Carvedilol

drug
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Also known as ArtistBM 14.190BM-14.190BM-14190C07AG02CoregCoronisDilatrendDimitoneDQ-2466EucardicEucardic 12.5Eucardic 25Eucardic 3.125Eucardic 6.25KorvasanKredexNSC-758694Querto

Summary

Carvedilol (CHEMBL723) is an approved small-molecule β-adrenergic antagonist (ATC C07AG02) targeting ADRA1A, ADRB1, and ADRB2; indicated across 37 conditions including heart failure and hypertensive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C07AG02
  • Targets: 5 (ADRA1A, ADRB1, ADRB2…)
  • Indications: 37 conditions
  • Clinical trials: 159
  • Chemistry: 406.5 Da · C24H26N2O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL723
NameCarvedilol
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID2585
ChEBICHEBI:3441
ATCC07AG02
Molecular formulaC24H26N2O4
Molecular weight406.5
InChIKeyOGHNVEJMJSYVRP-UHFFFAOYSA-N

SMILES: COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O

IUPAC name: 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol

ChEBI definition: A member of the class of carbazoles that is an adrenergic antagonist with non-selective β- and α-1 receptor blocking properties which helps in the management of congestive heart failure.

Pharmacological roles (ChEBI): β-adrenergic antagonist, antihypertensive agent, α-adrenergic antagonist, vasodilator agent, cardiovascular drug.

Also known as: Artist, BM 14.190, BM-14.190, BM-14190, C07AG02, Carvedilol, Coreg, Coronis, Dilatrend, Dimitone, DQ-2466, Eucardic

Parent form; salt/anhydrous children: CHEMBL1201167, CHEMBL1437006

Patent coverage: 7,715 distinct patent families (30,225 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 29,803 (99%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
ADRA1Aα1A-adrenoceptorAntagonist8.4P35348
ADRB1β1-adrenoceptorAntagonist9.80%P08588
ADRB2β2-adrenoceptorAntagonist10.60.4%P07550
ADRB3β3-adrenoceptorAntagonist8.30.1%P13945
RYR2RyR2Inhibition4.80.3%Q92736

Broader ChEMBL bioactivity targets: 67 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, UDP-glucuronosyltransferase 1A1, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, 4’-phosphopantetheinyl transferase ffp, Histone-lysine N-methyltransferase 2A, Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, 5-hydroxytryptamine receptor 2B.

Bioactivity

ChEMBL activities: 102 potent at pChembl ≥ 5 of 137 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ADRB19.99Ki0.1nMCHEMBL_ACT_7711855
ADRB29.78Ki0.17nMCHEMBL_ACT_7711857
ADRB19.75IC500.18nMCHEMBL_ACT_7711854
ADRB29.72Ki0.19nMCHEMBL_ACT_25553924
ADRB29.71Kd0.2nMCHEMBL_ACT_19132253
ADRB29.62IC500.24nMCHEMBL_ACT_7711856
P180909.09Ki0.81nMCHEMBL_ACT_2406517
ADRA1D9.05Ki0.88nMCHEMBL_ACT_7711847
ADRA1D8.75IC501.8nMCHEMBL_ACT_7711846
P158238.71Ki1.97nMCHEMBL_ACT_7711845
P158238.66Ki2.2nMCHEMBL_ACT_2406509
P158238.66Ki2.2nMCHEMBL_ACT_2930952
ADRB38.51Ki3.12nMCHEMBL_ACT_7711859
P431408.5Ki3.15nMCHEMBL_ACT_7711843
P193278.5Ki3.16nMCHEMBL_ACT_832803
P193278.48Ki3.34nMCHEMBL_ACT_7679594
P193288.47Ki3.4nMCHEMBL_ACT_2406513
ADRB18.47AC503.4nMCHEMBL_ACT_25121769
P193288.47Ki3.4nMCHEMBL_ACT_2930945
P158238.45IC503.55nMCHEMBL_ACT_7711844
ADRB28.41AC503.9nMCHEMBL_ACT_25122863
ADRB38.38IC504.16nMCHEMBL_ACT_7711858
P193278.23IC505.84nMCHEMBL_ACT_7679593
P431408.11IC507.79nMCHEMBL_ACT_7711842
ADRA1A8AC509.9nMCHEMBL_ACT_25138422
HTR2B8AC5010.1nMCHEMBL_ACT_25164110
ADRB37.92AC5012nMCHEMBL_ACT_25153302
ADRA2C7.89Ki13nMCHEMBL_ACT_7711853
HTR2B7.82Ki15nMCHEMBL_ACT_7679600
DRD47.76AC5017.2nMCHEMBL_ACT_25127378

Target pathways

Aggregated over 5 target gene(s): ADRA1A, ADRB1, ADRB2, ADRB3, RYR2.

