DGIdb - SERTRALINE Drug Record

SERTRALINE chembl:CHEMBL809 Approved

Alternate Names:

SERTRALINE
ZOLOFT®
CP-519741
SERTRALINE HYDROCHLORIDE
(+)-SERTRALINE
CP 51974
CP-51974-1
(1S,4S)-SERTRALINE
(1S-CIS)-1,2,3,4-TETRAHYDRO-4-(3,4-DICHLOROPHENYL)-N-METHYL-1-NAPHTHALENAMINE
CIS-(+)-SERTRALINE
LUSTRAL®
SERTRALINA
SERTRALINUM
ZOLOFT
chembl:CHEMBL809
drugbank:01104
rxcui:36437
chemidplus:79617-96-2
pubchem.compound:68617

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antidepressant,for treatment of obsessive compulsive disorder (OCD)
Year of Approval	1991
Drug Class	antidepressive agents
Drug Categories	agents that reduce seizure threshold
Drug Categories	central nervous system depressants
Drug Categories	cytochrome p-450 cyp2b6 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c9 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp2e1 substrates
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs causing inadvertant photosensitivity
Drug Categories	hypoglycemia-associated agents
Drug Categories	monoamine oxidase a substrates
Drug Categories	p-glycoprotein inhibitors
Drug Categories	photosensitizing agents
Drug Categories	qtc prolonging agents
Drug Categories	serotonergic drugs shown to increase risk of serotonin syndrome

(4 More Sources)

Publications:

Firouzabadi D et al., 2019, Response to sertraline is influenced by GNβ3 gene G-350A variant in patients with major depressive disorder., Eur J Clin Pharmacol
Yang Z et al., 2012, Association of APC and REEP5 gene polymorphisms with major depression disorder and treatment response to antidepressants in a Han Chinese population., Gen Hosp Psychiatry
Benmansour et al., 2002, Serotonin clearance in vivo is altered to a greater extent by antidepressant-induced downregulation of the serotonin transporter than by acute blockade of this transporter., J. Neurosci.
Benmansour et al., 1999, Effects of chronic antidepressant treatments on serotonin transporter function, density, and mRNA level., J. Neurosci.
Iehlé et al., 1993, Baculovirus-directed expression of human prostatic steroid 5 alpha-reductase 1 in an active form., J. Steroid Biochem. Mol. Biol.
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Chen et al., 2005, Characterization of an allosteric citalopram-binding site at the serotonin transporter., J. Neurochem.
Borkowska et al., [The effect of sertraline on cognitive functions in patients with obsessive-compulsive disorder]., Psychiatr. Pol.
Durham et al., 2004, The serotonin transporter polymorphism, 5HTTLPR, is associated with a faster response time to sertraline in an elderly population with major depressive disorder., Psychopharmacology (Berl.)
David et al., 2001, Comparison of antidepressant activity in 4- and 40-week-old male mice in the forced swimming test: involvement of 5-HT1A and 5-HT1B receptors in old mice., Psychopharmacology (Berl.)
Muneoka et al., 2009, Brain region-specific effects of short-term treatment with duloxetine, venlafaxine, milnacipran and sertraline on monoamine metabolism in rats., Neurochem. Res.
Rogóz et al., Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats., Pharmacol Rep
MacDonald ML et al., 2006, Identifying off-target effects and hidden phenotypes of drugs in human cells., Nat Chem Biol
Niitsu T et al., 2013, Pharmacogenetics in major depression: a comprehensive meta-analysis., Prog Neuropsychopharmacol Biol Psychiatry
Ishiguro S et al., 2011, Determinants of pharmacodynamic trajectory of the therapeutic response to paroxetine in Japanese patients with panic disorder., Eur J Clin Pharmacol
Yevtushenko OO et al., 2010, Early response to selective serotonin reuptake inhibitors in panic disorder is associated with a functional 5-HT1A receptor gene polymorphism., J Affect Disord
Illi A et al., 2009, 5-HTR1A, 5-HTR2A, 5-HTR6, TPH1 and TPH2 polymorphisms and major depression., Neuroreport
Kato M et al., 2009, Effect of 5-HT1A gene polymorphisms on antidepressant response in major depressive disorder., Am J Med Genet B Neuropsychiatr Genet
Baune BT et al., 2008, Serotonin receptor 1A-1019C/G variant: impact on antidepressant pharmacoresponse in melancholic depression?, Neurosci Lett
Drago A et al., 2008, 5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies., Int J Neuropsychopharmacol
Bahramali E et al., 2016, Influence of ACE gene on differential response to sertraline versus fluoxetine in patients with major depression: a randomized controlled trial., Eur J Clin Pharmacol
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
Lemke, 2007, [Antidepressant effects of dopamine agonists. Experimental and clinical findings]., Nervenarzt
Nemeroff et al., 2004, Pharmacologic differences among the SSRIs: focus on monoamine transporters and the HPA axis., CNS Spectr
Ghanizadeh, 2008, Sertraline-associated hair loss., J Drugs Dermatol
Goodnick et al., 1998, Selective serotonin reuptake inhibitors in affective disorders--I. Basic pharmacology., J. Psychopharmacol. (Oxford)
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
Breitenstein B et al., 2016, Association of ABCB1 gene variants, plasma antidepressant concentration, and treatment response: Results from a randomized clinical study., J Psychiatr Res
Huang X et al., 2013, ABCB6, ABCB1 and ABCG1 genetic polymorphisms and antidepressant response of SSRIs in Chinese depressive patients., Pharmacogenomics
de Klerk OL et al., 2013, ABCB1 gene variants influence tolerance to selective serotonin reuptake inhibitors in a large sample of Dutch cases with major depressive disorder., Pharmacogenomics J
Uhr M et al., 2008, Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression., Neuron
Yuce-Artun N et al., 2016, Influence of CYP2B6 and CYP2C19 polymorphisms on sertraline metabolism in major depression patients., Int J Clin Pharm
Zhou M et al., 2007, Evidence for significant contribution of a newly identified monoamine transporter (PMAT) to serotonin uptake in the human brain., Biochem Pharmacol
Haenisch B et al., 2010, Interaction of the human plasma membrane monoamine transporter (hPMAT) with antidepressants and antipsychotics., Naunyn Schmiedebergs Arch Pharmacol
Daws LC, 2009, Unfaithful neurotransmitter transporters: focus on serotonin uptake and implications for antidepressant efficacy., Pharmacol Ther
Sørensen L et al., 2012, Interaction of antidepressants with the serotonin and norepinephrine transporters: mutational studies of the S1 substrate binding pocket., J Biol Chem
Narita N et al., 1996, Interactions of selective serotonin reuptake inhibitors with subtypes of sigma receptors in rat brain., Eur J Pharmacol
Fishback JA et al., 2010, Sigma receptors: potential targets for a new class of antidepressant drug., Pharmacol Ther

