DGIdb - DONEPEZIL Drug Record

DONEPEZIL chembl:CHEMBL502 Approved

Alternate Names:

E-2020
ARICEPT
DONEPEZIL
ARICEPT®
DONEPEZILO
DONEPEZILUM
DOMEPEZIL
pubchem.compound:3152
chembl:CHEMBL502
chemidplus:120014-06-4
rxcui:135447
drugbank:00843

Drug Info:

Year of Approval	1996
Drug Class	nootropic agents
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	for treatment of alzheimer's disease
Drug Categories	piperidines
Drug Categories	bcrp/abcg2 substrates
Drug Categories	central nervous system depressants
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 substrates
Drug Categories	indans
Drug Categories	muscle relaxants
Drug Categories	muscle relaxants, centrally acting agents
Drug Categories	parasympathomemetic (cholinergic) agents
Drug Categories	qtc prolonging agents

(6 More Sources)

Publications:

Kryger et al., 1999, Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs., Structure
Davis, 1999, Alzheimer's disease: seeking new ways to preserve brain function. Interview by Alice V. Luddington., Geriatrics
Shepherd et al., Donepezil overdose: a tenfold dosing error., Ann Pharmacother
Repantis et al., 2010, Acetylcholinesterase inhibitors and memantine for neuroenhancement in healthy individuals: a systematic review., Pharmacol. Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Kosasa et al., 1999, Effect of donepezil hydrochloride (E2020) on basal concentration of extracellular acetylcholine in the hippocampus of rats., Eur. J. Pharmacol.
Jann, 2000, Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease., Pharmacotherapy
Ki et al., 2010, Donepezil, a potent acetylcholinesterase inhibitor, induces caspase-dependent apoptosis in human promyelocytic leukemia HL-60 cells., Biol. Pharm. Bull.
Sugimoto, 2001, Donepezil hydrochloride: a treatment drug for Alzheimer's disease., Chem Rec
Huang L et al., 2014, Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease., Eur J Med Chem
Braga IL et al., 2015, Effect of APOE and CHRNA7 genotypes on the cognitive response to cholinesterase inhibitor treatment at different stages of Alzheimer's disease., Am J Alzheimers Dis Other Demen
Hayslett et al., 2003, Effects of donepezil on DOI-induced head twitch response in mice: implications for Tourette syndrome., Pharmacol. Biochem. Behav.
Hayslett et al., 2005, Effects of donepezil, nicotine and haloperidol on the central serotonergic system in mice: implications for Tourette's syndrome., Pharmacol. Biochem. Behav.
Coin A et al., 2016, Donepezil plasma concentrations, CYP2D6 and CYP3A4 phenotypes, and cognitive outcome in Alzheimer's disease., Eur J Clin Pharmacol
Noetzli M et al., 2014, Population pharmacokinetic approach to evaluate the effect of CYP2D6, CYP3A, ABCB1, POR and NR1I2 genotypes on donepezil clearance., Br J Clin Pharmacol
Yoon H et al., 2015, Association of the choline acetyltransferase gene with responsiveness to acetylcholinesterase inhibitors in Alzheimer's disease., Pharmacopsychiatry
Bullock et al., 2005, Rivastigmine and donepezil treatment in moderate to moderately-severe Alzheimer's disease over a 2-year period., Curr Med Res Opin
Heydorn, 1997, Donepezil (E2020): a new acetylcholinesterase inhibitor. Review of its pharmacology, pharmacokinetics, and utility in the treatment of Alzheimer's disease., Expert Opin Investig Drugs
Sokolow S et al., 2017, Deleterious Effect of Butyrylcholinesterase K-Variant in Donepezil Treatment of Mild Cognitive Impairment., J Alzheimers Dis
De Beaumont L et al., 2016, Butyrylcholinesterase K and Apolipoprotein E-ɛ4 Reduce the Age of Onset of Alzheimer's Disease, Accelerate Cognitive Decline, and Modulate Donepezil Response in Mild Cognitively Impaired Subjects., J Alzheimers Dis
Scacchi R et al., 2009, Variability of AChE, BChE, and ChAT genes in the late-onset form of Alzheimer's disease and relationships with response to treatment with Donepezil and Rivastigmine., Am J Med Genet B Neuropsychiatr Genet
Blesa R et al., 2006, Effect of butyrylcholinesterase genotype on the response to rivastigmine or donepezil in younger patients with Alzheimer's disease., Pharmacogenet Genomics
Liston DR et al., 2004, Pharmacology of selective acetylcholinesterase inhibitors: implications for use in Alzheimer's disease., Eur J Pharmacol
Seltzer B, 2005, Donepezil: a review., Expert Opin Drug Metab Toxicol
Nordberg A et al., 2013, A review of butyrylcholinesterase as a therapeutic target in the treatment of Alzheimer's disease., Prim Care Companion CNS Disord
Ogura H et al., 2000, Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro., Methods Find Exp Clin Pharmacol
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
Leyhe et al., 2008, Increase of BDNF serum concentration during donepezil treatment of patients with early Alzheimer's disease., Eur Arch Psychiatry Clin Neurosci
Shen H et al., 2010, Neuroprotection by donepezil against glutamate excitotoxicity involves stimulation of alpha7 nicotinic receptors and internalization of NMDA receptors., Br J Pharmacol
Hwang J et al., 2010, Microglia signaling as a target of donepezil., Neuropharmacology
Kim HG et al., 2014, Donepezil inhibits the amyloid-beta oligomer-induced microglial activation in vitro and in vivo., Neurotoxicology
Srinivasan M et al., 2015, Significance of NF-κB as a pivotal therapeutic target in the neurodegenerative pathologies of Alzheimer's disease and multiple sclerosis., Expert Opin Ther Targets
Reale M et al., 2005, Acetylcholinesterase inhibitors effects on oncostatin-M, interleukin-1 beta and interleukin-6 release from lymphocytes of Alzheimer's disease patients., Exp Gerontol
Zhang T et al., 2015, Donepezil attenuates high glucose-accelerated senescence in human umbilical vein endothelial cells through SIRT1 activation., Cell Stress Chaperones
Nakahata K et al., 2008, Cholinesterase inhibitor donepezil dilates cerebral parenchymal arterioles via the activation of neuronal nitric oxide synthase., Anesthesiology
Haraguchi Y et al., 2017, Donepezil suppresses intracellular Ca<sup>2+</sup> mobilization through the PI3K pathway in rodent microglia., J Neuroinflammation