Top Reactome pathways

24 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction4ADRA1A, ADRB1, ADRB2, ADRB3
Signaling by GPCR4ADRA1A, ADRB1, ADRB2, ADRB3
Class A/1 (Rhodopsin-like receptors)4ADRA1A, ADRB1, ADRB2, ADRB3
Amine ligand-binding receptors4ADRA1A, ADRB1, ADRB2, ADRB3
GPCR downstream signalling4ADRA1A, ADRB1, ADRB2, ADRB3
Adrenoceptors4ADRA1A, ADRB1, ADRB2, ADRB3
GPCR ligand binding4ADRA1A, ADRB1, ADRB2, ADRB3
G alpha (s) signalling events3ADRB1, ADRB2, ADRB3
Membrane Trafficking1ADRB2
Stimuli-sensing channels1RYR2
Transport of small molecules1RYR2
Metabolism of proteins1ADRB2
Muscle contraction1RYR2
G alpha (q) signalling events1ADRA1A
G alpha (12/13) signalling events1ADRA1A
Cardiac conduction1RYR2
Ion homeostasis1RYR2
Vesicle-mediated transport1ADRB2
Deubiquitination1ADRB2
Ub-specific processing proteases1ADRB2
Post-translational protein modification1ADRB2
Cargo recognition for clathrin-mediated endocytosis1ADRB2
Clathrin-mediated endocytosis1ADRB2
Ion channel transport1RYR2

Dominant GO biological processes

GO termTargets
signal transduction4
G protein-coupled receptor signaling pathway4
positive regulation of MAPK cascade4
adenylate cyclase-activating adrenergic receptor signaling pathway4
adrenergic receptor signaling pathway3
diet induced thermogenesis3
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure3
adenylate cyclase-activating G protein-coupled receptor signaling pathway3
response to cold3
heat generation3
negative regulation of multicellular organism growth3
brown fat cell differentiation3
positive regulation of cold-induced thermogenesis3
positive regulation of heart rate by epinephrine-norepinephrine2
positive regulation of the force of heart contraction by epinephrine-norepinephrine2

Indications & clinical

Indications

37 indications (6 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).

IndicationTrial phaseMONDOEFO
heart failure4MONDO:0005252EFO:0003144
hypertensive disorder4MONDO:0005044EFO:0000537
congestive heart failure4MONDO:0005009EFO:0000373
cardiovascular disorder4MONDO:0004995EFO:0000319
myocardial infarction4MONDO:0005068EFO:0000612
atrial fibrillation3MONDO:0004981EFO:0000275
portal hypertension3MONDO:0005080EFO:0000666
acute myeloid leukemia3MONDO:0018874EFO:0000222
plasma cell myeloma3MONDO:0009693EFO:0001378
lymphoid leukemia3MONDO:0005402EFO:0004289
atherosclerosis3MONDO:0005311EFO:0003914
coronary artery disorder3MONDO:0005010EFO:0001645
essential hypertension3MONDO:0001134MONDO:0001134
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
lymphoma3MONDO:0005062EFO:0000574
lymphoid neoplasm3MONDO:0005157EFO:0001642
chronic kidney disease3MONDO:0005300EFO:0003884
pulmonary arterial hypertension2MONDO:0015924EFO:0001361
epilepsy2MONDO:0005027EFO:0000474
post-traumatic stress disorder2MONDO:0005146EFO:0001358
cocaine dependence2MONDO:0005186EFO:0002610
kidney disorder2MONDO:0005240EFO:0003086
hypoglycemia2MONDO:0004946HP:0001943
pulmonary hypertension2MONDO:0005149MONDO:0005149
breast neoplasm2MONDO:0021100MONDO:0007254
esophageal varices2MONDO:0001221EFO:0009545
cardiomyopathy2MONDO:0004994EFO:0000318
neoplasm2MONDO:0005070MONDO:0004992
vascular disorder1MONDO:0005385EFO:0004264
glioblastoma0MONDO:0018177EFO:0000519
rheumatoid arthritis0MONDO:0008383EFO:0000685

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

Clinical trials

Total trials: 159.

