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Modafinil

drug
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Also known as CEP 1538CEP-1538CRC-40476CRL 40476CRL-40476DEP-1538Modafinil civMODAFINIL COMPONENT OF THN-102MODAFINIL COMPONENT OF THN102ModafiniloModaphonilModiodalNSC-751178NSC-759110ProvigilSID26719679SID26749058SID26753746SID144205023

Summary

Modafinil (CHEMBL1373) is an approved small molecule (ATC N06BA07) targeting SLC6A3; indicated across 36 conditions including attention deficit-hyperactivity disorder and obstructive sleep apnea syndrome.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N06BA07
  • Targets: 1 (SLC6A3)
  • Indications: 36 conditions
  • Clinical trials: 143
  • Chemistry: 273.4 Da · C15H15NO2S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1373
NameModafinil
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID4236
ChEBICHEBI:77585
ATCN06BA07
Molecular formulaC15H15NO2S
Molecular weight273.4
InChIKeyYFGHCGITMMYXAQ-UHFFFAOYSA-N

SMILES: C1=CC=C(C=C1)C(C2=CC=CC=C2)S(=O)CC(=O)N

IUPAC name: 2-benzhydrylsulfinylacetamide

ChEBI definition: A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group.

Also known as: CEP 1538, CEP-1538, CRC-40476, CRL 40476, CRL-40476, DEP-1538, Modafinil, Modafinil civ, MODAFINIL COMPONENT OF THN-102, MODAFINIL COMPONENT OF THN102, Modafinilo, Modaphonil

Patent coverage: 3,722 distinct patent families (14,293 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
SLC6A3DATInhibition5.420.2%Q01959

Broader ChEMBL bioactivity targets: 11 (assay-derived). Sample: Prelamin-A/C, Endothelin receptor type B, D(3) dopamine receptor, Sodium-dependent dopamine transporter, Adenosine receptor A3, Melanocortin receptor 4, Sodium-dependent serotonin transporter, Sodium-dependent dopamine transporter, Cytochrome P450 2C19, Mitogen-activated protein kinase 1.

Bioactivity

ChEMBL activities: 20 potent at pChembl ≥ 5 of 33 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
LMNA8.74Potency1.8nMCHEMBL_ACT_3642546
SLC6A36.03Ki927nMCHEMBL_ACT_16772105
SLC6A35.84Ki1456nMCHEMBL_ACT_7754236
SLC6A35.74IC501832nMCHEMBL_ACT_7754235
SLC6A35.7Ki2000nMCHEMBL_ACT_16771864
P239775.6Ki2520nMCHEMBL_ACT_27439070
P239775.6Ki2520nMCHEMBL_ACT_28241264
P239775.6Ki2520nMCHEMBL_ACT_28904291
P239775.6Ki2520nMCHEMBL_ACT_5208035
P239775.58Ki2600nMCHEMBL_ACT_13943515
SLC6A35.51Ki3090nMCHEMBL_ACT_13941682
P239775.43IC503700nMCHEMBL_ACT_10891454
P239775.43IC503700nMCHEMBL_ACT_10926091
P239775.43IC503700nMCHEMBL_ACT_8060565
P239775.42Ki3800nMCHEMBL_ACT_1489157
P239775.37IC504300nMCHEMBL_ACT_10926961
P239775.37IC504300nMCHEMBL_ACT_8060563
P239775.09Ki8160nMCHEMBL_ACT_20645100
P239775.09Ki8160nMCHEMBL_ACT_22798420
SLC6A35.03AC509350nMCHEMBL_ACT_25124440

Target pathways

Aggregated over 1 target gene(s): SLC6A3.

Top Reactome pathways

13 total, by targets touching each:

PathwayTargetsGenes
Neurotransmitter clearance1SLC6A3
Transmission across Chemical Synapses1SLC6A3
Neuronal System1SLC6A3
Disease1SLC6A3
Dopamine clearance from the synaptic cleft1SLC6A3
Transport of small molecules1SLC6A3
R-HSA-4253661SLC6A3
SLC-mediated transmembrane transport1SLC6A3
SLC-mediated transport of neurotransmitters1SLC6A3
Defective neurotransmitter clearance by SLC6A3 causes Parkinsonism-dystonia infantile (PKDYS)1SLC6A3
SLC transporter disorders1SLC6A3
Disorders of transmembrane transporters1SLC6A3
Defective transport of neurotransmitters by SLC6A3 causes Parkinsonism-dystonia infantile (PKDYS)1SLC6A3