DONEPEZIL TNFAIP6

Interaction Score: 4.37

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
20153342

Sources:
DrugBank
DONEPEZIL BCHE

Interaction Score: 1.54

Interaction Types & Directionality:

inducer (activating)

Interaction Info:

PMIDs:
16083542 15989517 27911294 27567841 18780301 17047484 14751402 16863459 23930233 11256231

Sources:
DrugBank NCI PharmGKB
DONEPEZIL ACHE

Interaction Score: 1.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
10368299 10024872 10466911 20193764 11752352 10513568 10641971 20522977 11893059 25282266

Sources:
DTC DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
DONEPEZIL CHAT

Interaction Score: 0.79

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25730470

Sources:
PharmGKB
DONEPEZIL IL1B

Interaction Score: 0.37

Interaction Types & Directionality:

inhibitor (inhibitory)

inducer (activating)

Interaction Info:

PMIDs:
15763393 26194321 20153342

Sources:
DrugBank
DONEPEZIL NOS1

Interaction Score: 0.29

Interaction Types & Directionality:

inducer (activating)

inhibitor (inhibitory)

Interaction Info:

PMIDs:
20153342 18580182 29273047

Sources:
DrugBank
DONEPEZIL NFKB2

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
24189446 25652642

Sources:
DrugBank
DONEPEZIL CHRNA7

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24951635

Sources:
PharmGKB
DONEPEZIL GRIN1

Interaction Score: 0.13

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

PMIDs:
20718745

Sources:
DrugBank
DONEPEZIL BDNF

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17990049

Sources:
NCI
DONEPEZIL CYP3A5

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
DONEPEZIL HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

inducer (activating)

Interaction Info:

PMIDs:
14643839 16045972

Sources:
DrugBank
DONEPEZIL CYP2D6

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26952092 24433464

Sources:
PharmGKB FDA

DrugBank: DB00843

Version: 5.1.7

Alternate Names:

DONEPEZIL DrugBank Drug Name

120014-06-4 CAS Number

Accel-donepezil Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories anti-dementia drugs

Publications:

Shen H et al., 2010, Neuroprotection by donepezil against glutamate excitotoxicity involves stimulation of alpha7 nicotinic receptors and internalization of NMDA receptors., Br J Pharmacol

Srinivasan M et al., 2015, Significance of NF-κB as a pivotal therapeutic target in the neurodegenerative pathologies of Alzheimer's disease and multiple sclerosis., Expert Opin Ther Targets

Kim HG et al., 2014, Donepezil inhibits the amyloid-beta oligomer-induced microglial activation in vitro and in vivo., Neurotoxicology

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

DONEPEZIL Primary Drug Name

Drug Info:

Drug Class nootropic agents

Year of Approval 1996

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

Drug Info:

Drug Indications for treatment of alzheimer's disease

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: DONEPEZIL

Version: 14-September-2017

Alternate Names:

C2603 NCI drug code

Drug Info:

Publications:

Heydorn, 1997, Donepezil (E2020): a new acetylcholinesterase inhibitor. Review of its pharmacology, pharmacokinetics, and utility in the treatment of Alzheimer's disease., Expert Opin Investig Drugs

Bullock et al., 2005, Rivastigmine and donepezil treatment in moderate to moderately-severe Alzheimer's disease over a 2-year period., Curr Med Res Opin

Leyhe et al., 2008, Increase of BDNF serum concentration during donepezil treatment of patients with early Alzheimer's disease., Eur Arch Psychiatry Clin Neurosci

