Bisoprolol

Summary

Bisoprolol (CHEMBL645) is an approved small-molecule antihypertensive agent (ATC C07AB07) targeting ADRB1; indicated across 8 conditions including cardiovascular disorder and hypertensive disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C07AB07
• Targets: 1 (ADRB1)
• Indications: 8 conditions
• Clinical trials: 62
• Chemistry: 325.4 Da · C18H31NO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL645
Name	Bisoprolol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	2405
ChEBI	CHEBI:3127
ATC	C07AB07
Molecular formula	C18H31NO4
Molecular weight	325.4
InChIKey	VHYCDWMUTMEGQY-UHFFFAOYSA-N

SMILES: CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O

IUPAC name: 1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-ol

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

Also known as: Bisoprolol, CL 297,939, EMD 33 512, SID90341096, SID26751965, SID29215032, SID50104637, bisoprolol, BISOPROLOL, SID174007419, (+/-)-Bisoprolol, rac-Bisoprolol

Parent form; salt/anhydrous children: CHEMBL1472989

Patent coverage: 5,206 distinct patent families (20,416 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	7.9	0%	P08588

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, Beta-3 adrenergic receptor, Beta-1 adrenergic receptor.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 7 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P34971	8.28	Ki	5.3	nM	CHEMBL_ACT_19255938
ADRB1	7	AC50	99	nM	CHEMBL_ACT_25121442
ADRB2	6.82	Kd	150	nM	CHEMBL_ACT_19403982
ADRB2	6.6	Ki	250	nM	CHEMBL_ACT_19255922
ADRB2	5.75	AC50	1800	nM	CHEMBL_ACT_25122610

Target pathways

Aggregated over 1 target gene(s): ADRB1.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	ADRB1
Signaling by GPCR	1	ADRB1
Class A/1 (Rhodopsin-like receptors)	1	ADRB1
Amine ligand-binding receptors	1	ADRB1
GPCR downstream signalling	1	ADRB1
Adrenoceptors	1	ADRB1
G alpha (s) signalling events	1	ADRB1
GPCR ligand binding	1	ADRB1

Dominant GO biological processes

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

3 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
hypertensive disorder	3	MONDO:0005044	EFO:0000537
atrial fibrillation	3	MONDO:0004981	EFO:0000275
breast neoplasm	2	MONDO:0021100	MONDO:0007254

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

Clinical trials

Total trials: 62.

