Sotalol

Summary

Sotalol (CHEMBL471) is an approved small-molecule β-adrenergic antagonist (ATC C07AA07) targeting ADRB1 and ADRB2; indicated across 9 conditions including cardiovascular disorder and atrial fibrillation.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C07AA07
• Targets: 2 (ADRB1, ADRB2)
• Indications: 9 conditions
• Clinical trials: 22
• Chemistry: 272.37 Da · C12H20N2O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL471
Name	Sotalol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5253
ChEBI	CHEBI:63622
ATC	C07AA07
Molecular formula	C12H20N2O3S
Molecular weight	272.37
InChIKey	ZBMZVLHSJCTVON-UHFFFAOYSA-N

SMILES: CC(C)NCC(C1=CC=C(C=C1)NS(=O)(=O)C)O

IUPAC name: N-[4-[1-hydroxy-2-(propan-2-ylamino)ethyl]phenyl]methanesulfonamide

ChEBI definition: A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both β-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.

Pharmacological roles (ChEBI): β-adrenergic antagonist, anti-arrhythmia drug.

Other ChEBI roles (chemical / environmental): environmental contaminant, xenobiotic.

Also known as: C07AA07, Darob mite, Dl-sotalol, Sotalol, sotalol, SID26751989, SID90341280, SID104171235, SOTALOL, SID144203812, SOTALOL HYDROCHLORIDE

Parent form; salt/anhydrous children: CHEMBL1700

Patent coverage: 5,501 distinct patent families (21,777 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
ADRB1	β1-adrenoceptor	Antagonist	6.1	0%	P08588
ADRB2	β2-adrenoceptor	Antagonist	6.9	0.4%	P07550

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Prelamin-A/C, Adrenergic receptor beta, Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, Beta-2 adrenergic receptor, Beta-2 adrenergic receptor.

Bioactivity

ChEMBL activities: 15 potent at pChembl ≥ 5 of 15 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	8.46	Potency	3.5	nM	CHEMBL_ACT_3651614
ADRB2	6.53	Ki	298.3	nM	CHEMBL_ACT_7807542
ADRB2	6.36	IC50	433.9	nM	CHEMBL_ACT_7807541
Q28044	6.24	Kd	580	nM	CHEMBL_ACT_499869
ADRB1	6.08	Ki	833.5	nM	CHEMBL_ACT_7807540
ADRB2	5.97	AC50	1078	nM	CHEMBL_ACT_25123029
ADRB1	5.84	IC50	1443	nM	CHEMBL_ACT_7807539
ADRB1	5.41	AC50	3902	nM	CHEMBL_ACT_25121964
P54833	5.3	IC50	5000	nM	CHEMBL_ACT_1124238
P54833	5.3	IC50	5000	nM	CHEMBL_ACT_631135
P54833	5.28	IC50	5200	nM	CHEMBL_ACT_440103
ADRB2	5.14	IC50	7200	nM	CHEMBL_ACT_440101
ADRB1	5.05	IC50	9000	nM	CHEMBL_ACT_1124237
ADRB1	5.05	IC50	8900	nM	CHEMBL_ACT_440102
ADRB1	5.05	IC50	9000	nM	CHEMBL_ACT_631134

Target pathways

Aggregated over 2 target gene(s): ADRB1, ADRB2.

Top Reactome pathways

16 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	2	ADRB1, ADRB2
Signaling by GPCR	2	ADRB1, ADRB2
Class A/1 (Rhodopsin-like receptors)	2	ADRB1, ADRB2
Amine ligand-binding receptors	2	ADRB1, ADRB2
GPCR downstream signalling	2	ADRB1, ADRB2
Adrenoceptors	2	ADRB1, ADRB2
G alpha (s) signalling events	2	ADRB1, ADRB2
GPCR ligand binding	2	ADRB1, ADRB2
Membrane Trafficking	1	ADRB2
Metabolism of proteins	1	ADRB2
Vesicle-mediated transport	1	ADRB2
Deubiquitination	1	ADRB2
Ub-specific processing proteases	1	ADRB2
Post-translational protein modification	1	ADRB2
Cargo recognition for clathrin-mediated endocytosis	1	ADRB2
Clathrin-mediated endocytosis	1	ADRB2

