DGIdb - BUPROPION Drug Record

BUPROPION chembl:CHEMBL894 Approved

Alternate Names:

BUPROPION
AMFEBUTAMONE
ZYBAN®
BW-323
WELLBUTRIN®
chembl:CHEMBL894
rxcui:42347
drugbank:01156
chemidplus:34911-55-2
pubchem.compound:444

Drug Info:

Drug Class	antidepressive agents
Year of Approval	1985
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antidepressant,appetite suppressant,smoking-cessation agent

(2 More Sources)

Publications:

Tiwari AK et al., 2013, Analysis of 34 candidate genes in bupropion and placebo remission., Int J Neuropsychopharmacol
Stahl et al., 2004, A Review of the Neuropharmacology of Bupropion, a Dual Norepinephrine and Dopamine Reuptake Inhibitor., Prim Care Companion J Clin Psychiatry
Bondarev et al., 2003, Behavioral and biochemical investigations of bupropion metabolites., Eur. J. Pharmacol.
Mitchell et al., 2006, The effects of norepinephrine transporter inactivation on locomotor activity in mice., Biol. Psychiatry
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Shalabi AR et al., 2017, Deconstructed Analogues of Bupropion Reveal Structural Requirements for Transporter Inhibition versus Substrate-Induced Neurotransmitter Release., ACS Chem Neurosci
Mortensen OV et al., 2006, Gain of function mutants reveal sites important for the interaction of the atypical inhibitors benztropine and bupropion with monoamine transporters., J Neurochem
de Greef et al., 1987, Control of prolactin release induced by suckling., Endocrinology
Miller et al., 2002, Bupropion inhibits nicotine-evoked [(3)H]overflow from rat striatal slices preloaded with [(3)H]dopamine and from rat hippocampal slices preloaded with [(3)H]norepinephrine., J. Pharmacol. Exp. Ther.
Kugaya et al., 2003, Changes in human in vivo serotonin and dopamine transporter availabilities during chronic antidepressant administration., Neuropsychopharmacology
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Szabó et al., 2004, [Change of dopamine transporter activity (DAT) during the action of bupropion (in depression)]., Neuropsychopharmacol Hung
Meyer et al., 2002, Bupropion occupancy of the dopamine transporter is low during clinical treatment., Psychopharmacology (Berl.)
Learned-Coughlin et al., 2003, In vivo activity of bupropion at the human dopamine transporter as measured by positron emission tomography., Biol. Psychiatry
Simonsen U et al., 2016, Modulation of Dopaminergic Pathways to Treat Erectile Dysfunction., Basic Clin Pharmacol Toxicol
Bergen AW et al., 2015, Drug Metabolizing Enzyme and Transporter Gene Variation, Nicotine Metabolism, Prospective Abstinence, and Cigarette Consumption., PLoS One
Tomaz PR et al., 2015, CYP2B6 rs2279343 polymorphism is associated with smoking cessation success in bupropion therapy., Eur J Clin Pharmacol
Choi HD et al., 2015, Lack of association between DRD2 Taq1A gene polymorphism and smoking cessation therapy: a meta-analysis., Int J Clin Pharmacol Ther
David SP et al., 2007, Bupropion efficacy for smoking cessation is influenced by the DRD2 Taq1A polymorphism: analysis of pooled data from two clinical trials., Nicotine Tob Res
David SP et al., 2007, Pharmacogenetic clinical trial of sustained-release bupropion for smoking cessation., Nicotine Tob Res
Swan GE et al., 2005, Dopamine receptor DRD2 genotype and smoking cessation outcome following treatment with bupropion SR., Pharmacogenomics J
Lerman C et al., 2003, Effects of dopamine transporter and receptor polymorphisms on smoking cessation in a bupropion clinical trial., Health Psychol
Quaak M et al., 2012, Genetic variants in the serotonin transporter influence the efficacy of bupropion and nortriptyline in smoking cessation., Addiction
Lerman C et al., 2006, Role of functional genetic variation in the dopamine D2 receptor (DRD2) in response to bupropion and nicotine replacement therapy for tobacco dependence: results of two randomized clinical trials., Neuropsychopharmacology
Jönsson EG et al., 1999, Polymorphisms in the dopamine D2 receptor gene and their relationships to striatal dopamine receptor density of healthy volunteers., Mol Psychiatry
Pohjalainen T et al., 1998, The A1 allele of the human D2 dopamine receptor gene predicts low D2 receptor availability in healthy volunteers., Mol Psychiatry
Monteleone P et al., 2009, Management of schizophrenia with obesity, metabolic, and endocrinological disorders., Psychiatr Clin North Am
Hoenicka J et al., 2010, The ANKK1 gene associated with addictions is expressed in astroglial cells and upregulated by apomorphine., Biol Psychiatry
Blum K et al., 1990, Allelic association of human dopamine D2 receptor gene in alcoholism., JAMA
Kraschewski A et al., 2009, Association of the dopamine D2 receptor gene with alcohol dependence: haplotypes and subgroups of alcoholics as key factors for understanding receptor function., Pharmacogenet Genomics
Liu YZ et al., 2009, Association of the DRD2 and DRD3 polymorphisms with response to pramipexole in Parkinson's disease patients., Eur J Clin Pharmacol
Doehring A et al., 2009, Genetic variants altering dopamine D2 receptor expression or function modulate the risk of opiate addiction and the dosage requirements of methadone substitution., Pharmacogenet Genomics
Munafò MR et al., 2009, Lack of association of DRD2 rs1800497 (Taq1A) polymorphism with smoking cessation in a nicotine replacement therapy randomized trial., Nicotine Tob Res
Le Foll B et al., 2009, Genetics of dopamine receptors and drug addiction: a comprehensive review., Behav Pharmacol
Shen YC et al., 2009, Effects of DRD2/ANKK1 gene variations and clinical factors on aripiprazole efficacy in schizophrenic patients., J Psychiatr Res
Ikeda M et al., 2008, Variants of dopamine and serotonin candidate genes as predictors of response to risperidone treatment in first-episode schizophrenia., Pharmacogenomics
David SP et al., 2008, Genetic variation in the dopamine pathway and smoking cessation., Pharmacogenomics
Thelma B et al., 2008, Genetic underpinnings of tardive dyskinesia: passing the baton to pharmacogenetics., Pharmacogenomics
Blum K et al., 1991, Association of the A1 allele of the D2 dopamine receptor gene with severe alcoholism., Alcohol
Huang W et al., 2009, Significant association of ANKK1 and detection of a functional polymorphism with nicotine dependence in an African-American sample., Neuropsychopharmacology
Bakker PR et al., 2008, Antipsychotic-induced tardive dyskinesia and polymorphic variations in COMT, DRD2, CYP1A2 and MnSOD genes: a meta-analysis of pharmacogenetic interactions., Mol Psychiatry
Alenius M et al., 2008, Gene polymorphism influencing treatment response in psychotic patients in a naturalistic setting., J Psychiatr Res
Smith L et al., 2008, Meta-analysis of the association of the Taq1A polymorphism with the risk of alcohol dependency: a HuGE gene-disease association review., Am J Epidemiol
Zai CC et al., 2007, Meta-analysis of two dopamine D2 receptor gene polymorphisms with tardive dyskinesia in schizophrenia patients., Mol Psychiatry
Hwang R et al., 2005, Association study of 12 polymorphisms spanning the dopamine D(2) receptor gene and clozapine treatment response in two treatment refractory/intolerant populations., Psychopharmacology (Berl)
Young et al., 2004, Prolactin levels in antipsychotic treatment of patients with schizophrenia carrying the DRD2*A1 allele., Br J Psychiatry
Xu K et al., 2004, Association of specific haplotypes of D2 dopamine receptor gene with vulnerability to heroin dependence in 2 distinct populations., Arch Gen Psychiatry
Neville MJ et al., 2004, Identification and characterization of ANKK1: a novel kinase gene closely linked to DRD2 on chromosome band 11q23.1., Hum Mutat
Johnstone EC et al., 2004, Genetic variation in dopaminergic pathways and short-term effectiveness of the nicotine patch., Pharmacogenetics
Ritchie T et al., 2003, Association of seven polymorphisms of the D2 dopamine receptor gene with brain receptor-binding characteristics., Neurochem Res
Schäfer M et al., 2001, Association of short-term response to haloperidol treatment with a polymorphism in the dopamine D(2) receptor gene., Am J Psychiatry
Suzuki A et al., 2000, The relationship between dopamine D2 receptor polymorphism at the Taq1 A locus and therapeutic response to nemonapride, a selective dopamine antagonist, in schizophrenic patients., Pharmacogenetics
Mihara K et al., 2000, Prolactin response to nemonapride, a selective antagonist for D2 like dopamine receptors, in schizophrenic patients in relation to Taq1A polymorphism of DRD2 gene., Psychopharmacology (Berl)
Berrettini WH et al., 2007, Catechol-O-methyltransferase (COMT) gene variants predict response to bupropion therapy for tobacco dependence., Biol Psychiatry
Clark SL et al., 2012, Pharmacogenomic study of side-effects for antidepressant treatment options in STAR*D., Psychol Med

BUPROPION SACM1L

Interaction Score: 7.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22041458

Sources:
PharmGKB
BUPROPION ANKK1

Interaction Score: 2.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26153084 25881752 18058343 17654295 15492764 14570538

Sources:
PharmGKB
BUPROPION EPB41

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
BUPROPION GALR1

Interaction Score: 1.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
BUPROPION DBH

Interaction Score: 1.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22947179

Sources:
PharmGKB
BUPROPION SLC6A3

Interaction Score: 0.93

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BVF-033,Aplenzin

Novel drug target Established target

Trial Name Contrave

PMIDs:
12183670 12589396 9537821 15787205 12185406 14550679 11752352 15361919 28220701 16923164 27541930

Sources:
TdgClinicalTrial TEND
BUPROPION SLC6A2

Interaction Score: 0.75

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BVF-033,Aplenzin

Novel drug target Established target

Trial Name Contrave

PMIDs:
15361919 12909199 16893531 11752352 28220701 16923164

Sources:
TdgClinicalTrial TEND
BUPROPION DRD2

Interaction Score: 0.71

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16123753 10395223 9672901 19944883 19853839 1969501 19603545 19396436 19373123 19273465 19179847 18926547 18855532 18781857 18781856 1839129 18354387 18180754 18086475 17989061 17767146 15830237 15492764 15286066 15184239 15146457 15077009 12587665 11329406 10862524 10823405

Sources:
PharmGKB
BUPROPION FKBP5

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22947179

Sources:
PharmGKB
BUPROPION SLC18A2

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22947179

Sources:
PharmGKB
BUPROPION CYP2A6

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26132489

Sources:
PharmGKB
BUPROPION COMT

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16876132

Sources:
PharmGKB
BUPROPION PRL

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
3109881

Sources:
NCI
BUPROPION SLC6A4

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21658141

Sources:
PharmGKB
BUPROPION ACE

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22947179

Sources:
PharmGKB
BUPROPION HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22947179

Sources:
PharmGKB
BUPROPION DRD1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

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

BUPROPION Primary Drug Name

Drug Info:

Year of Approval 1985

Drug Class antidepressive agents

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

Drug Info:

Drug Indications antidepressant,appetite suppressant,smoking-cessation agent

Drug Class Small Molecule

FDA Approval approved

Publications:
NCI: BUPROPION
- Version: 14-September-2017
Alternate Names:

C1317 NCI drug code

Drug Info:

Publications:

de Greef et al., 1987, Control of prolactin release induced by suckling., Endocrinology

PharmGKB: bupropion

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Tiwari AK et al., 2013, Analysis of 34 candidate genes in bupropion and placebo remission., Int J Neuropsychopharmacol

Swan GE et al., 2005, Dopamine receptor DRD2 genotype and smoking cessation outcome following treatment with bupropion SR., Pharmacogenomics J

Choi HD et al., 2015, Lack of association between DRD2 Taq1A gene polymorphism and smoking cessation therapy: a meta-analysis., Int J Clin Pharmacol Ther

TTD: Bupropion
- Version: 2020.06.01
Alternate Names:

D0X4ZR TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL894
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Trial Name	BVF-033,Aplenzin
Novel drug target	Established target
Trial Name	Contrave

BUPROPION Drug Record

BUPROPION chembl:CHEMBL894 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22041458

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26153084 25881752 18058343 17654295 15492764 14570538

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22947179

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name BVF-033,Aplenzin Novel drug target Established target Trial Name Contrave

PMIDs: 12183670 12589396 9537821 15787205 12185406 14550679 11752352 15361919 28220701 16923164 27541930

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name BVF-033,Aplenzin Novel drug target Established target Trial Name Contrave

PMIDs: 15361919 12909199 16893531 11752352 28220701 16923164

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16123753 10395223 9672901 19944883 19853839 1969501 19603545 19396436 19373123 19273465 19179847 18926547 18855532 18781857 18781856 1839129 18354387 18180754 18086475 17989061 17767146 15830237 15492764 15286066 15184239 15146457 15077009 12587665 11329406 10862524 10823405

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22947179

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22947179

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26132489

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16876132

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 3109881

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21658141

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22947179

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22947179

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

TEND: BUPROPION

Alternate Names: BUPROPION Primary Drug Name

Drug Info: Year of Approval 1985 Drug Class antidepressive agents

Publications:

TdgClinicalTrial: BUPROPION

Alternate Names:

Drug Info: Drug Indications antidepressant,appetite suppressant,smoking-cessation agent Drug Class Small Molecule FDA Approval approved

Interaction Types & Directionality:

n/a

PMIDs:
22041458

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26153084 25881752 18058343 17654295 15492764 14570538

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22947179

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BVF-033,Aplenzin

Novel drug target Established target

Trial Name Contrave

PMIDs:
12183670 12589396 9537821 15787205 12185406 14550679 11752352 15361919 28220701 16923164 27541930

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BVF-033,Aplenzin

Novel drug target Established target

Trial Name Contrave

PMIDs:
15361919 12909199 16893531 11752352 28220701 16923164

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
16123753 10395223 9672901 19944883 19853839 1969501 19603545 19396436 19373123 19273465 19179847 18926547 18855532 18781857 18781856 1839129 18354387 18180754 18086475 17989061 17767146 15830237 15492764 15286066 15184239 15146457 15077009 12587665 11329406 10862524 10823405

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22947179

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22947179

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26132489

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16876132

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
3109881

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
21658141

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22947179

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22947179

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Alternate Names:

BUPROPION Primary Drug Name

Drug Info:

Year of Approval 1985

Drug Class antidepressive agents

Drug Info:

Drug Indications antidepressant,appetite suppressant,smoking-cessation agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C1317 NCI drug code

Publications:

de Greef et al., 1987, Control of prolactin release induced by suckling., Endocrinology

Alternate Names:

D0X4ZR TTD Drug ID