Identification

Name
Modafinil
Accession Number
DB00745  (APRD00534)
Type
Small Molecule
Groups
Approved, Investigational
Description

Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA.

Structure
Thumb
Synonyms
  • 2-((diphenylmethyl)sulfinyl)acetamide
  • Modafinil
  • Modafinilo
  • Modafinilum
  • Moderateafinil
External IDs
CEP 1538 / CEP-1538 / CRC-40476 / CRL 40476 / CRL-40476 / DEP-1538
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AlertecTablet100 mgOralTeva1999-03-24Not applicableCanada
ProvigilTablet200 mg/1OralUnit Dose Services1998-12-24Not applicableUs
ProvigilTablet200 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2011-07-20Not applicableUs
ProvigilTablet200 mg/1OralCephalon, Incorporated1999-02-15Not applicableUs
ProvigilTablet200 mg/1OralPhysicians Total Care, Inc.2004-01-19Not applicableUs
ProvigilTablet100 mg/1OralRebel Distributors2005-06-03Not applicableUs
ProvigilTablet100 mg/1OralCephalon, Incorporated1999-02-15Not applicableUs
ProvigilTablet200 mg/1Oralbryant ranch prepack1998-12-24Not applicableUs
ProvigilTablet100 mg/1OralPhysicians Total Care, Inc.2005-06-03Not applicableUs63459 0101 30 nlmimage10 dd1c6e93
ProvigilTablet100 mg/1Oralbryant ranch prepack1998-12-24Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-modafinilTablet100 mgOralApotex Corporation2008-05-01Not applicableCanada
Auro-modafinilTablet100 mgOralAuro Pharma Inc2014-10-24Not applicableCanada
Bio-modafinilTablet100 mgOralBiomed Pharma2015-10-06Not applicableCanada
Ipg-modafinilTablet100 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mar-modafinilTablet100 mgOralMarcan Pharmaceuticals Inc2015-01-09Not applicableCanada
ModafinilTablet200 mg/1OralWest Ward Pharmaceutical2012-09-26Not applicableUs
ModafinilTablet100 mg/1OralHikma Pharmaceutical2008-04-04Not applicableUs
ModafinilTablet100 mg/1OralActavis Pharma Company2013-04-03Not applicableUs
ModafinilTablet200 mg/1OralDispensing Solutions, Inc.2012-03-29Not applicableUs
ModafinilTablet100 mg/1OralZydus Pharmaceuticals Usa, Inc.2018-01-04Not applicableUs
International/Other Brands
Alertex (Saval) / Aspendos (Medochemie) / Forcilin (LKM) / Mentix (Royal Pharma) / Modasomil (Cephalon) / Modavigil (CSL) / Modiodal (Cephalon) / Provake (Ranbaxy) / Resotyl (Drugtech) / Sparlon (Cephalon) / Stavigile (Libbs) / Vigicer (Beta) / Vigil (Cephalon) / Zalux
Categories
UNII
R3UK8X3U3D
CAS number
68693-11-8
Weight
Average: 273.35
Monoisotopic: 273.082349419
Chemical Formula
C15H15NO2S
InChI Key
YFGHCGITMMYXAQ-UHFFFAOYSA-N
InChI
InChI=1S/C15H15NO2S/c16-14(17)11-19(18)15(12-7-3-1-4-8-12)13-9-5-2-6-10-13/h1-10,15H,11H2,(H2,16,17)
IUPAC Name
2-diphenylmethanesulfinylacetamide
SMILES
NC(=O)CS(=O)C(C1=CC=CC=C1)C1=CC=CC=C1

Pharmacology

Indication

To improve wakefulness in patients with excessive daytime sleepiness (EDS) associated with narcolepsy.

Associated Conditions
Pharmacodynamics

Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. Modafinil is not indicated for complaints of lack of energy or fatigue; but it appears to be very helpful for some patients. Also, it has been used in the treatment of hypersomnia, a disorder in which patients lack the capacity for meaningful sleep and may require ten or more hours per day. Recent studies have have found that modafinil may help recovering cocaine addicts fight their addiction.

Mechanism of action

The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA. Modafinil is thought to have less potential for abuse than other stimulants due to the absence of any significant euphoric or pleasurable effects. It is possible that modafinil acts by a synergistic combination of mechanisms including direct inhibition of dopamine reuptake, indirect inhibition of noradrenalin reuptake in the VLPO and orexin activation. Modafinil has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors.

TargetActionsOrganism
ASodium-dependent dopamine transporter
inhibitor
Human
UAlpha-1B adrenergic receptor
partial agonist
Human
Absorption

Rapid following oral administration.

Volume of distribution
  • 0.9 L/kg
Protein binding

60%

Metabolism

Hepatic

Route of elimination

The major route of elimination is metabolism (~90%), primarily by the liver, with subsequent renal elimination of the metabolites.