DTC: DONEPEZIL
- Version: 02-September-2020
Alternate Names:

CHEMBL502 ChEMBL Drug ID

Drug Info:

Publications:

Huang L et al., 2014, Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease., Eur J Med Chem

PharmGKB: donepezil

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Noetzli M et al., 2014, Population pharmacokinetic approach to evaluate the effect of CYP2D6, CYP3A, ABCB1, POR and NR1I2 genotypes on donepezil clearance., Br J Clin Pharmacol

Coin A et al., 2016, Donepezil plasma concentrations, CYP2D6 and CYP3A4 phenotypes, and cognitive outcome in Alzheimer's disease., Eur J Clin Pharmacol

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

TTD: Donepezil
- Version: 2020.06.01
Alternate Names:

D0NS6H TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103212
- Version: 29-September-2020
Alternate Names:

DONEPEZIL GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL502
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

Publications:

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

DONEPEZIL	DrugBank Drug Name
120014-06-4	CAS Number
Accel-donepezil	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	anti-dementia drugs

inhibitor (inhibitory)
inducer (activating)

inducer (activating)
inhibitor (inhibitory)

DONEPEZIL Drug Record

DONEPEZIL chembl:CHEMBL502 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 20153342

Sources: DrugBank

Interaction Types & Directionality: inducer (activating)

Interaction Info:

PMIDs: 16083542 15989517 27911294 27567841 18780301 17047484 14751402 16863459 23930233 11256231

Sources: DrugBank NCI PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 10368299 10024872 10466911 20193764 11752352 10513568 10641971 20522977 11893059 25282266

Sources: DTC DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25730470

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory) inducer (activating)

Interaction Info:

PMIDs: 15763393 26194321 20153342

Sources: DrugBank

Interaction Types & Directionality: inducer (activating) inhibitor (inhibitory)

Interaction Info:

PMIDs: 20153342 18580182 29273047

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 24189446 25652642

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24951635

Sources: PharmGKB

Interaction Types & Directionality: negative modulator (inhibitory)

Interaction Info:

PMIDs: 20718745

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17990049

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978

Sources: PharmGKB

Interaction Types & Directionality: inducer (activating)

Interaction Info:

PMIDs: 14643839 16045972

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26952092 24433464

Sources: PharmGKB FDA

DrugBank: DB00843

Alternate Names: DONEPEZIL DrugBank Drug Name 120014-06-4 CAS Number Accel-donepezil Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Categories anti-dementia drugs

TEND: DONEPEZIL

Alternate Names: DONEPEZIL Primary Drug Name

Drug Info: Drug Class nootropic agents Year of Approval 1996

Publications:

TdgClinicalTrial: DONEPEZIL

Alternate Names:

Drug Info: Drug Indications for treatment of alzheimer's disease Drug Class Small Molecule FDA Approval approved

Publications:

NCI: DONEPEZIL

Alternate Names: C2603 NCI drug code

Drug Info:

DTC: DONEPEZIL

Alternate Names: CHEMBL502 ChEMBL Drug ID

Drug Info:

Publications: Huang L et al., 2014, Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease., Eur J Med Chem

PharmGKB: donepezil

Alternate Names:

Drug Info:

TTD: Donepezil

Alternate Names: D0NS6H TTD Drug ID

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
20153342

Sources:
DrugBank

Interaction Types & Directionality:

inducer (activating)

PMIDs:
16083542 15989517 27911294 27567841 18780301 17047484 14751402 16863459 23930233 11256231

Sources:
DrugBank NCI PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
10368299 10024872 10466911 20193764 11752352 10513568 10641971 20522977 11893059 25282266

Sources:
DTC DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
25730470

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

inducer (activating)

PMIDs:
15763393 26194321 20153342

Sources:
DrugBank

Interaction Types & Directionality:

inducer (activating)

inhibitor (inhibitory)

PMIDs:
20153342 18580182 29273047

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
24189446 25652642

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
24951635

Sources:
PharmGKB

Interaction Types & Directionality:

negative modulator (inhibitory)

PMIDs:
20718745

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
17990049

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
18695978

Sources:
PharmGKB

Interaction Types & Directionality:

inducer (activating)

PMIDs:
14643839 16045972

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
26952092 24433464

Sources:
PharmGKB FDA

Alternate Names:

DONEPEZIL DrugBank Drug Name

120014-06-4 CAS Number

Accel-donepezil Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories anti-dementia drugs

Alternate Names:

DONEPEZIL Primary Drug Name

Drug Info:

Drug Class nootropic agents

Year of Approval 1996

Drug Info:

Drug Indications for treatment of alzheimer's disease

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C2603 NCI drug code

Alternate Names:

CHEMBL502 ChEMBL Drug ID

Publications:

Huang L et al., 2014, Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease., Eur J Med Chem

Alternate Names:

D0NS6H TTD Drug ID

Alternate Names:

DONEPEZIL GuideToPharmacology Ligand Name