | 5.11 | AC50 | 7758 | nM | CHEMBL_ACT_25209963 |
Target pathways
Aggregated over 1 target gene(s): KCNA5.
Top Reactome pathways
6 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Neuronal System | 1 | KCNA5 |
| Potassium Channels | 1 | KCNA5 |
| Voltage gated Potassium channels | 1 | KCNA5 |
| Muscle contraction | 1 | KCNA5 |
| Phase 3 - rapid repolarisation | 1 | KCNA5 |
| Cardiac conduction | 1 | KCNA5 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| action potential | 1 |
| response to hypoxia | 1 |
| potassium ion transport | 1 |
| Notch signaling pathway | 1 |
| response to mechanical stimulus | 1 |
| regulation of vasoconstriction | 1 |
| regulation of membrane potential | 1 |
| response to hydrogen peroxide | 1 |
| regulation of insulin secretion | 1 |
| protein homooligomerization | 1 |
| negative regulation of cytosolic calcium ion concentration | 1 |
| potassium ion homeostasis | 1 |
| response to hyperoxia | 1 |
| membrane hyperpolarization | 1 |
| regulation of atrial cardiac muscle cell membrane repolarization | 1 |
Indications & clinical
Indications
4 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| atrial fibrillation | 3 | MONDO:0004981 | EFO:0000275 |
| congestive heart failure | 3 | MONDO:0005009 | EFO:0000373 |
| atrial flutter | 3 | MONDO:0005310 | EFO:0003911 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 27.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 10 |
| PHASE3 | 8 |
| Not specified | 6 |
| PHASE2 | 2 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT07270848 | PHASE4 | NOT_YET_RECRUITING | Dronedarone Rhythm Intervention for Early Atrial Fibrillation |
| NCT01026090 | PHASE4 | TERMINATED | Dronedarone Pattern of Use in Patients Scheduled for Elective Cardioversion (ELECTRA) |
| NCT01047566 | PHASE4 | COMPLETED | Effect of Addition of Dronedarone to Standard Rate Control Therapy on Ventricular Rate During Persistent Atrial Fibrillation (AFRODITE) |
| NCT01070667 | PHASE4 | UNKNOWN | Dronedarone in Pacemakers Patients With Paroxysmal Atrial Fibrillation |
| NCT01135017 | PHASE4 | TERMINATED | Effects of Dronedarone on Atrial Fibrillation Burden in Subjects With Permanent Pacemakers |
| NCT01140581 | PHASE4 | COMPLETED | Optimal Timing of Dronedarone Initiation After Conversion in Patients With Persistent Atrial Fibrillation |
| NCT01198873 | PHASE4 | TERMINATED | Effects of Dronedarone on Cardiac Geometry and Function in Patients With Atrial Fibrillation and Left Atrial Enlargement |
| NCT01199081 | PHASE4 | COMPLETED | Pharmacokinetics and Optimal Timing of Dronedarone Initiation Following Long-term Amiodarone in Patients With Paroxysmal or Persistent Atrial Fibrillation |
| NCT05130268 | PHASE4 | COMPLETED | Early Dronedarone Versus Usual Care to Improve Outcomes in Persons With Newly Diagnosed Atrial Fibrillation |
| NCT05655468 | PHASE4 | UNKNOWN | Effect of Prolonged Use of Dronedarone on Recurrence in Patients With Non-paroxysmal Atrial Fibrillation After Radiofrequency Ablation |
| NCT00174785 | PHASE3 | COMPLETED | A Trial With Dronedarone to Prevent Hospitalization or Death in Patients With Atrial Fibrillation |
| NCT00259376 | PHASE3 | COMPLETED | American-Australian-African Trial With Dronedarone in Patients With Atrial Fibrillation or Atrial Flutter for the Maintenance of Sinus Rhythm |
| NCT00259428 | PHASE3 | COMPLETED | EURopean Trial In Atrial Fibrillation(AF) or Flutter (AFL) Patients Receiving Dronedarone for the maIntenance of Sinus Rhythm (EURIDIS) |
| NCT00489736 | PHASE3 | COMPLETED | Efficacy & Safety of Dronedarone Versus Amiodarone for the Maintenance of Sinus Rhythm in Patients With Atrial Fibrillation |
| NCT00696631 | PHASE3 | TERMINATED | European Trial of Dronedarone in Moderate to Severe Congestive Heart Failure |
| NCT00697086 | PHASE3 | COMPLETED | European Study of Dronedarone in Atrial Fibrillation |
| NCT01151137 | PHASE3 | TERMINATED | Permanent Atrial fibriLLAtion Outcome Study Using Dronedarone on Top of Standard Therapy |
| NCT01182376 | PHASE3 | COMPLETED | SOAR: Study Observing Antiarrhythmic Remodelling Using LGE-MRI |
| NCT03905759 | PHASE2/PHASE3 | UNKNOWN | Prophylaxis Against Postoperative Atrial Fibrillation in Patients Undergoing On-pump CABG |
| NCT01213368 | PHASE2 | COMPLETED | Dose Ranging Study of Dronedarone for the Control of Ventricular Rate in Japanese Patients With Permanent Atrial Fibrillation |
| NCT01522651 | PHASE2 | COMPLETED | Study to Evaluate the Effect of Ranolazine and Dronedarone When Given Alone and in Combination in Patients With Paroxysmal Atrial Fibrillation |
| NCT06096337 | Not specified | ACTIVE_NOT_RECRUITING | Pulsed Field Ablation (PFA) vs Anti-Arrhythmic Drug (AAD) Therapy as a First Line Treatment for Persistent Atrial Fibrillation |
| NCT01266681 | Not specified | UNKNOWN | Amiodarone Compared to Dronedarone , Post Cardioversion Maintenance of Sinus Rhythm |
| NCT01430806 | Not specified | UNKNOWN | Dronaderone to Prevent Recurrent Implantable Cardioverter Defibrillator (ICD) Shocks |
| NCT01991119 | Not specified | COMPLETED | Efficacy of Propafenone Versus Dronedarone for the Maintenance of Sinus Rhythm in Patients With Atrial Fibrillation |
| NCT02294955 | Not specified | UNKNOWN | Catheter Ablation Compared With Pharmacological Therapy for Atrial Fibrillation (CAPTAF Trial) |
| NCT05279833 | Not specified | COMPLETED | Systematic Review and Meta-Analysis of Multaq® for Safety in Atrial Fibrillation |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
10 molecules share ≥1 primary target. Top 10 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| FLECAINIDE | ChEMBL + PubChem | Phase 4 (approved) | KCNA5 |
| QUINIDINE | ChEMBL + PubChem | Phase 4 (approved) | KCNA5 |
| NIFEDIPINE | ChEMBL | Phase 4 (approved) | KCNA5 |
| SERTINDOLE | ChEMBL | Phase 4 (approved) | KCNA5 |
| VERNAKALANT | ChEMBL | Phase 4 (approved) | KCNA5 |
| BMS-919373 | ChEMBL | Phase 2 | KCNA5 |
| Belzutifan | PubChem | Approved | KCNA5 |
| dalfampridine | PubChem | Approved | KCNA5 |
| Diltiazem | PubChem | Approved | KCNA5 |
| Lidocaine | PubChem | Approved | KCNA5 |
Related Atlas pages
- Genes: KCNA5
- Diseases: atrial fibrillation, congestive heart failure, atrial flutter
- Drugs: Flecainide, Quinidine, Nifedipine, Sertindole, Vernakalant, Belzutifan, dalfampridine, Diltiazem, Lidocaine