Phase distribution

Phase	Trials
PHASE4	32
Not specified	12
PHASE3	8
PHASE1	5
EARLY_PHASE1	2
PHASE2/PHASE3	1
PHASE2	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03778554	PHASE4	ACTIVE_NOT_RECRUITING	Danish Trial of Beta Blocker Treatment After Myocardial Infarction Without Reduced Ejection Fraction
NCT05569382	PHASE4	RECRUITING	Treatment Effects of Bisoprolol and Verapamil in Symptomatic Patients With Non-obstructive Hypertrophic Cardiomyopathy
NCT06562582	PHASE4	RECRUITING	STunning in Acute Myocardial Infarction - BAS
NCT07103655	PHASE4	NOT_YET_RECRUITING	The Therapeutic Value of Mavacamten in Hypertrophic Cardiomyopathy With Mid-to-Apical Left Ventricular Obstruction
NCT00391846	PHASE4	COMPLETED	Evaluation of Heart Failure Treatment Guided by N-terminal Pro B-type Natriuretic Peptide (NTproBNP) vs Clinical Symptoms and Signs Alone
NCT00517725	PHASE4	COMPLETED	Nebivolol Versus Bisoprolol Versus Carvedilol in Heart Failure
NCT01066039	PHASE4	COMPLETED	Phase 4 Study to Assess the Effect of Bisoprolol on Glycemic Level in Type II Diabetic Subjects With Suboptimal Blood Pressure Control
NCT01079962	PHASE4	COMPLETED	An Active-controlled, Clinical Trial to Assess Central Hemodynamic Effects of Bisoprolol in Hypertensive Patients (Central Hemodynamic Assessment Measured in Patient With HypertensION [CHAMPION])
NCT01104558	PHASE4	COMPLETED	Association Between Genetic Polymorphism of Beta-adrenergic Receptor and Effects of Bisoprolol in Korean Heart Failure Patients.
NCT01190436	PHASE4	COMPLETED	A 12-week, Multicentric Study to Evaluate the Safety and Efficacy of Bisoprolol in Filipino Hypertensive Subjects With Diabetes
NCT01243827	PHASE4	UNKNOWN	Comparison of Effect of cARvedilol Compared To bISoprolol on cenTral Pulse Pressure in Hypertension (ARTIST) Study
NCT01251146	PHASE4	COMPLETED	A Randomized Controlled Study to Assess the Effects of Bisoprolol and Atenolol on Resting Heart Rate and Sympathetic Nervous System’s Activity in Subjects With Essential Hypertension
NCT01508325	PHASE4	COMPLETED	Comparison of Bisoprolol With Metoprolol Succinate Sustained-release on Heart Rate and Blood Pressure in Hypertensive Patients
NCT01579058	PHASE4	TERMINATED	Effect of Bisoprolol on Progression of Aortic Stenosis
NCT01656005	PHASE4	COMPLETED	Beta Blocker Therapy in Moderate to Severe COPD
NCT01762436	PHASE4	COMPLETED	Effects of Bisoprolol and Atenolol on Sympathetic Nervous Activity and Central Aortic Pressure in Patients With Essential Hypertension
NCT01939509	PHASE4	COMPLETED	Hemodynamic Changes of Patients Receiving Atenolol/Bisoprolol
NCT02171988	PHASE4	COMPLETED	Effect of Medical Treatment and Prognosis of Postural Orthostatic Tachycardia Syndrome (POTS)
NCT02369081	PHASE4	UNKNOWN	Optimum Treatment for Drug-Resistant Hypertension
NCT02380053	PHASE4	COMPLETED	Chronic Beta-blockade and Cardiopulmonary Exercise in COPD
NCT02391337	PHASE4	COMPLETED	Rate Control Therapy Evaluation in Permanent Atrial Fibrillation (RATE-AF)
NCT02398929	PHASE4	COMPLETED	BRAVE Study With Uncontrolled Essential Hypertension (BRAVE Study)
NCT02832973	PHASE4	COMPLETED	Sequential Nephron Blockade vs. Dual Blockade Renin-angiotensin System + Bisoprolol in Resistant Arterial Hypertension
NCT03026088	PHASE4	TERMINATED	Efficacy of Oral Bisoprolol on Heart Rate Reduction in Chinese Chronic Heart Failure Participants
NCT03276598	PHASE4	COMPLETED	A Study on Molecular Genetics of Drug Responsiveness in Essential Hypertension
NCT03278509	PHASE4	UNKNOWN	Evaluation of Decreased Usage of Betablockers After Myocardial Infarction in the SWEDEHEART Registry (REDUCE-SWEDEHEART)
NCT03800264	PHASE4	COMPLETED	Bisoprolol Versus Corticosteroid and Bisoprolol Combination for Prophylaxis Against Atrial Fibrillation After on Pump Coronary Artery Bypass Surgery
NCT03850093	PHASE4	COMPLETED	Preoperative Gabapentin Versus Bisoprolol for Hemodynamic Optimization During Sinus Surgery
NCT05294887	PHASE4	UNKNOWN	Randomized Trial to Examine a Differential Therapeutic Response in Symptomatic Patients With Non-obstructive Coronary Artery Disease