Half life

23-215 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Catechol O-methyltransferase---(A;A)AA alleleEffect Directly StudiedPatients with this genotype have reduced improvement in vigor and well-being with modafinil.Details
Catechol O-methyltransferase---(G;G)GG alleleEffect Directly StudiedPatients with this genotype have increased improvement in vigor and well-being with modafinil.Details

Interactions

Drug Interactions
DrugInteractionDrug group
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Modafinil.Approved, Investigational
Acetyl sulfisoxazoleThe metabolism of Modafinil can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AdinazolamThe metabolism of Adinazolam can be decreased when combined with Modafinil.Approved
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Modafinil.Approved, Investigational
AmbrisentanThe metabolism of Ambrisentan can be decreased when combined with Modafinil.Approved, Investigational
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Modafinil.Approved, Withdrawn
AmiodaroneThe metabolism of Modafinil can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Modafinil.Approved
AmoxicillinThe metabolism of Amoxicillin can be decreased when combined with Modafinil.Approved, Vet Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Modafinil.Approved, Investigational
ApalutamideThe serum concentration of Modafinil can be decreased when it is combined with Apalutamide.Approved, Investigational
ApixabanThe metabolism of Apixaban can be decreased when combined with Modafinil.Approved
AprepitantThe serum concentration of Modafinil can be increased when it is combined with Aprepitant.Approved, Investigational
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Modafinil.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Modafinil.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Modafinil.Approved
AsunaprevirThe serum concentration of Asunaprevir can be decreased when it is combined with Modafinil.Approved, Investigational, Withdrawn
AtazanavirThe metabolism of Modafinil can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Modafinil can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Modafinil is combined with Atorvastatin.Approved
AxitinibThe metabolism of Axitinib can be decreased when combined with Modafinil.Approved, Investigational
AzelastineThe metabolism of Azelastine can be decreased when combined with Modafinil.Approved
BenzatropineThe metabolism of Benzatropine can be decreased when combined with Modafinil.Approved
BioallethrinThe metabolism of Bioallethrin can be decreased when combined with Modafinil.Approved, Experimental
BoceprevirThe metabolism of Modafinil can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Modafinil can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Modafinil can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Modafinil.Approved
BrivaracetamThe metabolism of Brivaracetam can be decreased when combined with Modafinil.Approved, Investigational
BromazepamThe metabolism of Bromazepam can be decreased when combined with Modafinil.Approved, Illicit, Investigational
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Modafinil.Approved, Investigational
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Modafinil.Approved
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Modafinil.Approved, Investigational
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Modafinil.Approved
CannabidiolThe metabolism of Cannabidiol can be decreased when combined with Modafinil.Approved, Investigational
CarbamazepineThe metabolism of Modafinil can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Modafinil.Approved
CarisoprodolThe metabolism of Carisoprodol can be decreased when combined with Modafinil.Approved
CeritinibThe serum concentration of Modafinil can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Modafinil.Approved, Withdrawn
ChloramphenicolThe metabolism of Chloramphenicol can be decreased when combined with Modafinil.Approved, Vet Approved
ChlorpropamideThe metabolism of Chlorpropamide can be decreased when combined with Modafinil.Approved, Investigational
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Modafinil.Approved, Investigational
CisaprideThe metabolism of Cisapride can be decreased when combined with Modafinil.Approved, Investigational, Withdrawn
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Modafinil.Approved
ClarithromycinThe metabolism of Modafinil can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Modafinil can be decreased when combined with Clemastine.Approved, Investigational
ClobazamThe metabolism of Clobazam can be decreased when combined with Modafinil.Approved, Illicit
clomethiazoleThe metabolism of clomethiazole can be decreased when combined with Modafinil.Investigational
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Modafinil resulting in a loss in efficacy.Approved
ClotiazepamThe metabolism of Clotiazepam can be decreased when combined with Modafinil.Approved, Illicit
ClotrimazoleThe metabolism of Modafinil can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Modafinil.Approved
CobicistatThe metabolism of Modafinil can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Modafinil.Approved, Investigational
CrizotinibThe metabolism of Modafinil can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Modafinil can be decreased when combined with Curcumin.Approved, Investigational
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Modafinil.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Modafinil.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Modafinil can be decreased when it is combined with Dabrafenib.Approved, Investigational
DapsoneThe metabolism of Dapsone can be decreased when combined with Modafinil.Approved, Investigational