Phase distribution

PhaseTrials
PHASE458
Not specified39
PHASE319
PHASE219
PHASE111
EARLY_PHASE15
PHASE2/PHASE34
PHASE1/PHASE24

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03778554PHASE4ACTIVE_NOT_RECRUITINGDanish Trial of Beta Blocker Treatment After Myocardial Infarction Without Reduced Ejection Fraction
NCT05872698PHASE4ACTIVE_NOT_RECRUITINGBeta-blockers or Placebo for Primary Prophylaxis (BOPPP) of Oesophageal Varices Trial.
NCT06449339PHASE4RECRUITINGNon-selective Beta-blocker in Compensated Advanced Chronic Liver Disease
NCT06594744PHASE4RECRUITINGEndoscopic Variceal Ligation vs Carvedilol for the Prevention of First Esophageal Variceal Bleeding in Patients With HCC
NCT06594783PHASE4RECRUITINGCarvedilol Plus EVL or Not for the Primary Prevention of Esophageal Variceal Bleeding in Carvedilol Non-responders
NCT06964464PHASE4RECRUITINGComparative Effectiveness of Carvedilol Versus Metoprolol Succinate in Heart Failure Patients With an Implantable Cardioverter Defibrillator
NCT07103655PHASE4NOT_YET_RECRUITINGThe Therapeutic Value of Mavacamten in Hypertrophic Cardiomyopathy With Mid-to-Apical Left Ventricular Obstruction
NCT07322237PHASE4RECRUITINGDICE Study- Diastolic Improvement With Carvedilol & Empagliflozin in Patients With Cirrhosis
NCT07352228PHASE4ENROLLING_BY_INVITATIONCarvedilol vs. Propranolol for Preventing Rebleeding After Endoscopic Treatment of Cirrhotic Varices
NCT07521332PHASE4RECRUITINGApixaban-PK Trial: Preventing Portal Hypertension Complications in Cirrhosis
NCT00060918PHASE4COMPLETEDGlycemic Control Of Carvedilol Versus Metoprolol In Patients With Type II Diabetes Mellitus And Hypertension
NCT00060931PHASE4COMPLETEDEffect Of Carvedilol Versus Metoprolol On Glycemic Control In Patients With Type II Diabetes And Hypertension
NCT00123604PHASE4COMPLETEDVascular Effects of Carvedilol Versus Metoprolol in Hypertensive Patients With Type 2 Diabetes
NCT00374465PHASE4UNKNOWNTherapy With Verapamil or Carvedilol in Chronic Heart Failure
NCT00384566PHASE4WITHDRAWNA Comparison of the Effect of Carvedilol and Metoprolol on Airways Tone in Patients With Heart Failure
NCT00391846PHASE4COMPLETEDEvaluation of Heart Failure Treatment Guided by N-terminal Pro B-type Natriuretic Peptide (NTproBNP) vs Clinical Symptoms and Signs Alone
NCT00402376PHASE4TERMINATEDEvaluation of Myocardial Improvement in Patients Supported by Ventricular Assist Device Under Optimal Pharmacological Therapy
NCT00496834PHASE4COMPLETEDLAAS (Losartan Anti-Atherosclerosis Study)(0954-330)(COMPLETED)
NCT00517725PHASE4COMPLETEDNebivolol Versus Bisoprolol Versus Carvedilol in Heart Failure
NCT00606775PHASE4UNKNOWNThe Preventive Efficacy of Carvedilol on Cardiac Dysfunction in Duchenne Muscular Dystrophy
NCT00642434PHASE4COMPLETEDComparison of Blood Pressure Medications on Metabolism
NCT00673075PHASE4COMPLETEDThe Effect of Nebivolol in Hypertensive Patients With Coronary Artery Disease
NCT00732511PHASE4UNKNOWNCoreg CR, Blood Vessel Stiffness and Blood Vessel Function
NCT00819845PHASE4UNKNOWNRamipril Versus Carvedilol in Duchenne and Becker Patients
NCT00827775PHASE4COMPLETEDMechanisms and Treatment of Intradialytic Hypertension
NCT00924833PHASE4COMPLETEDEffects of Nebivolol Versus Carvedilol on Cardiopulmonary Function at High Altitude in Healthy Subjects.
NCT01059396PHASE4COMPLETEDStudy on B-blockers to Prevent Decompensation of Cirrhosis With HTPortal
NCT01070641PHASE4UNKNOWNRCT of Carvedilol Versus Variceal Band Ligation in the Primary Prophylaxis of Oesophageal Variceal Haemorrhage
NCT01103154PHASE4COMPLETEDA Trial of Nadolol Plus Isosorbide Mononitrate Versus Carvedilol for the Prevention of Variceal Rebleeding
NCT01155635PHASE4COMPLETEDCarvedilol Post-intervention Long-term Administration in Large-scale Trial
NCT01243827PHASE4UNKNOWNComparison of Effect of cARvedilol Compared To bISoprolol on cenTral Pulse Pressure in Hypertension (ARTIST) Study
NCT01261065PHASE4COMPLETEDMechanisms of Improvement With Beta-Blocker Treatment in Heart Failure
NCT01354444PHASE4COMPLETEDTrial of Carvedilol in Alzheimer’s Disease
NCT01383044PHASE4TERMINATEDBanding Ligation With Carvedilol Versus Carvedilol for the Prevention of First Bleeding
NCT01425164PHASE4UNKNOWNIschemia In Hemodialysed Patients: Ivabradine Versus Carvedilol
NCT01656005PHASE4COMPLETEDBeta Blocker Therapy in Moderate to Severe COPD
NCT01798992PHASE4COMPLETEDEffect of Beta-blockers on Structural Remodeling and Gene Expression in the Failing Human Heart
NCT02056626PHASE4COMPLETEDConditioned Pharmacotherapeutic Effects in Hypertension
NCT02251509PHASE4UNKNOWNRate Control in Atrial Fibrillation
NCT02385422PHASE4UNKNOWNThe Effect of Carvedilol Vs Propranolol in Cirrhotic Patients With Variceal Bleeding