Dominant GO biological processes

GO termTargets
neurotransmitter transport1
amino acid transport1
lactation1
sensory perception of smell1
locomotory behavior1
response to xenobiotic stimulus1
response to iron ion1
obsolete monoamine transport1
obsolete dopamine transport1
adenohypophysis development1
response to nicotine1
sodium ion transmembrane transport1
positive regulation of multicellular organism growth1
regulation of dopamine metabolic process1
response to cocaine1

Indications & clinical

Indications

36 indications (4 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
attention deficit-hyperactivity disorder4MONDO:0007743EFO:0003888
obstructive sleep apnea syndrome4MONDO:0007147EFO:0003918
narcolepsy4MONDO:0021107MONDO:0021107
cocaine dependence3MONDO:0005186EFO:0002610
brain neoplasm3MONDO:0021211EFO:0003833
Ewing sarcoma3MONDO:0012817EFO:0000174
stroke disorder3MONDO:0005098EFO:0000712
postpoliomyelitis syndrome3MONDO:0017416EFO:0007454
sleep disorder3MONDO:0100081EFO:0008568
major depressive disorder3MONDO:0002009MONDO:0002009
Alzheimer disease3MONDO:0004975MONDO:0004975
multiple sclerosis3MONDO:0005301MONDO:0005301
methamphetamine dependence2MONDO:0005419EFO:0004701
post-traumatic stress disorder2MONDO:0005146EFO:0001358
drug dependence2MONDO:0005303EFO:0003890
opiate dependence2MONDO:0005530EFO:0005611
depressive disorder2MONDO:0002050MONDO:0002050
Parkinson disease2MONDO:0005180MONDO:0005180
alcohol abuse2MONDO:0002046MONDO:0007079
ovarian carcinoma2MONDO:0005140EFO:0001075
orthostatic hypotension1MONDO:0005469EFO:0005252
sleep apnea syndrome1MONDO:0005296EFO:0003877
melanoma1MONDO:0005105EFO:0000756
nicotine dependence1MONDO:0008575EFO:0003768
insomnia1MONDO:0013600EFO:0004698
schizoaffective disorder1MONDO:0005487EFO:0005411
metastatic melanoma1MONDO:0005191EFO:0002617

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

Clinical trials

Total trials: 143.

Phase distribution

PhaseTrials
PHASE240
PHASE327
PHASE122
Not specified22
PHASE420
PHASE1/PHASE25
EARLY_PHASE14
PHASE2/PHASE33