DarunavirThe metabolism of Modafinil can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Modafinil can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Modafinil can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Modafinil can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Desipramine can be decreased when combined with Modafinil.Approved, Investigational
DexlansoprazoleThe metabolism of Dexlansoprazole can be decreased when combined with Modafinil.Approved, Investigational
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Modafinil.Approved
DiazepamThe metabolism of Diazepam can be decreased when combined with Modafinil.Approved, Illicit, Investigational, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Modafinil.Approved, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Modafinil.Approved, Investigational
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Modafinil.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Modafinil.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Modafinil.Experimental
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Modafinil.Approved, Investigational
DiltiazemThe metabolism of Modafinil can be decreased when combined with Diltiazem.Approved, Investigational
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Modafinil.Approved, Investigational
DopamineThe metabolism of Dopamine can be decreased when combined with Modafinil.Approved
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Modafinil.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Modafinil.Approved, Investigational
DoxycyclineThe metabolism of Modafinil can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe metabolism of Dronabinol can be decreased when combined with Modafinil.Approved, Illicit
DronedaroneThe metabolism of Modafinil can be decreased when combined with Dronedarone.Approved
EletriptanThe metabolism of Eletriptan can be decreased when combined with Modafinil.Approved, Investigational
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Modafinil.Approved, Investigational
EnfuvirtideThe metabolism of Enfuvirtide can be decreased when combined with Modafinil.Approved, Investigational
EnzalutamideThe serum concentration of Modafinil can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Modafinil.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Modafinil.Approved
ErythromycinThe metabolism of Modafinil can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Modafinil.Approved, Investigational
EsomeprazoleThe metabolism of Esomeprazole can be decreased when combined with Modafinil.Approved, Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Modafinil.Approved, Investigational, Vet Approved
Estradiol acetateThe metabolism of Estradiol acetate can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
Estradiol benzoateThe metabolism of Estradiol benzoate can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
Estradiol cypionateThe serum concentration of Estradiol cypionate can be decreased when it is combined with Modafinil.Approved, Investigational, Vet Approved
Estradiol dienanthateThe metabolism of Estradiol dienanthate can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
Estradiol valerateThe serum concentration of Estradiol valerate can be decreased when it is combined with Modafinil.Approved, Investigational, Vet Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Modafinil.Approved
EtizolamThe metabolism of Etizolam can be decreased when combined with Modafinil.Approved
EtravirineThe metabolism of Etravirine can be decreased when combined with Modafinil.Approved
FamotidineThe metabolism of Famotidine can be decreased when combined with Modafinil.Approved
FluconazoleThe metabolism of Modafinil can be decreased when combined with Fluconazole.Approved, Investigational
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Modafinil.Approved, Illicit
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Modafinil.Approved, Vet Approved
FlutamideThe metabolism of Flutamide can be decreased when combined with Modafinil.Approved, Investigational
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Modafinil.Approved
FluvoxamineThe metabolism of Modafinil can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolThe metabolism of Formoterol can be decreased when combined with Modafinil.Approved, Investigational
FosamprenavirThe metabolism of Modafinil can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Modafinil can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Modafinil can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Modafinil can be increased when it is combined with Fusidic Acid.Approved, Investigational
GliclazideThe metabolism of Gliclazide can be decreased when combined with Modafinil.Approved
GlucosamineThe metabolism of Glucosamine can be decreased when combined with Modafinil.Approved, Investigational
GlyburideThe metabolism of Glyburide can be decreased when combined with Modafinil.Approved
GuanfacineThe metabolism of Guanfacine can be decreased when combined with Modafinil.Approved, Investigational
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Modafinil.Approved
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Modafinil.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Modafinil.Approved
IbuprofenThe metabolism of Ibuprofen can be decreased when combined with Modafinil.Approved
IdelalisibThe metabolism of Modafinil can be decreased when combined with Idelalisib.Approved
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Modafinil.Approved
ImatinibThe metabolism of Modafinil can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Imipramine can be decreased when combined with Modafinil.Approved
IndinavirThe metabolism of Modafinil can be decreased when combined with Indinavir.Approved
IndomethacinThe metabolism of Indomethacin can be decreased when combined with Modafinil.Approved, Investigational
IsavuconazoleThe serum concentration of Modafinil can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Modafinil can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Modafinil can be decreased when combined with Isradipine.Approved, Investigational