SERTRALINE P3H3

Interaction Score: 2.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30324302

Sources:
PharmGKB
SERTRALINE PGRMC1

Interaction Score: 2.37

Interaction Types & Directionality:

inhibitor (inhibitory)

binder

Interaction Info:

PMIDs:
8831113 20438757

Sources:
DrugBank
SERTRALINE SRP19

Interaction Score: 1.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22795047

Sources:
PharmGKB
SERTRALINE REEP5

Interaction Score: 1.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22795047

Sources:
PharmGKB
SERTRALINE SLC29A4

Interaction Score: 0.86

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17046718 20012264 19022290

Sources:
DrugBank
SERTRALINE CFL1

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16680159

Sources:
DTC
SERTRALINE SLC6A4

Interaction Score: 0.37

Interaction Types & Directionality:

inhibitor (inhibitory)

binder

negative modulator (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
12151556 10575045 8664165 9537821 15606893 12647451 12955294 11243491 18751896 16963794

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology
SERTRALINE GNB3

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30324302

Sources:
PharmGKB
SERTRALINE SLC6A3

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

binder

Interaction Info:

Trial Name Zoloft

Novel drug target Established target

PMIDs:
17187269 15181382 18664165 9537821 9808077

Sources:
DrugBank TdgClinicalTrial
SERTRALINE HLA-A

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
SERTRALINE HTR1A

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23733030 21688171 19800133 19590397 18484082 18387740 18047755

Sources:
PharmGKB
SERTRALINE JUN

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16680159

Sources:
DTC
SERTRALINE CYP2B6

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26830411

Sources:
PharmGKB
SERTRALINE SLC6A2

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

negative modulator (inhibitory)

Interaction Info:

PMIDs:
9537821 23086945

Sources:
DrugBank
SERTRALINE CDK1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16680159

Sources:
DTC
SERTRALINE ACE

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27262302

Sources:
PharmGKB
SERTRALINE COMT

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
SERTRALINE ABCB1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26704739 24192121 22641028 18215618

Sources:
PharmGKB
SERTRALINE CYP3A5

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
SERTRALINE DRD1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SERTRALINE TP53