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06041048PHASE4RECRUITINGInvestigation of Locus Coeruleus Function in Sustained Attention
NCT00102284PHASE4TERMINATEDNeuromodulation and Language Acquisition (Project Stage Ia)
NCT00118378PHASE4COMPLETEDEffectiveness of Modafinil for Treating Fatigue in Adults With HIV/AIDS
NCT00124384PHASE4COMPLETEDThe Effects of Modafinil on Waking Function and on Sleep in Individuals With Primary Insomnia
NCT00208715PHASE4COMPLETEDProvigil in Conjunction With SSRIs for the Treatment of Mild or Moderate Depression With Attendant Symptoms of Sleepiness and Fatigue.
NCT00423943PHASE4COMPLETEDModafinil for Treatment of Cognitive Dysfunction in Schizophrenia
NCT00573417PHASE4COMPLETEDA Placebo-Controlled Trial of Modafinil (Provigil) Added to Clozapine in Patients With Schizophrenia
NCT00614926PHASE4COMPLETEDModafinil for Treatment of Fatigue in ALS Patients
NCT00626210PHASE4TERMINATEDModafinil Treatment for Sleep/Wake Disturbances in Older Adults
NCT00711464PHASE4COMPLETEDModafinil Effects on Cognition in Schizophrenia Patients
NCT00751023PHASE4COMPLETEDEffects of Modafinil in Methamphetamine Dependence
NCT00829322PHASE4COMPLETEDModafinil for the Treatment of Fatigue in Lung Cancer V9.0
NCT01365897PHASE4COMPLETEDEffectiveness of Modafinil in Improving Cognitive Performance of University Students
NCT01913327PHASE4TERMINATEDAntipsychotic Effects on Brain Function in Schizophrenia
NCT01965925PHASE4COMPLETEDTargeting Circadian and Cognitive Dysfunction in Bipolar Disorder With Modafinil
NCT02155257PHASE4COMPLETEDPain Expectations in Subjects With Osteoarthritis
NCT02385656PHASE4UNKNOWNThe Efficacy and Tolerability of Modafinil for Fatigue and Daytime Sleepiness in Cancer Patients: Preliminary Study
NCT02494102PHASE4TERMINATEDEvaluation of Modafinil vs Placebo for Treatment of Anesthesia Delayed Emergence in Obstructive Sleep Apnea
NCT03616717PHASE4COMPLETEDModafinil Effects on EEG Biomarkers of Reward and Motivation
NCT03621761PHASE4COMPLETEDCognitive Behavioral Therapy, Modafinil, or Both for Multiple Sclerosis Fatigue
NCT06354985PHASE3NOT_YET_RECRUITINGModafinil and Exercise for Post Stroke Fatigue
NCT07231497PHASE3RECRUITINGCognitive Strategies in Early Psychosis 1
NCT07263022PHASE3NOT_YET_RECRUITINGCognitive Strategies in Early Psychosis 2
NCT07582458PHASE2/PHASE3NOT_YET_RECRUITINGModafinil for Debilitating Fatigue in Quiescent Inflammatory Bowel Disease MODIFI-IBD Trial)
NCT00042848PHASE3COMPLETEDModafinil in Treating Fatigue in Patients Receiving Chemotherapy for Cancer
NCT00066170PHASE3COMPLETEDTrial Comparing Effects of Xyrem Taken Orally and Modafinil With Placebo in Treating Daytime Sleepiness in Narcolepsy
NCT00067496PHASE3TERMINATEDModafinil to Treat Fatigue in Post-Polio Syndrome
NCT00107796PHASE3COMPLETEDStudy of PROVIGIL ® (Modafinil) Treatment in Children and Adolescents With Excessive Sleepiness Associated With Narcolepsy
NCT00107809PHASE3COMPLETEDStudy of PROVIGIL ® (Modafinil) Treatment in Children and Adolescents With Excessive Sleepiness Associated With Obstructive Sleep Apnea/Hypopnea Syndrome
NCT00107848PHASE3COMPLETEDPROVIGIL® (Modafinil) Treatment in Children and Adolescents With Excessive Sleepiness Associated With Narcolepsy or Obstructive Sleep Apnea/Hypopnea Syndrome
NCT00214968PHASE3COMPLETEDAssess the Safety and Effectiveness of PROVIGIL Treatment in Children and Adolescents With Excessive Sleepiness
NCT00214981PHASE3COMPLETEDEvaluate the Safety and Efficacy of Modafinil in Children and Adolescents With ADHD
NCT00215176PHASE2/PHASE3COMPLETEDModafinil for Atypical Depression
NCT00228540PHASE3COMPLETEDStudy to Assess Satisfaction With Modafinil Treatment in Children and Adolescents With ADHD
NCT00236080PHASE3COMPLETEDStudy of the Efficacy and Multiple-Dose Plasma Concentration-Time Profiles of Armodafinil and PROVIGIL
NCT00267332PHASE3TERMINATEDModafinil in Opioid Induced Sedation
NCT00343811PHASE3COMPLETEDStudy to Evaluate the Efficacy of Modafinil Treatment in Patients With Attention Deficit Hyperactivity Disorder (ADHD) Who Are Responders to Modafinil Treatment
NCT00418691PHASE3TERMINATEDEffects of Methylphenidate Versus Sustained Release Methylphenidate on Cognitive Functioning
NCT00701532PHASE3COMPLETEDBrain Imaging Study of the Effects of Modafinil in Cocaine Addiction
NCT00917748PHASE3COMPLETEDStudy With Modafinil in Patients Treated With Docetaxel-Based Chemotherapy for Metastatic Breast or Prostate Cancer (MOTIF)

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 4 clinical and 7 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.