ItraconazoleThe metabolism of Modafinil can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Modafinil can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Modafinil.Approved, Investigational
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Modafinil.Approved, Investigational
KetoconazoleThe metabolism of Modafinil can be decreased when combined with Ketoconazole.Approved, Investigational
LansoprazoleThe metabolism of Lansoprazole can be decreased when combined with Modafinil.Approved, Investigational
LapatinibThe metabolism of Lapatinib can be decreased when combined with Modafinil.Approved, Investigational
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Modafinil.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Modafinil.Approved, Investigational
LofexidineThe metabolism of Lofexidine can be decreased when combined with Modafinil.Approved, Investigational
LopinavirThe metabolism of Modafinil can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Modafinil.Approved
LorpiprazoleThe serum concentration of Modafinil can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Modafinil.Approved, Investigational
LuliconazoleThe serum concentration of Modafinil can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Modafinil can be increased when combined with Lumacaftor.Approved
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Modafinil.Approved, Investigational
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Modafinil.Illicit, Investigational, Withdrawn
MacitentanThe metabolism of Macitentan can be decreased when combined with Modafinil.Approved
Medical CannabisThe metabolism of Medical Cannabis can be decreased when combined with Modafinil.Experimental, Investigational
MelatoninThe metabolism of Melatonin can be decreased when combined with Modafinil.Approved, Nutraceutical, Vet Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Modafinil.Investigational, Withdrawn
MeprobamateThe metabolism of Meprobamate can be decreased when combined with Modafinil.Approved, Illicit
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Modafinil.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Modafinil.Experimental
MethadoneThe metabolism of Methadone can be decreased when combined with Modafinil.Approved
MethsuximideThe metabolism of Methsuximide can be decreased when combined with Modafinil.Approved
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Modafinil.Approved
MethylphenobarbitalThe metabolism of Methylphenobarbital can be decreased when combined with Modafinil.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Modafinil.Approved
MetoprololThe metabolism of Metoprolol can be decreased when combined with Modafinil.Approved, Investigational
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Modafinil.Experimental
MifepristoneThe serum concentration of Modafinil can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Modafinil can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Modafinil.Approved, Investigational
NabiximolsThe metabolism of Nabiximols can be decreased when combined with Modafinil.Approved, Investigational
NefazodoneThe metabolism of Modafinil can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Modafinil can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Modafinil can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Modafinil can be increased when combined with Nevirapine.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Modafinil.Approved, Investigational
NicotineThe metabolism of Nicotine can be decreased when combined with Modafinil.Approved
NilotinibThe metabolism of Modafinil can be decreased when combined with Nilotinib.Approved, Investigational
NilutamideThe metabolism of Nilutamide can be decreased when combined with Modafinil.Approved, Investigational
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Modafinil.Approved
OlaparibThe metabolism of Modafinil can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Omeprazole can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Modafinil can be increased when it is combined with Osimertinib.Approved
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Modafinil.Approved, Investigational
OxiconazoleThe metabolism of Oxiconazole can be decreased when combined with Modafinil.Approved
PalbociclibThe serum concentration of Modafinil can be increased when it is combined with Palbociclib.Approved, Investigational
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Modafinil.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Modafinil.Approved, Investigational
PentobarbitalThe metabolism of Modafinil can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Modafinil.Approved, Investigational, Vet Approved, Withdrawn
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Modafinil.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Modafinil.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Modafinil.Withdrawn
PhenobarbitalThe metabolism of Modafinil can be increased when combined with Phenobarbital.Approved, Investigational
PhenytoinThe metabolism of Modafinil can be increased when combined with Phenytoin.Approved, Vet Approved
PiperaquineThe metabolism of Piperaquine can be decreased when combined with Modafinil.Approved, Investigational
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Modafinil.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Modafinil.Approved
PitolisantThe serum concentration of Modafinil can be decreased when it is combined with Pitolisant.Approved, Investigational
PodofiloxThe metabolism of Podofilox can be decreased when combined with Modafinil.Approved
PosaconazoleThe metabolism of Modafinil can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Modafinil.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Modafinil.Approved