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (4) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

GuidelineSourceGene(s)DosingRecommendation
Annotation of DPWG Guideline for carvedilol and CYP2D6DPWGCYP2D6
Annotation of CPIC Guideline for acebutolol, betaxolol, bisoprolol, caCPICCYP2D6
Annotation of CPIC Guideline for acebutolol, atenolol, betaxolol, bisoCPICADRA2C;ADRB1;GRK4;GRK5
Annotation of CPIC Guideline for carvedilol, labetalol, nadolol, pindoCPICADRB2

PharmGKB also curates 8 clinical and 56 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

684 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
DESLORATADINEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
PRAMIPEXOLEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
PROPOXYPHENEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
PYRAZINAMIDEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
RIFAMPINChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
TEGASERODChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
ARIPIPRAZOLEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
BROMOCRIPTINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
EPINEPHRINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
FENOTEROLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
ISOPROTERENOLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
LABETALOLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
NOREPINEPHRINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
PHENYLEPHRINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
PIMOZIDEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
PINDOLOLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
PROPAFENONEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
PROPRANOLOLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
SALMETEROLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
THIORIDAZINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2, ADRB3
ALPRENOLOLChEMBLPhase 2ADRA1A, ADRB1, ADRB2, ADRB3
AlogliptinPubChemApprovedADRA1A, ADRB1, ADRB2, ADRB3
BosentanPubChemApprovedADRA1A, ADRB1, ADRB2, ADRB3
FidaxomicinPubChemApprovedADRA1A, ADRB1, ADRB2, ADRB3
Tiotropium Bromide MonohydratePubChemApprovedADRA1A, ADRB1, ADRB2, ADRB3
ACLIDINIUM BROMIDEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2
CHENODIOLChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2
CLOFARABINEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2
CLOZAPINEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB2, ADRB3
OLANZAPINEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB2, ADRB3
OLODATEROLChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2
TAMSULOSINChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRB1, ADRB2
AMIODARONEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB3
AMITRIPTYLINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
AMLODIPINEChEMBLPhase 4 (approved)ADRA1A, ADRB2, ADRB3
ARFORMOTEROLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
ASTEMIZOLEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB3
ATENOLOLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
BENPERIDOLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
BEPRIDILChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB3
BISOPROLOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
BREXPIPRAZOLEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
CHLORHEXIDINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
CLEMASTINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
CLOMIPRAMINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
CLOTRIMAZOLEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
DARIFENACINChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB3
DOBUTAMINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
DOMPERIDONEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
DOXAZOSINChEMBLPhase 4 (approved)ADRA1A, ADRB2, ADRB3
EBASTINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB3
ERGOTAMINEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
FLUSPIRILENEChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2
FORMOTEROLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
HALOPERIDOLChEMBLPhase 4 (approved)ADRA1A, ADRB2, ADRB3
INDACATEROLChEMBLPhase 4 (approved)ADRA1A, ADRB1, ADRB2