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
- 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.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Symptomatic treatment of Adhd ••• ••••• Management of Fatigue ••• ••••• Management of Fatigue ••• ••••• Adjunct therapy in treatment of Major depressive disorder ••• ••••• Symptomatic treatment of Narcolepsy •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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.
Target Actions Organism ASodium-dependent dopamine transporter inhibitorHumans UAlpha-1B adrenergic receptor partial agonistHumans - 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Catechol O-methyltransferase --- (A;A) AA allele Effect Directly Studied Patients with this genotype have reduced improvement in vigor and well-being with modafinil. Details Catechol O-methyltransferase --- (G;G) GG allele Effect Directly Studied Patients with this genotype have increased improvement in vigor and well-being with modafinil. Details
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Modafinil can be increased when it is combined with Abametapir. Abatacept The metabolism of Modafinil can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Modafinil. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Modafinil. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Modafinil. - Food Interactions
- Take with or without food. The absorption is unaffected by food.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- 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
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-modafinil Tablet 100 mg Oral Apotex Corporation 2008-05-01 Not applicable Canada Auro-modafinil Tablet 100 mg Oral Auro Pharma Inc 2014-10-24 Not applicable Canada Bio-modafinil Tablet 100 mg Oral Biomed Pharma 2015-10-06 2022-07-19 Canada Ipg-modafinil Tablet 100 mg Oral Marcan Pharmaceuticals Inc Not applicable Not applicable Canada Jamp Modafinil Tablet 100 mg Oral Jamp Pharma Corporation 2021-03-11 Not applicable Canada
Categories
- ATC Codes
- N06BA07 — Modafinil
- Drug Categories
- Benzene Derivatives
- Benzhydryl Compounds
- Central Nervous System Agents
- Central Nervous System Stimulants
- Central Nervous System Stimulation
- Centrally Acting Sympathomimetics
- Cytochrome P-450 CYP1A2 Inducers
- Cytochrome P-450 CYP1A2 Inducers (strength unknown)
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (moderate)
- Cytochrome P-450 CYP3A4 Inducers (weak)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (moderate)
- Cytochrome P-450 CYP3A5 Inducers (weak)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Increased Sympathetic Activity
- Nervous System
- Psychoanaleptics
- Psychostimulants, Agents Used for ADHD and Nootropics
- Stimulants
- Sympathomimetic-like Agent
- Wakefulness-Promoting Agents
- 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
- 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]
- 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]
- External Links
- Human Metabolome Database
- HMDB0014883
- KEGG Drug
- D01832
- PubChem Compound
- 4236
- PubChem Substance
- 46504648
- ChemSpider
- 4088
- BindingDB
- 50156055
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Basic Science Osteoarthritis (OA) 1 4 Completed Other Healthy Adults 1 4 Completed Treatment Attention / Executive Function (Cognition) / Memory, Short-Term 1 4 Completed Treatment Bipolar Disorder (BD) 1 4 Completed Treatment Fatigue 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
Form Route Strength Tablet Oral Tablet Oral 100 mg Tablet Oral 200.000 mg Tablet Oral 200 mg Tablet Oral 100 mg/1 Tablet Oral 200 mg/1 Capsule, liquid filled Oral 200 mg Capsule, liquid filled Oral 20000000 mg Capsule, liquid filled Oral 100 mg - Prices
Unit description Cost Unit Provigil 200 mg tablet 15.33USD tablet Provigil 100 mg tablet 13.58USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region USRE37516 No 2002-01-15 2014-10-06 US CA2165824 No 2005-08-02 2014-06-14 Canada CA2201967 No 2002-12-10 2015-10-04 Canada US7297346 Yes 2007-11-20 2024-05-29 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 164-166 °C Not Available water solubility Slightly soluble Not Available logP 0.6 Not Available - Predicted Properties
Property Value Source Water Solubility 0.622 mg/mL ALOGPS logP 1.75 ALOGPS logP 1.53 Chemaxon logS -2.6 ALOGPS pKa (Strongest Acidic) 8.84 Chemaxon pKa (Strongest Basic) -4.4 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 60.16 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 77.39 m3·mol-1 Chemaxon Polarizability 28.71 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9947 Caco-2 permeable + 0.5066 P-glycoprotein substrate Non-substrate 0.8912 P-glycoprotein inhibitor I Non-inhibitor 0.8842 P-glycoprotein inhibitor II Non-inhibitor 0.9962 Renal organic cation transporter Non-inhibitor 0.8153 CYP450 2C9 substrate Non-substrate 0.793 CYP450 2D6 substrate Non-substrate 0.8659 CYP450 3A4 substrate Non-substrate 0.5971 CYP450 1A2 substrate Non-inhibitor 0.6653 CYP450 2C9 inhibitor Non-inhibitor 0.6045 CYP450 2D6 inhibitor Non-inhibitor 0.9117 CYP450 2C19 inhibitor Non-inhibitor 0.6952 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6395 Ames test Non AMES toxic 0.6562 Carcinogenicity Non-carcinogens 0.6665 Biodegradation Ready biodegradable 0.6304 Rat acute toxicity 2.0926 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9799 hERG inhibition (predictor II) Non-inhibitor 0.9279
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-014i-2900000000-528a0bbea5cbea3771e1 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0900000000-55724283143adb967127 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0w29-0940000000-3fb2b28684be0db5d11b Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-9180000000-ac48fd1eebe59ea8cc8b Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0900000000-268fac20d4bebd0d237b Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-9110000000-f5e78ab116ca3103ec83 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-2900000000-3fded198d424bf150f12 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 169.1783845 predictedDarkChem Lite v0.1.0 [M-H]- 156.1436 predictedDeepCCS 1.0 (2019) [M+H]+ 169.8829845 predictedDarkChem Lite v0.1.0 [M+H]+ 158.5016 predictedDeepCCS 1.0 (2019) [M+Na]+ 169.2068845 predictedDarkChem Lite v0.1.0 [M+Na]+ 164.59474 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- 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
- 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]
- 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]
- Swanson JM: Role of executive function in ADHD. J Clin Psychiatry. 2003;64 Suppl 14:35-9. [Article]
- 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]
- 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
- 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
- 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
- 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]
- Robertson P Jr, Hellriegel ET: Clinical pharmacokinetic profile of modafinil. Clin Pharmacokinet. 2003;42(2):123-37. [Article]
- Modafinil FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- 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
- Robertson P Jr, Hellriegel ET: Clinical pharmacokinetic profile of modafinil. Clin Pharmacokinet. 2003;42(2):123-37. [Article]
- 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]
- 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]
- FDA interactions table [Link]
- Flockhart Table of Drug Interactions [Link]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInducer
- 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
- 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]
- 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]
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorInducer
- 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
- 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]
- 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]
- 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
- InhibitorInducer
- 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
- 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]
- 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]
- Modafinil FDA [File]
- Modafinil EMA label [File]
- 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
- 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 at June 13, 2005 13:24 / Updated at February 20, 2024 23:55