PraziquantelThe metabolism of Praziquantel can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Modafinil can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Modafinil.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Modafinil.Approved
PromazineThe metabolism of Promazine can be decreased when combined with Modafinil.Approved, Vet Approved
PropofolThe metabolism of Propofol can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Modafinil.Approved, Investigational
QuazepamThe metabolism of Quazepam can be decreased when combined with Modafinil.Approved, Illicit
QuetiapineThe metabolism of Quetiapine can be decreased when combined with Modafinil.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Modafinil.Approved
RabeprazoleThe metabolism of Rabeprazole can be decreased when combined with Modafinil.Approved, Investigational
RamelteonThe metabolism of Ramelteon can be decreased when combined with Modafinil.Approved, Investigational
RanitidineThe metabolism of Ranitidine can be decreased when combined with Modafinil.Approved
RanolazineThe metabolism of Modafinil can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Modafinil can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Modafinil can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Modafinil can be increased when combined with Rifapentine.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Modafinil.Approved
RomidepsinThe metabolism of Romidepsin can be decreased when combined with Modafinil.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Modafinil.Approved
RucaparibThe metabolism of Modafinil can be decreased when combined with Rucaparib.Approved, Investigational
RupatadineThe metabolism of Rupatadine can be decreased when combined with Modafinil.Approved
SaquinavirThe metabolism of Modafinil can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Modafinil can be decreased when used in combination with Sarilumab.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Modafinil.Approved
SelegilineThe metabolism of Selegiline can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Modafinil.Approved
SertralineThe metabolism of Sertraline can be decreased when combined with Modafinil.Approved
SildenafilThe metabolism of Modafinil can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Modafinil can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Modafinil can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Modafinil.Approved
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Modafinil.Approved
St. John's WortThe serum concentration of Modafinil can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Modafinil can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Modafinil can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Modafinil.Approved
TapentadolThe metabolism of Tapentadol can be decreased when combined with Modafinil.Approved
TelaprevirThe metabolism of Modafinil can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Modafinil can be decreased when combined with Telithromycin.Approved
TemazepamThe metabolism of Temazepam can be decreased when combined with Modafinil.Approved, Investigational
TeniposideThe metabolism of Teniposide can be decreased when combined with Modafinil.Approved
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Modafinil.Approved, Investigational, Vet Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Modafinil.Experimental
TestosteroneThe metabolism of Testosterone can be decreased when combined with Modafinil.Approved, Investigational
Testosterone cypionateThe metabolism of Testosterone cypionate can be decreased when combined with Modafinil.Approved
Testosterone enanthateThe metabolism of Testosterone enanthate can be decreased when combined with Modafinil.Approved
Testosterone undecanoateThe metabolism of Testosterone undecanoate can be decreased when combined with Modafinil.Approved, Investigational
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Modafinil.Approved, Investigational, Withdrawn
ThioridazineThe metabolism of Thioridazine can be decreased when combined with Modafinil.Approved, Withdrawn
TiclopidineThe metabolism of Modafinil can be decreased when combined with Ticlopidine.Approved
TimololThe metabolism of Timolol can be decreased when combined with Modafinil.Approved
TipranavirThe metabolism of Tipranavir can be decreased when combined with Modafinil.Approved, Investigational
TocilizumabThe serum concentration of Modafinil can be decreased when it is combined with Tocilizumab.Approved
TofacitinibThe metabolism of Tofacitinib can be decreased when combined with Modafinil.Approved, Investigational
TolbutamideThe metabolism of Tolbutamide can be decreased when combined with Modafinil.Approved, Investigational
TolterodineThe metabolism of Tolterodine can be decreased when combined with Modafinil.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Modafinil.Approved
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Modafinil.Approved, Investigational
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Modafinil.Approved
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Modafinil.Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Modafinil.Investigational, Withdrawn
Valproic AcidThe metabolism of Valproic Acid can be decreased when combined with Modafinil.Approved, Investigational
VemurafenibThe serum concentration of Modafinil can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Modafinil can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Modafinil can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Modafinil can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Modafinil.Approved, Investigational
WarfarinThe metabolism of Warfarin can be decreased when combined with Modafinil.Approved
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Modafinil.Approved
ZiprasidoneThe metabolism of Modafinil can be decreased when combined with Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Modafinil.Approved
Food Interactions
  • Take without regard to meals.

References

Synthesis Reference
US4177290
General References
  1. Lindsay SE, Gudelsky GA, Heaton PC: Use of modafinil for the treatment of attention deficit/hyperactivity disorder. Ann Pharmacother. 2006 Oct;40(10):1829-33. Epub 2006 Sep 5. [PubMed:16954326]
  2. Ishizuka T, Sakamoto Y, Sakurai T, Yamatodani A: Modafinil increases histamine release in the anterior hypothalamus of rats. Neurosci Lett. 2003 Mar 20;339(2):143-6. [PubMed:12614915]
External Links
Human Metabolome Database
HMDB0014883
KEGG Drug
D01832
PubChem Compound
4236
PubChem Substance
46504648
ChemSpider
4088
BindingDB
50156055
ChEBI
77585
ChEMBL
CHEMBL1373
PharmGKB
PA450530
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Modafinil
ATC Codes
N06BA07 — Modafinil
AHFS Codes
  • 28:20.80 — Wakefulness-promoting Agents
FDA label
Download (98.9 KB)
MSDS
Download (57 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingTreatmentPostural Tachycardia Syndrome1
0CompletedBasic ScienceHealthy Volunteers / Moods Disorders / Substance-Related Disorders1
0CompletedSupportive CareFluid Inteligence / Healthy Young Subjects / Modafinil / Resting State Networks1
0CompletedTreatmentCannabis / Marijuana Abuse1
0Enrolling by InvitationTreatmentParkinson's Disease (PD)1
1Active Not RecruitingBasic ScienceCognitive Symptom / Schizophrenic Disorders1
1Active Not RecruitingTreatmentEwing's Sarcoma (ES) / Liver Cancer / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedNot AvailableAutonomic Failure / Idiopathic orthostatic hypotension1
1CompletedNot AvailableCocaine Abuse / Dependence, Cocaine / Substance Abuse1
1CompletedNot AvailableCognitive Impairments1
1CompletedNot AvailableHealthy Volunteers3
1CompletedBasic ScienceHealthy Volunteers1
1CompletedHealth Services ResearchCognitively Healthy Subjects Influenced by Psychoactive Drugs1
1CompletedOtherSchizoaffective Disorders / Schizophrenic Disorders1
1CompletedTreatmentMalignant Melanoma / Melanoma / Melanoma Recurrent1
1CompletedTreatmentPrimary Biliary Cirrhosis (PBC) / Tiredness1
1CompletedTreatmentSleep Apnea Syndrome1
1CompletedTreatmentSleep Deprivation1
1CompletedTreatmentTiredness1
1CompletedTreatmentTobacco Use Disorders1
1RecruitingOtherHealthy Volunteers1
1RecruitingTreatmentDependence, Cocaine1
1TerminatedTreatmentTinnitus1
1Unknown StatusTreatmentAmphetamine-Related Disorders1
1Unknown StatusTreatmentCocaine-Related Disorders / Drug Administration Schedule / Intravenous Infusions1
1, 2Active Not RecruitingTreatmentChronic Orthostatic Intolerance / Tachycardia1
1, 2CompletedTreatmentSchizophrenia and Schizophrenia Spectrum Psychosis1
1, 2WithdrawnSupportive CareLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingTreatmentCancer of the Ovary1
2Active Not RecruitingTreatmentCancer of the Ovary / Neoplasms, Ovarian1
2Active Not RecruitingTreatmentEwing's Sarcoma (ES)1
2CompletedDiagnosticCocaine-Related Disorders1
2CompletedOtherCocaine Related Disorders1
2CompletedSupportive CareBrain and Central Nervous System Tumors / Cognitive/Functional Effects / Neurotoxicity / Psychosocial Effects of Cancer and Its Treatment / Tiredness1
2CompletedTreatmentAlcohol-Related Disorders / Alcoholism / Cocaine-Related Disorders1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
2CompletedTreatmentCancer treatment / Cancers / Tiredness1
2CompletedTreatmentCocaine-Related Disorders2
2CompletedTreatmentDependence, Cocaine5
2CompletedTreatmentMethamphetamine Addiction1
2CompletedTreatmentMethamphetamine Dependence4
2CompletedTreatmentNarcolepsy1
2CompletedTreatmentNeglect / Spatial Neglect / Swallowing Disorders1
2Enrolling by InvitationTreatmentCancer of the Ovary / Cancer, Breast / Cervical Cancers / Endometrial Cancers / Fallopian Tube Cancer / Primary Peritoneal Carcinoma / Triple Negative Breast Cancer (TNBC) / Uterine Cancers1
2RecruitingTreatmentAdvanced Gynecological Cancers / Cancer of the Ovary / Cervical Cancers / Uterine Cancers1
2RecruitingTreatmentAlcohol Use Disorder (AUD)1
2RecruitingTreatmentCocaine-Related Disorders1
2RecruitingTreatmentMajor Depressive Disorder (MDD)1
2RecruitingTreatmentNarcolepsy1
2TerminatedSupportive CareCentral Nervous System Tumor, Pediatric / Specific Disorders of Sleep / Tiredness1
2TerminatedTreatmentExcessive Daytime Sleepiness / Hypopnoea Syndrome / Sleep Apnea, Obstructive1
2TerminatedTreatmentMethamphetamine Dependence1
2TerminatedTreatmentTiredness1
2Unknown StatusTreatmentAmphetamine Dependence1
2Unknown StatusTreatmentAmphetamine Dependence / Substance Dependence1
2Unknown StatusTreatmentCocaine Abuse / Cocaine-Related Disorders1
2Unknown StatusTreatmentCocaine Abuse / Opiate Dependence1
2Unknown StatusTreatmentDependence, Cocaine1
2WithdrawnBasic ScienceDepression1
2WithdrawnTreatmentAdvanced Non-Small Cell Lung Cancer / Metastatic Non-Small Cell Lung Cancer / Neoplasms, Lung1
2WithdrawnTreatmentParkinson's Disease (PD)1
2WithdrawnTreatmentSchizophrenic Disorders1
2, 3CompletedTreatmentAtypical Depression1
2, 3Unknown StatusTreatmentPosttraumatic Stress Disorders1
3CompletedSupportive CareCancer Related Fatigue / Quality of Life1
3CompletedSupportive CareTiredness / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedTreatmentAlzheimer's Disease (AD) / Apathy1
3CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)2
3CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Attention Deficit/Hyperactivity Disorder1
3CompletedTreatmentCancer, Breast / Prostatic Neoplasms1
3CompletedTreatmentCataplexy / Excessive Daytime Sleepiness / Narcolepsy1
3CompletedTreatmentCataplexy / Excessive Daytime Sleepiness / Narcolepsy / Sleep disorders and disturbances1
3CompletedTreatmentChronic Shift Work Sleep Disorder1
3CompletedTreatmentDependence, Cocaine1
3CompletedTreatmentNarcolepsy3
3CompletedTreatmentNarcolepsy / Sleep Apnea, Obstructive1
3CompletedTreatmentSleep Apnea, Obstructive1
3CompletedTreatmentTreatment of Excessive Daytime Sleepiness in Narcolepsy1
3Not Yet RecruitingTreatmentEwing Family of Tumors / Ewing's Sarcoma (ES) / Ewing's sarcoma metastatic / Ewing's Tumor Metastatic1
3RecruitingTreatmentFatigue in Multiple Sclerosis1
3TerminatedTreatmentCancers / Pain1
3TerminatedTreatmentNeoplasms, Brain1
3TerminatedTreatmentPost Stroke Fatigue / Strokes1
3TerminatedTreatmentPostpoliomyelitis Syndrome1
3Unknown StatusSupportive CareCancers / Excessive Sleepiness / Pain Palliation1
3WithdrawnTreatmentDelirium / Respiratory Failure1
4CompletedBasic ScienceOsteoarthritis (OA)1
4CompletedTreatmentAttention / Executive Function / Memory, Short-Term1
4CompletedTreatmentBipolar Disorder (BD)1
4CompletedTreatmentDelayed Emergence From Anesthesia / Obstructive Sleep Apnea (OSA)1
4CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Tiredness1
4CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
4CompletedTreatmentMajor Depressive Disorder (MDD) / Mental Health1
4CompletedTreatmentMethamphetamine Dependence1
4CompletedTreatmentObstructive Sleep Apnea Syndrome (OSAS)1
4CompletedTreatmentPrimary Insomnia1
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
4CompletedTreatmentSchizophrenic Disorders2
4CompletedTreatmentTiredness1
4RecruitingTreatmentTiredness1
4TerminatedTreatmentAlzheimer's Disease (AD) / Sleep Initiation and Maintenance Disorders / Sleeplessness1
4TerminatedTreatmentHealthy Volunteers1
4Unknown StatusTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
Not AvailableCompletedNot AvailableDependence, Cocaine / Substance-induced Cognitive Disorder / Substance-induced Sleep Disorder1
Not AvailableCompletedBasic ScienceCognitive Performance / Creativity / Healthy Volunteers / Motivation / Reward / Subjective Pleasure1
Not AvailableCompletedBasic ScienceHealthy Volunteers2
Not AvailableCompletedDiagnosticHypersomnia / Narcolepsy1
Not AvailableCompletedPreventionWeight gain therapy1
Not AvailableCompletedSupportive CareBrain and Central Nervous System Tumors / Cognitive/Functional Effects / Tiredness1
Not AvailableCompletedTreatmentCataplexy / Excessive Sleepiness / Hypersomnolence / Narcolepsy / Sleep disorders and disturbances1
Not AvailableCompletedTreatmentDependence, Cocaine1
Not AvailableCompletedTreatmentDisseminated Sclerosis1
Not AvailableCompletedTreatmentImpaired Glucose Metabolism / Sleep Restriction1
Not AvailableCompletedTreatmentSchizophrenic Disorders1
Not AvailableRecruitingNot AvailableAlcohol Dependence / Cocaine Abuse / Dependence, Cocaine / Opiate Dependence / Substance Abuse1
Not AvailableRecruitingNot AvailableNarcolepsy / Obstructive Sleep Apnea (OSA) / Shift-work related sleep disturbance1
Not AvailableRecruitingBasic ScienceHealthy Volunteers1
Not AvailableSuspendedTreatmentCocaine-Related Disorders / Opioid-Related Disorders1
Not AvailableTerminatedTreatmentSystemic Lupus Erythematosus (SLE)1
Not AvailableUnknown StatusSupportive CareCognitive/Functional Effects / Depression / Tiredness / Unspecified Adult Solid Tumor, Protocol Specific1
Not AvailableUnknown StatusTreatmentAll Multiple Sclerosis Patients1
Not AvailableUnknown StatusTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
Not AvailableUnknown StatusTreatmentSevere Traumatic Brain Injury / Traumatic Brain Injury (TBI)1
Not AvailableWithdrawnTreatmentParkinson's Disease (PD)1