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16680159

Sources:
DTC
SERTRALINE ATXN2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SERTRALINE IDH1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SERTRALINE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528

Sources:
PharmGKB

DrugBank: DB01104

Version: 5.1.7

Alternate Names:

SERTRALINE DrugBank Drug Name

79617-96-2 CAS Number

Act Sertraline Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories agents that reduce seizure threshold

Publications:

Daws LC, 2009, Unfaithful neurotransmitter transporters: focus on serotonin uptake and implications for antidepressant efficacy., Pharmacol Ther

Haenisch B et al., 2010, Interaction of the human plasma membrane monoamine transporter (hPMAT) with antidepressants and antipsychotics., Naunyn Schmiedebergs Arch Pharmacol

Zhou M et al., 2007, Evidence for significant contribution of a newly identified monoamine transporter (PMAT) to serotonin uptake in the human brain., Biochem Pharmacol

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

SERTRALINE Primary Drug Name

Drug Info:

Drug Class antidepressive agents

Year of Approval 1991

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

Drug Info:

Drug Indications antidepressant,for treatment of obsessive compulsive disorder (OCD)

Drug Class Small Molecule

FDA Approval approved

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

CHEMBL809 ChEMBL Drug ID

Drug Info:

Publications:

MacDonald ML et al., 2006, Identifying off-target effects and hidden phenotypes of drugs in human cells., Nat Chem Biol

PharmGKB: sertraline

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Yang Z et al., 2012, Association of APC and REEP5 gene polymorphisms with major depression disorder and treatment response to antidepressants in a Han Chinese population., Gen Hosp Psychiatry

Firouzabadi D et al., 2019, Response to sertraline is influenced by GNβ3 gene G-350A variant in patients with major depressive disorder., Eur J Clin Pharmacol

Drago A et al., 2008, 5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies., Int J Neuropsychopharmacol

GuideToPharmacology: 178101500
- Version: 29-September-2020
Alternate Names:

SERTRALINE GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Sertraline
- Version: 2020.06.01
Alternate Names:

D0K0TC TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL809
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

SERTRALINE	DrugBank Drug Name
79617-96-2	CAS Number
Act Sertraline	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	agents that reduce seizure threshold

inhibitor (inhibitory)
binder

inhibitor (inhibitory)
binder
negative modulator (inhibitory)

inhibitor (inhibitory)
binder

Trial Name	Zoloft
Novel drug target	Established target

SERTRALINE Drug Record

SERTRALINE chembl:CHEMBL809 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30324302

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory) binder

Interaction Info:

PMIDs: 8831113 20438757

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22795047

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22795047

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17046718 20012264 19022290

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16680159

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory) binder negative modulator (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: 12151556 10575045 8664165 9537821 15606893 12647451 12955294 11243491 18751896 16963794

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30324302

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory) binder

Interaction Info: Trial Name Zoloft Novel drug target Established target

PMIDs: 17187269 15181382 18664165 9537821 9808077

Sources: DrugBank TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23733030 21688171 19800133 19590397 18484082 18387740 18047755

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16680159

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26830411

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory) negative modulator (inhibitory)

Interaction Info:

PMIDs: 9537821 23086945

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16680159

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27262302

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26704739 24192121 22641028 18215618

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978

Interaction Types & Directionality:

n/a

PMIDs:
30324302

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

binder

PMIDs:
8831113 20438757

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
22795047

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22795047

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
17046718 20012264 19022290

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
16680159

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

binder

negative modulator (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
12151556 10575045 8664165 9537821 15606893 12647451 12955294 11243491 18751896 16963794

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
30324302

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

binder

Interaction Info:

Trial Name Zoloft

Novel drug target Established target

PMIDs:
17187269 15181382 18664165 9537821 9808077

Sources:
DrugBank TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23733030 21688171 19800133 19590397 18484082 18387740 18047755

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16680159

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
26830411

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

negative modulator (inhibitory)

PMIDs:
9537821 23086945

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
16680159

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
27262302

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26704739 24192121 22641028 18215618

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18695978

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
16680159

Sources:
DTC

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:
9187528

Sources:
PharmGKB

Alternate Names:

SERTRALINE DrugBank Drug Name

79617-96-2 CAS Number

Act Sertraline Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories agents that reduce seizure threshold

Alternate Names:

SERTRALINE Primary Drug Name

Drug Info:

Drug Class antidepressive agents

Year of Approval 1991

Drug Info:

Drug Indications antidepressant,for treatment of obsessive compulsive disorder (OCD)

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

CHEMBL809 ChEMBL Drug ID