Modafinil

Identification

Summary

Modafinil is a stimulant used to improve wakefulness in patients with sleep apnea, narcolepsy, or shift work disorder.

Brand Names
Provigil
Generic Name
Modafinil
DrugBank Accession Number
DB00745
Background

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.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 273.35
Monoisotopic: 273.082349419
Chemical Formula
C15H15NO2S
Synonyms
  • 2-((diphenylmethyl)sulfinyl)acetamide
  • Modafinil
  • Modafinilo
  • Modafinilum
External IDs
  • CEP 1538
  • CEP-1538
  • CRC-40476
  • CRL 40476
  • CRL-40476
  • DEP-1538

Pharmacology

Indication

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

Pharmacology
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Associated Conditions
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Contraindications
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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
Humans
UAlpha-1B adrenergic receptor
partial agonist
Humans
Absorption

Rapid following oral administration.

Volume of distribution
  • 0.9 L/kg
Protein binding

60%

Metabolism

Hepatic

Hover over products below to view reaction partners

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

Adverse Effects
Adverseeffects
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Toxicity

Not Available

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
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Modafinil can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Modafinil can be increased when combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Modafinil.
AbirateroneThe metabolism of Modafinil can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Modafinil.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Modafinil.
AcetohexamideThe metabolism of Acetohexamide can be decreased when combined with Modafinil.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be decreased when combined with Modafinil.
AdalimumabThe metabolism of Modafinil can be increased when combined with Adalimumab.
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Modafinil.
Interactions
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Food Interactions
  • Take with or without food. The absorption is unaffected by food.

Products

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Product Images
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
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AlertecTablet100 mgOralTEVA Canada Limited1999-03-24Not applicableCanada flag
Modafinil TabletsTablet100 mgOralStrides Pharma Canada IncNot applicableNot applicableCanada flag
ProvigilTablet200 mg/1OralCaremark L.L.C.2007-12-172013-06-30US flag
ProvigilTablet200 mg/1OralCephalon, Inc.1999-02-15Not applicableUS flag
ProvigilTablet100 mg/1OralRebel Distributors2005-06-03Not applicableUS flag21695 023420210327 31328 2sxv8h
ProvigilTablet200 mg/1OralUnit Dose Services1999-02-152017-12-31US flag50436 020120180907 15195 18b2w5r
ProvigilTablet100 mg/1OralPhysicians Total Care, Inc.2005-06-03Not applicableUS flag63459 0101 30 nlmimage10 dd1c6e93
ProvigilTablet100 mg/1OralCephalon, Inc.1999-02-15Not applicableUS flag
ProvigilTablet200 mg/1OralLake Erie Medical Surgical & Supply DBA Quality Care Products LLC2011-07-202019-10-11US flag
ProvigilTablet200 mg/1OralRebel Distributors2004-01-19Not applicableUS flag63459 0201 30 nlmimage10 36429b14
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-modafinilTablet100 mgOralApotex Corporation2008-05-01Not applicableCanada flag
Auro-modafinilTablet100 mgOralAuro Pharma Inc2014-10-24Not applicableCanada flag
Bio-modafinilTablet100 mgOralBiomed Pharma2015-10-06Not applicableCanada flag
Ipg-modafinilTablet100 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada flag
Jamp ModafinilTablet100 mgOralJamp Pharma Corporation2021-03-11Not applicableCanada flag
Mar-modafinilTablet100 mgOralMarcan Pharmaceuticals Inc2015-01-09Not applicableCanada flag
ModafinilTablet100 mg/1OralMylan Pharmaceuticals Inc.2012-08-10Not applicableUS flag
ModafinilTablet200 mg/1OralProficient Rx LP2012-09-27Not applicableUS flag
ModafinilTablet200 mg/1OralAmerican Health Packaging2014-05-30Not applicableUS flag
ModafinilTablet100 mg/1OralViona Pharmaceuticals Inc2019-02-15Not applicableUS flag

Categories

ATC Codes
N06BA07 — Modafinil
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Aromatic homomonocyclic compound / Benzyl alkyl sulfoxide / Benzyl sulfoxide / Carbonyl group / Carboxamide group / Carboxylic acid derivative / Diphenylmethane / Hydrocarbon derivative / Organic nitrogen compound / Organic oxide
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
monocarboxylic acid amide, sulfoxide (CHEBI:77585)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
R3UK8X3U3D
CAS number
68693-11-8
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