Pharmacoeconomics

Manufacturers
  • Cephalon inc
  • Cephalon, Inc.
Packagers
  • Bryant Ranch Prepack
  • Caremark LLC
  • Cephalon Inc.
  • Cima Laboratories Inc.
  • DispenseXpress Inc.
  • Diversified Healthcare Services Inc.
  • DSM Corp.
  • Innoviant Pharmacy Inc.
  • Kaiser Foundation Hospital
  • Patheon Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Prepak Systems Inc.
  • Rebel Distributors Corp.
  • Resource Optimization and Innovation LLC
  • Shire Inc.
  • Southwood Pharmaceuticals
  • Stat Rx Usa
  • Watson Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral100 mg
TabletOral100 mg/1
TabletOral200 mg/1
Prices
Unit descriptionCostUnit
Provigil 200 mg tablet15.33USD tablet
Provigil 100 mg tablet13.58USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
USRE37516No1994-10-062014-10-06Us
CA2165824No2005-08-022014-06-14Canada
CA2201967No2002-12-102015-10-04Canada
US7297346Yes2004-05-292024-05-29Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)164-166 °CNot Available
water solubilitySlightly solubleNot Available
logP0.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.622 mg/mLALOGPS
logP1.75ALOGPS
logP1.53ChemAxon
logS-2.6ALOGPS
pKa (Strongest Acidic)8.84ChemAxon
pKa (Strongest Basic)-4.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area60.16 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity77.39 m3·mol-1ChemAxon
Polarizability28.71 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9947
Caco-2 permeable+0.5066
P-glycoprotein substrateNon-substrate0.8912
P-glycoprotein inhibitor INon-inhibitor0.8842
P-glycoprotein inhibitor IINon-inhibitor0.9962
Renal organic cation transporterNon-inhibitor0.8153
CYP450 2C9 substrateNon-substrate0.793
CYP450 2D6 substrateNon-substrate0.8659
CYP450 3A4 substrateNon-substrate0.5971
CYP450 1A2 substrateNon-inhibitor0.6653
CYP450 2C9 inhibitorNon-inhibitor0.6045
CYP450 2D6 inhibitorNon-inhibitor0.9117
CYP450 2C19 inhibitorNon-inhibitor0.6952
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6395
Ames testNon AMES toxic0.6562
CarcinogenicityNon-carcinogens0.6665
BiodegradationReady biodegradable0.6304
Rat acute toxicity2.0926 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9799
hERG inhibition (predictor II)Non-inhibitor0.9279
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Benzyl alkyl sulfoxides / Sulfoxides / Primary carboxylic acid amides / Sulfinyl compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Diphenylmethane / Benzyl alkyl sulfoxide / Benzyl sulfoxide / Carboxamide group / Primary carboxylic acid amide / Sulfoxide / Sulfinyl compound / Carboxylic acid derivative / Hydrocarbon derivative / Carbonyl group
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
monocarboxylic acid amide, sulfoxide (CHEBI:77585)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Monoamine transmembrane transporter activity
Specific Function
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A3
Uniprot ID
Q01959
Uniprot Name
Sodium-dependent dopamine transporter
Molecular Weight
68494.255 Da
References
  1. Zhou J, He R, Johnson KM, Ye Y, Kozikowski AP: Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization. J Med Chem. 2004 Nov 18;47(24):5821-4. [PubMed:15537337]
  2. Madras BK, Xie Z, Lin Z, Jassen A, Panas H, Lynch L, Johnson R, Livni E, Spencer TJ, Bonab AA, Miller GM, Fischman AJ: Modafinil occupies dopamine and norepinephrine transporters in vivo and modulates the transporters and trace amine activity in vitro. J Pharmacol Exp Ther. 2006 Nov;319(2):561-9. Epub 2006 Aug 2. [PubMed:16885432]
  3. Swanson JM: Role of executive function in ADHD. J Clin Psychiatry. 2003;64 Suppl 14:35-9. [PubMed:14658934]
  4. Dopheide MM, Morgan RE, Rodvelt KR, Schachtman TR, Miller DK: Modafinil evokes striatal [(3)H]dopamine release and alters the subjective properties of stimulants. Eur J Pharmacol. 2007 Jul 30;568(1-3):112-23. Epub 2007 Apr 5. [PubMed:17477916]
  5. Wisor JP, Nishino S, Sora I, Uhl GH, Mignot E, Edgar DM: Dopaminergic role in stimulant-induced wakefulness. J Neurosci. 2001 Mar 1;21(5):1787-94. [PubMed:11222668]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Chen CR, Qu WM, Qiu MH, Xu XH, Yao MH, Urade Y, Huang ZL: Modafinil exerts a dose-dependent antiepileptic effect mediated by adrenergic alpha1 and histaminergic H1 receptors in mice. Neuropharmacology. 2007 Sep;53(4):534-41. Epub 2007 Jun 30. [PubMed:17681557]

Enzymes

Details
1. Cytochrome P450 2C19
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Robertson P Jr, Hellriegel ET: Clinical pharmacokinetic profile of modafinil. Clin Pharmacokinet. 2003;42(2):123-37. [PubMed:12537513]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on July 19, 2018 17:49