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

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)SLC6A3
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)SLC6A3
DACOMITINIBChEMBL + PubChemPhase 4 (approved)SLC6A3
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)SLC6A3
IDELALISIBChEMBL + PubChemPhase 4 (approved)SLC6A3
OLODATEROLChEMBL + PubChemPhase 4 (approved)SLC6A3
PIMAVANSERINChEMBL + PubChemPhase 4 (approved)SLC6A3
REGORAFENIBChEMBL + PubChemPhase 4 (approved)SLC6A3
TAFENOQUINEChEMBL + PubChemPhase 4 (approved)SLC6A3
UMECLIDINIUMChEMBL + PubChemPhase 4 (approved)SLC6A3
ACETOPHENAZINEChEMBLPhase 4 (approved)SLC6A3
AMINEPTINEChEMBLPhase 4 (approved)SLC6A3
AMINOCAPROIC ACIDChEMBLPhase 4 (approved)SLC6A3
AMIODARONEChEMBLPhase 4 (approved)SLC6A3
AMITRIPTYLINEChEMBLPhase 4 (approved)SLC6A3
AMLODIPINEChEMBLPhase 4 (approved)SLC6A3
AMODIAQUINEChEMBLPhase 4 (approved)SLC6A3
AMOXAPINEChEMBLPhase 4 (approved)SLC6A3
AMPHOTERICIN BChEMBLPhase 4 (approved)SLC6A3
ANTAZOLINEChEMBLPhase 4 (approved)SLC6A3
ARFORMOTEROLChEMBLPhase 4 (approved)SLC6A3
ARIPIPRAZOLEChEMBLPhase 4 (approved)SLC6A3
ARMODAFINILChEMBLPhase 4 (approved)SLC6A3
ASENAPINEChEMBLPhase 4 (approved)SLC6A3
ASTEMIZOLEChEMBLPhase 4 (approved)SLC6A3
ATOMOXETINEChEMBLPhase 4 (approved)SLC6A3
AXITINIBChEMBLPhase 4 (approved)SLC6A3
AZELASTINEChEMBLPhase 4 (approved)SLC6A3
BAZEDOXIFENEChEMBLPhase 4 (approved)SLC6A3
BEDAQUILINEChEMBLPhase 4 (approved)SLC6A3
BENDROFLUMETHIAZIDEChEMBLPhase 4 (approved)SLC6A3
BENFLUOREXChEMBLPhase 4 (approved)SLC6A3
BENOXINATEChEMBLPhase 4 (approved)SLC6A3
BENPERIDOLChEMBLPhase 4 (approved)SLC6A3
BENZBROMARONEChEMBLPhase 4 (approved)SLC6A3
BENZIODARONEChEMBLPhase 4 (approved)SLC6A3
BENZPHETAMINEChEMBLPhase 4 (approved)SLC6A3
BENZTROPINEChEMBLPhase 4 (approved)SLC6A3
BENZYDAMINEChEMBLPhase 4 (approved)SLC6A3
BENZYL BENZOATEChEMBLPhase 4 (approved)SLC6A3
BEPRIDILChEMBLPhase 4 (approved)SLC6A3
BEXAROTENEChEMBLPhase 4 (approved)SLC6A3
BISACODYLChEMBLPhase 4 (approved)SLC6A3
BITHIONOLChEMBLPhase 4 (approved)SLC6A3
BOSUTINIBChEMBLPhase 4 (approved)SLC6A3
BREXPIPRAZOLEChEMBLPhase 4 (approved)SLC6A3
BROMHEXINEChEMBLPhase 4 (approved)SLC6A3
BROMODIPHENHYDRAMINEChEMBLPhase 4 (approved)SLC6A3
BROMPERIDOLChEMBLPhase 4 (approved)SLC6A3
BROMPHENIRAMINEChEMBLPhase 4 (approved)SLC6A3
BUPROPIONChEMBLPhase 4 (approved)SLC6A3
BUTOCONAZOLEChEMBLPhase 4 (approved)SLC6A3
CABERGOLINEChEMBLPhase 4 (approved)SLC6A3
CALCITRIOLChEMBLPhase 4 (approved)SLC6A3
CANAGLIFLOZINChEMBLPhase 4 (approved)SLC6A3
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)SLC6A3
CANNABIDIOLChEMBLPhase 4 (approved)SLC6A3
CARBINOXAMINEChEMBLPhase 4 (approved)SLC6A3
CARIPRAZINEChEMBLPhase 4 (approved)SLC6A3
CARVEDILOLChEMBLPhase 4 (approved)SLC6A3

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot