DGIdb - CARVEDILOL Drug Record

CARVEDILOL chembl:CHEMBL723 Approved

Alternate Names:

COREG
EUCARDIC 3.125
SKF-105517
BM-14-190
C07AG02
DQ-2466
EUCARDIC 12.5
CARVEDILOL
COREG CR
BM-14.190
BM-14190
BM 14.190
EUCARDIC 25
EUCARDIC 6.25
DQ 2466
SKF 105517
(+-)-1-(CARBAZOL-4-YLOXY)-3-((2-(O-METHOXYPHENOXY)ETHYL)AMINO)-2-PROPANOL
CARVEDILOLUM
drugbank:01136
rxcui:20352
chemidplus:72956-09-3
chembl:CHEMBL723
pubchem.compound:2585

Drug Info:

Drug Indications	cardiovascular agent
FDA Approval	not approved
Drug Class	Small Molecule
Drug Indications	for treatment of congestive heart failure
Year of Approval	1995
Drug Class	antihypertensive agents

(5 More Sources)

Publications:

McCrink KA et al., 2016, β<sub>1</sub>-adrenoceptor Arg389Gly polymorphism confers differential β-arrestin-binding tropism in cardiac myocytes., Pharmacogenomics
Rau T et al., 2012, Impact of the β1-adrenoceptor Arg389Gly polymorphism on heart-rate responses to bisoprolol and carvedilol in heart-failure patients., Clin Pharmacol Ther
Huntgeburth M et al., 2011, The Arg389Gly β1-adrenoceptor gene polymorphism influences the acute effects of β-adrenoceptor blockade on contractility in the human heart., Clin Res Cardiol
Baudhuin LM et al., 2010, Relation of ADRB1, CYP2D6, and UGT1A1 polymorphisms with dose of, and response to, carvedilol or metoprolol therapy in patients with chronic heart failure., Am J Cardiol
Metra M et al., 2010, Role of beta-adrenergic receptor gene polymorphisms in the long-term effects of beta-blockade with carvedilol in patients with chronic heart failure., Cardiovasc Drugs Ther
Filigheddu F et al., 2010, Haplotypes of the adrenergic system predict the blood pressure response to beta-blockers in women with essential hypertension., Pharmacogenomics
Chen L et al., 2007, Arg389Gly-beta1-adrenergic receptors determine improvement in left ventricular systolic function in nonischemic cardiomyopathy patients with heart failure after chronic treatment with carvedilol., Pharmacogenet Genomics
Lobmeyer MT et al., 2007, Synergistic polymorphisms of beta1 and alpha2C-adrenergic receptors and the influence on left ventricular ejection fraction response to beta-blocker therapy in heart failure., Pharmacogenet Genomics
Liu J et al., 2006, beta1-Adrenergic receptor polymorphisms influence the response to metoprolol monotherapy in patients with essential hypertension., Clin Pharmacol Ther
Terra SG et al., 2005, Beta1-adrenergic receptor polymorphisms and left ventricular remodeling changes in response to beta-blocker therapy., Pharmacogenet Genomics
de Groote P et al., 2005, Association between beta-1 and beta-2 adrenergic receptor gene polymorphisms and the response to beta-blockade in patients with stable congestive heart failure., Pharmacogenet Genomics
Terra SG et al., 2005, beta-Adrenergic receptor polymorphisms and responses during titration of metoprolol controlled release/extended release in heart failure., Clin Pharmacol Ther
Liu et al., 2003, Gly389Arg polymorphism of beta1-adrenergic receptor is associated with the cardiovascular response to metoprolol., Clin. Pharmacol. Ther.
Mialet Perez J et al., 2003, Beta 1-adrenergic receptor polymorphisms confer differential function and predisposition to heart failure., Nat Med
White HL et al., 2003, An evaluation of the beta-1 adrenergic receptor Arg389Gly polymorphism in individuals with heart failure: a MERIT-HF sub-study., Eur J Heart Fail
Johnson et al., 2003, Beta 1-adrenergic receptor polymorphisms and antihypertensive response to metoprolol., Clin. Pharmacol. Ther.
Sofowora GG et al., 2003, A common beta1-adrenergic receptor polymorphism (Arg389Gly) affects blood pressure response to beta-blockade., Clin Pharmacol Ther
Nichols et al., 1989, The interaction of the enantiomers of carvedilol with alpha 1- and beta 1-adrenoceptors., Chirality
Nichols et al., 1989, In vitro pharmacologic profile of the novel beta-adrenoceptor antagonist and vasodilator, carvedilol., Pharmacology
de Mey et al., 1994, Dose-effect and pharmacokinetic-pharmacodynamic relationships of the beta 1-adrenergic receptor blocking properties of various doses of carvedilol in healthy humans., Clin. Pharmacol. Ther.
Nichols et al., 1991, Studies on the mechanism of arterial vasodilation produced by the novel antihypertensive agent, carvedilol., Fundam Clin Pharmacol
Yeh et al., 2006, Reduced expression of endothelial connexins 43 and 37 in hypertensive rats is rectified after 7-day carvedilol treatment., Am. J. Hypertens.
Fan et al., 2005, [Effects and the mechanism of carvedilol on gap junctional intercellular communication in rat myocardium]., Zhonghua Xin Xue Guan Bing Za Zhi
Koshimizu et al., 2004, Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors., Cardiovasc. Res.
Sehrt D et al., 2011, Carvedilol pharmacokinetics and pharmacodynamics in relation to CYP2D6 and ADRB pharmacogenetics., Pharmacogenomics
Kaye et al., 2003, Beta-adrenoceptor genotype influences the response to carvedilol in patients with congestive heart failure., Pharmacogenetics
Maebara et al., 2002, Nightmares and panic disorder associated with carvedilol overdose., Ann Pharmacother
Irodova et al., 2002, [Carvedilol in treating primary pulmonary hypertension patients: effect on severity of cardiac failure, degree of pulmonary hypertension, concentration of catecholamines in blood plasma and dependence of cyclic AMP synthesis in lymphocytes on beta-adrenergic receptors]., Ter. Arkh.
Okajima et al., 2004, Activation of capsaicin-sensitive sensory neurons by carvedilol, a nonselective beta-blocker, in spontaneous hypertensive rats., J. Pharmacol. Exp. Ther.
Yang et al., 2006, [Beneficial effects of carvedilol on cardiomyocyte apoptosis and bcl-2/bax expression after acute myocardial infarction an experiment with rats]., Zhonghua Yi Xue Za Zhi
Zeng et al., 2003, Effects of carvedilol on cardiomyocyte apoptosis and gene expression in vivo after ischemia-reperfusion in rats., J. Huazhong Univ. Sci. Technol. Med. Sci.
Oliveira et al., 2005, Are the antioxidant properties of carvedilol important for the protection of cardiac mitochondria?, Curr Vasc Pharmacol
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
O'Connell TD et al., 2013, Cardiac alpha1-adrenergic receptors: novel aspects of expression, signaling mechanisms, physiologic function, and clinical importance., Pharmacol Rev
Jensen BC et al., 2009, {alpha}1-Adrenergic receptor subtypes in nonfailing and failing human myocardium., Circ Heart Fail
Hryniewicz et al., 2003, Partial reversal of cachexia by beta-adrenergic receptor blocker therapy in patients with chronic heart failure., J. Card. Fail.
Afonso et al., 2006, Carvedilol action is dependent on endogenous production of nitric oxide., Am. J. Hypertens.
Oldham et al., 1997, In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)- and S(-)-carvedilol., Drug Metab. Dispos.
Bajcetic et al., 2008, Effects of carvedilol on left ventricular function and oxidative stress in infants and children with idiopathic dilated cardiomyopathy: a 12-month, two-center, open-label study., Clin Ther
Takekuma Y et al., 2006, Contribution of polymorphisms in UDP-glucuronosyltransferase and CYP2D6 to the individual variation in disposition of carvedilol., J Pharm Pharm Sci

CARVEDILOL GJA1

Interaction Score: 1.72

Interaction Types & Directionality:

other/unknown

Interaction Info:

PMIDs:
16448880 16563290

Sources:
NCI
CARVEDILOL ADRB1

Interaction Score: 1.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name carvedilol,Coreg

Novel drug target Established target

Mechanism of Interaction Adrenergic receptor beta antagonist

PMIDs:
27643874 22617224 21311897 20643254 20352314 20235788 18075464 17496726 16815314 15864115 15861037 15735607 14534524 14502278 12921807 12844134 12709726 2577144 2575762 7908256 1712335

Sources:
TdgClinicalTrial ChemblInteractions TEND PharmGKB
CARVEDILOL GSR

Interaction Score: 0.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18498919

Sources:
NCI
CARVEDILOL LEP

Interaction Score: 0.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14966787

Sources:
NCI
CARVEDILOL ADRB2

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name carvedilol,Coreg

Novel drug target Established target

Direct Interaction yes

PMIDs:
21599570 20352314 15861037 12835612 12398570 12360591 14764656 1712335

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND PharmGKB
CARVEDILOL XDH

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15853634

Sources:
NCI
CARVEDILOL UGT1A1

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20643254 16849011

Sources:
PharmGKB
CARVEDILOL ADRA1A

Interaction Score: 0.28

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

potentiator

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

Trial Name carvedilol, Coreg

PMIDs:
17016423 17139284 24368739 19919991

Sources:
TdgClinicalTrial ChemblInteractions TEND
CARVEDILOL BAX

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16759520 12973927

Sources:
NCI
CARVEDILOL NOS1

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16580580

Sources:
NCI
CARVEDILOL ADRB3

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor beta antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CARVEDILOL ADRA1B

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

PMIDs:
15306222

Sources:
ChemblInteractions
CARVEDILOL DRD1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CARVEDILOL ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
CARVEDILOL CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9280405

Sources:
NCI
CARVEDILOL KDM4E

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CARVEDILOL BAZ2B

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CARVEDILOL CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA

TEND: CARVEDILOL
- Version: 01-August-2011
Alternate Names:

CARVEDILOL Primary Drug Name

Drug Info:

Drug Class antihypertensive agents

Year of Approval 1995

Publications:
TdgClinicalTrial: CARVEDILOL
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications for treatment of congestive heart failure

Drug Class Small Molecule

FDA Approval not approved

Publications:

NCI: CARVEDILOL

Version: 14-September-2017

Alternate Names:

C28906 NCI drug code

Drug Info:

Publications:

Afonso et al., 2006, Carvedilol action is dependent on endogenous production of nitric oxide., Am. J. Hypertens.

Bajcetic et al., 2008, Effects of carvedilol on left ventricular function and oxidative stress in infants and children with idiopathic dilated cardiomyopathy: a 12-month, two-center, open-label study., Clin Ther

Kaye et al., 2003, Beta-adrenoceptor genotype influences the response to carvedilol in patients with congestive heart failure., Pharmacogenetics

PharmGKB: carvedilol

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Baudhuin LM et al., 2010, Relation of ADRB1, CYP2D6, and UGT1A1 polymorphisms with dose of, and response to, carvedilol or metoprolol therapy in patients with chronic heart failure., Am J Cardiol

Takekuma Y et al., 2006, Contribution of polymorphisms in UDP-glucuronosyltransferase and CYP2D6 to the individual variation in disposition of carvedilol., J Pharm Pharm Sci

Terra SG et al., 2005, Beta1-adrenergic receptor polymorphisms and left ventricular remodeling changes in response to beta-blocker therapy., Pharmacogenet Genomics

TTD: Carvedilol
- Version: 2020.06.01
Alternate Names:

D0W9LX TTD Drug ID

Drug Info:

Publications:
DTC: CARVEDILOL
- Version: 02-September-2020
Alternate Names:

CHEMBL723 ChEMBL Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL723
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL723
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
FDA: Carvedilol
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Trial Name	carvedilol,Coreg
Novel drug target	Established target
Mechanism of Interaction	Adrenergic receptor beta antagonist

Mechanism of Interaction	Adrenergic receptor alpha-1 antagonist
Direct Interaction	yes
Trial Name	carvedilol, Coreg

antagonist (inhibitory)
inhibitor (inhibitory)
potentiator

CARVEDILOL Drug Record

CARVEDILOL chembl:CHEMBL723 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: other/unknown

Interaction Info:

PMIDs: 16448880 16563290

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name carvedilol,Coreg Novel drug target Established target Mechanism of Interaction Adrenergic receptor beta antagonist

PMIDs: 27643874 22617224 21311897 20643254 20352314 20235788 18075464 17496726 16815314 15864115 15861037 15735607 14534524 14502278 12921807 12844134 12709726 2577144 2575762 7908256 1712335

Sources: TdgClinicalTrial ChemblInteractions TEND PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18498919

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14966787

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name carvedilol,Coreg Novel drug target Established target Direct Interaction yes

PMIDs: 21599570 20352314 15861037 12835612 12398570 12360591 14764656 1712335

Sources: TdgClinicalTrial ChemblInteractions NCI TEND PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15853634

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20643254 16849011

Sources: PharmGKB

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory) potentiator

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-1 antagonist Direct Interaction yes Trial Name carvedilol, Coreg

PMIDs: 17016423 17139284 24368739 19919991

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16759520 12973927

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16580580

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Adrenergic receptor beta antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-1 antagonist Direct Interaction yes

PMIDs: 15306222

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9280405

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA

TEND: CARVEDILOL

Alternate Names: CARVEDILOL Primary Drug Name

Drug Info: Drug Class antihypertensive agents Year of Approval 1995

Interaction Types & Directionality:

other/unknown

PMIDs:
16448880 16563290

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name carvedilol,Coreg

Novel drug target Established target

Mechanism of Interaction Adrenergic receptor beta antagonist

PMIDs:
27643874 22617224 21311897 20643254 20352314 20235788 18075464 17496726 16815314 15864115 15861037 15735607 14534524 14502278 12921807 12844134 12709726 2577144 2575762 7908256 1712335

Sources:
TdgClinicalTrial ChemblInteractions TEND PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18498919

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
14966787

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name carvedilol,Coreg

Novel drug target Established target

Direct Interaction yes

PMIDs:
21599570 20352314 15861037 12835612 12398570 12360591 14764656 1712335

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15853634

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
20643254 16849011

Sources:
PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

potentiator

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

Trial Name carvedilol, Coreg

PMIDs:
17016423 17139284 24368739 19919991

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

n/a

PMIDs:
16759520 12973927

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16580580

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor beta antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

PMIDs:
15306222

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9280405

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA

Alternate Names:

CARVEDILOL Primary Drug Name

Drug Info:

Drug Class antihypertensive agents

Year of Approval 1995

Drug Info:

Drug Indications for treatment of congestive heart failure

Drug Class Small Molecule

FDA Approval not approved

Alternate Names:

C28906 NCI drug code

Alternate Names:

D0W9LX TTD Drug ID

Alternate Names:

CHEMBL723 ChEMBL Drug ID