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. [Article]
  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. [Article]
Human Metabolome Database
HMDB0014883
KEGG Drug
D01832
PubChem Compound
4236
PubChem Substance
46504648
ChemSpider
4088
BindingDB
50156055
RxNav
30125
ChEBI
77585
ChEMBL
CHEMBL1373
PharmGKB
PA450530
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Modafinil
FDA label
Download (98.9 KB)
MSDS
Download (57 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentMultiple Sclerosis1
4CompletedBasic ScienceOsteoarthritis (OA)1
4CompletedTreatmentAttention / Executive Function (Cognition) / Memory, Short-Term1
4CompletedTreatmentBipolar Disorder (BD)1
4CompletedTreatmentFatigue1
4CompletedTreatmentFatigue / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentMajor Depressive Disorder (MDD) / Mental Health1
4CompletedTreatmentMethamphetamine Dependence1
4CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
4CompletedTreatmentObstructive Sleep Apnea (OSA)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
TabletOral200 mg
TabletOral
TabletOral100 mg
TabletOral100 mg/1
TabletOral200 mg/1
Capsule, liquid filledOral200 mg
Capsule, liquid filledOral100 mg
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)Region
USRE37516No2002-01-152014-10-06US flag
CA2165824No2005-08-022014-06-14Canada flag
CA2201967No2002-12-102015-10-04Canada flag
US7297346Yes2007-11-202024-05-29US flag

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

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
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. [Article]
  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. [Article]
  3. Swanson JM: Role of executive function in ADHD. J Clin Psychiatry. 2003;64 Suppl 14:35-9. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
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. [Article]

Enzymes

Details
1. Cytochrome P450 2C19
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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. Robertson P, DeCory HH, Madan A, Parkinson A: In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil. Drug Metab Dispos. 2000 Jun;28(6):664-71. [Article]
  2. Robertson P Jr, Hellriegel ET: Clinical pharmacokinetic profile of modafinil. Clin Pharmacokinet. 2003;42(2):123-37. [Article]
  3. Modafinil FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. [Article]
  2. Robertson P, DeCory HH, Madan A, Parkinson A: In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil. Drug Metab Dispos. 2000 Jun;28(6):664-71. [Article]
  3. Robertson P Jr, Hellriegel ET, Arora S, Nelson M: Effect of modafinil on the pharmacokinetics of ethinyl estradiol and triazolam in healthy volunteers. Clin Pharmacol Ther. 2002 Jan;71(1):46-56. [Article]
  4. FDA interactions table [Link]
  5. Flockhart Table of Drug Interactions [Link]
  6. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. Robertson P Jr, Hellriegel ET, Arora S, Nelson M: Effect of modafinil on the pharmacokinetics of ethinyl estradiol and triazolam in healthy volunteers. Clin Pharmacol Ther. 2002 Jan;71(1):46-56. [Article]
  2. Robertson P, DeCory HH, Madan A, Parkinson A: In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil. Drug Metab Dispos. 2000 Jun;28(6):664-71. [Article]
  3. FDA interactions table [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
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. Robertson P Jr, Hellriegel ET: Clinical pharmacokinetic profile of modafinil. Clin Pharmacokinet. 2003;42(2):123-37. [Article]
  2. Alan H.B. Wu (2006). Tietz Clinical Guide to Laboratory Tests. Elsevier.
  3. Pharmacogenomics Table [File]
Kind
Protein
Organism
Humans
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. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
  2. Robertson P, DeCory HH, Madan A, Parkinson A: In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil. Drug Metab Dispos. 2000 Jun;28(6):664-71. [Article]
  3. Robertson P Jr, Hellriegel ET: Clinical pharmacokinetic profile of modafinil. Clin Pharmacokinet. 2003;42(2):123-37. [Article]
Kind
Protein
Organism
Humans
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. Robertson P, DeCory HH, Madan A, Parkinson A: In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil. Drug Metab Dispos. 2000 Jun;28(6):664-71. [Article]
  2. Robertson P Jr, Hellriegel ET, Arora S, Nelson M: Effect of modafinil at steady state on the single-dose pharmacokinetic profile of warfarin in healthy volunteers. J Clin Pharmacol. 2002 Feb;42(2):205-14. [Article]
  3. Modafinil FDA [File]
  4. Modafinil EMA label [File]
  5. Modafinil FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
Curator comments
There is some evidence that modafinil may act as a weak CYP2D6 inducer, however this is not expected to be clinically relevant.
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Rowland A, van Dyk M, Warncken D, Mangoni AA, Sorich MJ, Rowland A: Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol. Br J Clin Pharmacol. 2018 Mar;84(3):501-509. doi: 10.1111/bcp.13478. Epub 2018 Jan 10. [Article]

Drug created on June 13, 2005 13:24 / Updated on October 20, 2021 19:48