NCT05730413	PHASE4	UNKNOWN	Once Versus Twice Bisoprolol Dosage Regimen in Prevention of Atrial Fibrillation Post Coronary Artery Bypass Graft Surgery
NCT06035978	PHASE4	UNKNOWN	Determination of Drug Levels for Pharmacotherapy of Heart Failure
NCT07327749	PHASE4	COMPLETED	Comparing Bisoprolol and Valsartan-Amlodipine for Hypertension
NCT06276127	PHASE3	NOT_YET_RECRUITING	Oral Bisoprolol Vs IV Diltiazem in Atrial Fibrillation or Flutter With Rapid Ventricular Rate.
NCT00323973	PHASE3	COMPLETED	Chagas Cardiomyopathy Bisoprolol Intervention Study: Charity
NCT00562952	PHASE2/PHASE3	COMPLETED	Nt-proBNP Guided Primary Prevention of CV Events in Diabetic Patients
NCT01977794	PHASE3	COMPLETED	Fixed Dose Combination of Bisoprolol and Amlodipine in the Treatment of Hypertension
NCT02236806	PHASE3	UNKNOWN	Cardiotoxicity Prevention in Breast Cancer Patients Treated With Anthracyclines and/or Trastuzumab
NCT03485482	PHASE3	COMPLETED	Pharmacokinetic Drug-Drug Interaction Between Bisoprolol and Ivabradine in Healthy Volunteers
NCT03917914	PHASE3	COMPLETED	Preventing Adverse Cardiac Events in COPD
NCT05175066	PHASE3	COMPLETED	Bisoprolol Administration to Prevent Anthracycline-induced Cardiotoxicity
NCT05540600	PHASE3	UNKNOWN	Left Atrium Reservoir Function Modulation in Patients With Atrial Fibrillation: Digoxin Versus Beta Blocker
NCT00702156	PHASE2	TERMINATED	Bisoprolol in Patients With Heart Failure and Chronic Obstructive Pulmonary Disease
NCT01246037	PHASE1/PHASE2	UNKNOWN	Beta-blockers in i-PAH
NCT01284868	PHASE1	COMPLETED	A Study in Healthy Young Men to Look at What Drives the Cardiovascular Effects After Dosing With Mirabegron.
NCT01741623	PHASE1	COMPLETED	Bioequivalence Study of Bisoprolol Fumarate Tablet 10 mg Under Fasting Condition
NCT01744873	PHASE1	COMPLETED	Bioequivalence Study of Bisoprolol Fumarate Tablet 10 mg Under Fed Condition
NCT02256722	PHASE1	COMPLETED	In Vivo Specificity of KUC 7483 CL Co-administered With Bisoprolol, Propranolol, and Acipimox in Healthy Male Subjects
NCT03226275	PHASE1	COMPLETED	Bioequivalence Trial of Concor AM® vs Bisoprolol and Amlodipine in Chinese Participants
NCT02106286	EARLY_PHASE1	COMPLETED	Effects of Beta-blockade on Cardiopulmonary Exercise Testing
NCT04356196	EARLY_PHASE1	UNKNOWN	Comparative Study Between the Efficacy of Verapamil and Bisoprolol on Reduction of Bleeding During Endoscopic Sinus Surgery Under General Anaesthesia.
NCT07029906	Not specified	RECRUITING	pErsonalised Nocebo Assessment of Beta-blockEr Symptoms in Heart Failure
NCT07491718	Not specified	RECRUITING	Manganese-enhanced Magnetic Resonance Imaging in Takotsubo Cardiomyopathy
NCT07568574	Not specified	ENROLLING_BY_INVITATION	Impact of Medically Supervised Performance-Enhancing Substances (PES) on Elite Athletes
NCT00292162	Not specified	COMPLETED	Curing Atrial Fibrillation in Heart Failure
NCT00382421	Not specified	COMPLETED	Study to Investigate Effects of Antiischemic Drug Therapy in Silent Ischemia
NCT00882856	Not specified	COMPLETED	Treating Clozapine-induced Sinustachycardia With Bisoprolol
NCT01273298	Not specified	COMPLETED	Effects of Cardioselective β-blockers on Dynamic Hyperinflation in COPD
NCT02137733	Not specified	UNKNOWN	The Cardiac Insufficiency BIsoprolol Study in Japanese Patients With Chronic Heart Failure (CIBIS-J)
NCT02355821	Not specified	COMPLETED	Comparative Effects of Moxonidine on Bone Metabolism, Vascular and Cellular Aging in Hypertensive Postmenopausal Women
NCT03701880	Not specified	UNKNOWN	Early Use of Ivabradine in Heart Failure
NCT03730116	Not specified	COMPLETED	Assessment of the Efficacy and Tolerability of the Fixed-dose Combination of Bisoprolol/Perindopril
NCT04513509	Not specified	COMPLETED	Rate Control in Patients With 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 bisoprolol and CYP2D6	DPWG	CYP2D6
Annotation of CPIC Guideline for acebutolol, betaxolol, bisoprolol, ca	CPIC	CYP2D6
Annotation of CPIC Guideline for acebutolol, atenolol, betaxolol, biso	CPIC	ADRA2C;ADRB1;GRK4;GRK5