Dominant GO biological processes

GO term	Targets
diet induced thermogenesis	2
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	2
adenylate cyclase-activating G protein-coupled receptor signaling pathway	2
response to cold	2
positive regulation of cardiac muscle cell apoptotic process	2
heat generation	2
negative regulation of multicellular organism growth	2
positive regulation of MAPK cascade	2
brown fat cell differentiation	2
adenylate cyclase-activating adrenergic receptor signaling pathway	2
positive regulation of cold-induced thermogenesis	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
positive regulation of heart rate by epinephrine-norepinephrine	1
positive regulation of the force of heart contraction by epinephrine-norepinephrine	1

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
cardiovascular disorder	4	MONDO:0004995	EFO:0000319

6 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
atrial fibrillation	3	MONDO:0004981	EFO:0000275
heart failure	3	MONDO:0005252	EFO:0003144
ventricular fibrillation	3	MONDO:0000190	EFO:0004287
ventricular tachycardia	3	MONDO:0005477	EFO:0005306
myocardial infarction	3	MONDO:0005068	EFO:0000612
heart disorder	3	MONDO:0005267	EFO:0003777

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 22.

Phase distribution

Phase	Trials
Not specified	8
PHASE3	7
PHASE4	4
PHASE1	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02347111	PHASE4	RECRUITING	Pharmacogenetic Study of Antiarrhythmic Drugs for Atrial Fibrillation
NCT02145546	PHASE4	UNKNOWN	Antiarrhythmic Drugs Assessment in Preventing Atrial Fibrillation
NCT03895411	PHASE4	UNKNOWN	Efficacy and Safety of Sotalol in Children With Arrhythmia
NCT05418036	PHASE4	UNKNOWN	Safety Assessment for Sotalol Protocol in Outpatient Unit
NCT00000464	PHASE3	COMPLETED	Cardiac Arrest in Seattle: Conventional Versus Amiodarone Drug Evaluation (CASCADE)
NCT00000518	PHASE3	COMPLETED	Electrophysiologic Study Versus Electrocardiographic Monitoring (ESVEM)
NCT00000531	PHASE3	COMPLETED	Antiarrhythmics Versus Implantable Defibrillators (AVID)
NCT00000556	PHASE3	COMPLETED	Atrial Fibrillation Follow-up Investigation of Rhythm Management (AFFIRM)
NCT00007605	PHASE3	COMPLETED	Comparing the Effects of Amiodarone, Sotalol, and Placebo in Maintaining Sinus Rhythm in Patients With Atrial Fibrillation Converted to Sinus Rhythm
NCT00035451	PHASE3	COMPLETED	Efficacy and Safety Evaluation of Azimilide or Sotalol vs Placebo for Treatment of Patients With Atrial Fibrillation.
NCT02624765	PHASE3	COMPLETED	Prospective Randomized Clinical Trial of Fetal Atrial Flutter & Supraventricular Tachycardia Therapy (FAST RCT)
NCT00773201	PHASE1	COMPLETED	Genetic Sources of Variability of the Adaptation of the Ventricular Repolarisation
NCT02153437	PHASE1	TERMINATED	Study of the Effects of BMS-919373 on the Electrical Activity of the Heart Using Pacemakers
NCT03799536	PHASE1	COMPLETED	Bioequivalence Study of Sotalol, Tablets, 160 mg (Pharmtechnology LLC, Belarus), and Sotalex ®, Tablets, 160 mg (Bristol-Myers Squibb GmbH & Co. KGaA, Germany), in Healthy Volunteers Under Fasting Conditions
NCT06322017	Not specified	RECRUITING	Prospective Multicenter Randomized and Controlled Study Evaluating the Benefit of Early Pulmonary Vein Isolation Compared to Usual Treatment in Patients Aged Over 75 Years and Presenting With Atrial Fibrillation
NCT06669299	Not specified	RECRUITING	Non-Invasive Programmed Stimulation (NIPS) to Guide the Subsequent VT Therapeutic Strategies
NCT01576042	Not specified	TERMINATED	Pilot Study of Catheter Ablation for Ventricular Tachycardia in Patients With an Implantable Cardioverter Defibrillator
NCT02294955	Not specified	UNKNOWN	Catheter Ablation Compared With Pharmacological Therapy for Atrial Fibrillation (CAPTAF Trial)
NCT03845010	Not specified	COMPLETED	Elimination of VPB With Ablation Versus Anti-arrhythmic Drug Treatment
NCT04128878	Not specified	COMPLETED	Improvement in Endothelial Dysfunction After Initiation of Anti-arrhythmic Therapy in Atrial Fibrillation Patients
NCT05247320	Not specified	COMPLETED	Prospective Evaluation Analysis and Kinetics Registry
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

PharmGKB dosing guidelines (3) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for sotalol and CYP2D6	DPWG	CYP2D6
Annotation of CPIC Guideline for acebutolol, atenolol, betaxolol, biso	CPIC	ADRA2C;ADRB1;GRK4;GRK5
Annotation of CPIC Guideline for carvedilol, labetalol, nadolol, pindo	CPIC	ADRB2

PharmGKB also curates 1 clinical and 11 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.