PharmGKB also curates 2 clinical and 16 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.

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

Molecule	Source	Status	Shared targets
OLODATEROL	ChEMBL + PubChem	Phase 4 (approved)	ADRB1
TAMSULOSIN	ChEMBL + PubChem	Phase 4 (approved)	ADRB1
ACEBUTOLOL	ChEMBL	Phase 4 (approved)	ADRB1
ALBUTEROL	ChEMBL	Phase 4 (approved)	ADRB1
AMIODARONE	ChEMBL	Phase 4 (approved)	ADRB1
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1
ARFORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRB1
ATENOLOL	ChEMBL	Phase 4 (approved)	ADRB1
AZELASTINE	ChEMBL	Phase 4 (approved)	ADRB1
BENFLUOREX	ChEMBL	Phase 4 (approved)	ADRB1
BENPERIDOL	ChEMBL	Phase 4 (approved)	ADRB1
BENZBROMARONE	ChEMBL	Phase 4 (approved)	ADRB1
BEPRIDIL	ChEMBL	Phase 4 (approved)	ADRB1
BETAXOLOL	ChEMBL	Phase 4 (approved)	ADRB1
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRB1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	ADRB1
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRB1
CARTEOLOL	ChEMBL	Phase 4 (approved)	ADRB1
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRB1
CELIPROLOL	ChEMBL	Phase 4 (approved)	ADRB1
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	ADRB1
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	ADRB1
CINACALCET	ChEMBL	Phase 4 (approved)	ADRB1
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRB1
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRB1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRB1
CODEINE	ChEMBL	Phase 4 (approved)	ADRB1
DARIFENACIN	ChEMBL	Phase 4 (approved)	ADRB1
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	ADRB1
DECITABINE	ChEMBL	Phase 4 (approved)	ADRB1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	ADRB1
DOBUTAMINE	ChEMBL	Phase 4 (approved)	ADRB1
DOMPERIDONE	ChEMBL	Phase 4 (approved)	ADRB1
DULOXETINE	ChEMBL	Phase 4 (approved)	ADRB1
EBASTINE	ChEMBL	Phase 4 (approved)	ADRB1
ECONAZOLE	ChEMBL	Phase 4 (approved)	ADRB1
EFAVIRENZ	ChEMBL	Phase 4 (approved)	ADRB1
EPALRESTAT	ChEMBL	Phase 4 (approved)	ADRB1
EPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ADRB1
ESMOLOL	ChEMBL	Phase 4 (approved)	ADRB1
FENOTEROL	ChEMBL	Phase 4 (approved)	ADRB1
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	ADRB1
FORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1
INDACATEROL	ChEMBL	Phase 4 (approved)	ADRB1
INDOCYANINE GREEN ACID FORM	ChEMBL	Phase 4 (approved)	ADRB1
ISOCONAZOLE	ChEMBL	Phase 4 (approved)	ADRB1
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	ADRB1
LABETALOL	ChEMBL	Phase 4 (approved)	ADRB1
LASOFOXIFENE	ChEMBL	Phase 4 (approved)	ADRB1
LEVOBUNOLOL	ChEMBL	Phase 4 (approved)	ADRB1
LORCASERIN	ChEMBL	Phase 4 (approved)	ADRB1
METARAMINOL	ChEMBL	Phase 4 (approved)	ADRB1
METHYLERGONOVINE	ChEMBL	Phase 4 (approved)	ADRB1
METOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1
MICONAZOLE	ChEMBL	Phase 4 (approved)	ADRB1
MONTELUKAST	ChEMBL	Phase 4 (approved)	ADRB1
NADOLOL	ChEMBL	Phase 4 (approved)	ADRB1
NAFTOPIDIL	ChEMBL	Phase 4 (approved)	ADRB1
NEBIVOLOL	ChEMBL	Phase 4 (approved)	ADRB1
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	ADRB1
NOREPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1
NOSCAPINE	ChEMBL	Phase 4 (approved)	ADRB1
OXPRENOLOL	ChEMBL	Phase 4 (approved)	ADRB1
OXYPERTINE	ChEMBL	Phase 4 (approved)	ADRB1
PHENYLEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRB1
PINDOLOL	ChEMBL	Phase 4 (approved)	ADRB1
PRACTOLOL	ChEMBL	Phase 4 (approved)	ADRB1
PRENYLAMINE	ChEMBL	Phase 4 (approved)	ADRB1
PRIMAQUINE	ChEMBL	Phase 4 (approved)	ADRB1
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	ADRB1
PROPAFENONE	ChEMBL	Phase 4 (approved)	ADRB1
PROPRANOLOL	ChEMBL	Phase 4 (approved)	ADRB1
PYRVINIUM	ChEMBL	Phase 4 (approved)	ADRB1
RANOLAZINE	ChEMBL	Phase 4 (approved)	ADRB1
RIFAMPIN	ChEMBL	Phase 4 (approved)	ADRB1
RIFAXIMIN	ChEMBL	Phase 4 (approved)	ADRB1
RITODRINE	ChEMBL	Phase 4 (approved)	ADRB1
RUCAPARIB	ChEMBL	Phase 4 (approved)	ADRB1
SALMETEROL	ChEMBL	Phase 4 (approved)	ADRB1
SERTINDOLE	ChEMBL	Phase 4 (approved)	ADRB1
SERTRALINE	ChEMBL	Phase 4 (approved)	ADRB1
SORAFENIB	ChEMBL	Phase 4 (approved)	ADRB1
SOTALOL	ChEMBL	Phase 4 (approved)	ADRB1
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRB1
TAMOXIFEN	ChEMBL	Phase 4 (approved)	ADRB1
TEGASEROD	ChEMBL	Phase 4 (approved)	ADRB1
THIORIDAZINE	ChEMBL	Phase 4 (approved)	ADRB1
TIMOLOL	ChEMBL	Phase 4 (approved)	ADRB1
TIOCONAZOLE	ChEMBL	Phase 4 (approved)	ADRB1
TROGLITAZONE	ChEMBL	Phase 4 (approved)	ADRB1
VALDECOXIB	ChEMBL	Phase 4 (approved)	ADRB1
VILANTEROL	ChEMBL	Phase 4 (approved)	ADRB1
AROTINOLOL	ChEMBL	Phase 3	ADRB1
AZELNIDIPINE	ChEMBL	Phase 3	ADRB1