238 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
Desloratadine	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
OLODATEROL	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
Pramipexole	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
TAMSULOSIN	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
ACEBUTOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ALBUTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ARFORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ATENOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BENPERIDOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BETAXOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BISOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CARTEOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CELIPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DARIFENACIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DOBUTAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DOMPERIDONE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
EPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ESMOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FENOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
INDACATEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
LABETALOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
LEVOBUNOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
METOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
MONTELUKAST	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NADOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NEBIVOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NOREPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
OXPRENOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PHENYLEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PINDOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRACTOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRENYLAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRIMAQUINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PROPAFENONE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PROPRANOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RANOLAZINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RIFAMPIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RIFAXIMIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RITODRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SALMETEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
TAMOXIFEN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
TEGASEROD	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
TIMOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
TIOCONAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
VALDECOXIB	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
VILANTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
AROTINOLOL	ChEMBL	Phase 3	ADRB1, ADRB2
LISURIDE	ChEMBL	Phase 3	ADRB1, ADRB2
OTILONIUM BROMIDE	ChEMBL	Phase 3	ADRB1, ADRB2
PROCATEROL	ChEMBL	Phase 3	ADRB1, ADRB2
URAPIDIL	ChEMBL	Phase 3	ADRB1, ADRB2
ABEDITEROL	ChEMBL	Phase 2	ADRB1, ADRB2
ALPRENOLOL	ChEMBL	Phase 2	ADRB1, ADRB2
AMOSULALOL	ChEMBL	Phase 2	ADRB1, ADRB2
BENZETHONIUM	ChEMBL	Phase 2	ADRB1, ADRB2
BEVANTOLOL	ChEMBL	Phase 2	ADRB1, ADRB2
BOPINDOLOL	ChEMBL	Phase 2	ADRB1, ADRB2
CIMATEROL	ChEMBL	Phase 2	ADRB1, ADRB2
CLENBUTEROL	ChEMBL	Phase 2	ADRB1, ADRB2
CLORPRENALINE	ChEMBL	Phase 2	ADRB1, ADRB2
DENOPAMINE	ChEMBL	Phase 2	ADRB1, ADRB2
DEXPROPRANOLOL	ChEMBL	Phase 2	ADRB1, ADRB2
DIHYDREXIDINE	ChEMBL	Phase 2	ADRB1, ADRB2
DOMIPHEN	ChEMBL	Phase 2	ADRB1, ADRB2
FLESTOLOL	ChEMBL	Phase 2	ADRB1, ADRB2
LEVISOPRENALINE	ChEMBL	Phase 2	ADRB1, ADRB2
LEVOPROPRANOLOL	ChEMBL	Phase 2	ADRB1, ADRB2
LYSERGIDE	ChEMBL	Phase 2	ADRB1, ADRB2
MILVETEROL	ChEMBL	Phase 2	ADRB1, ADRB2
NEMONAPRIDE	ChEMBL	Phase 2	ADRB1, ADRB2
NYLIDRIN	ChEMBL	Phase 2	ADRB1, ADRB2
RAFABEGRON	ChEMBL	Phase 2	ADRB1, ADRB2
SIBENADET	ChEMBL	Phase 2	ADRB1, ADRB2
SOFALCONE	ChEMBL	Phase 2	ADRB1, ADRB2
SOLABEGRON	ChEMBL	Phase 2	ADRB1, ADRB2
SPIRAMIDE	ChEMBL	Phase 2	ADRB1, ADRB2
TALINOLOL	ChEMBL	Phase 2	ADRB1, ADRB2
TRETOQUINOL	ChEMBL	Phase 2	ADRB1, ADRB2
TULOBUTEROL	ChEMBL	Phase 2	ADRB1, ADRB2
XAMOTEROL	ChEMBL	Phase 2	ADRB1, ADRB2