Armodafinil

Summary

Armodafinil (CHEMBL1201192) is an approved small-molecule central nervous system stimulant (ATC N06BA13); indicated across 20 conditions including attention deficit-hyperactivity disorder and obstructive sleep apnea syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N06BA13
• Indications: 20 conditions
• Clinical trials: 55
• Chemistry: 273.4 Da · C15H15NO2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201192
Name	Armodafinil
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9690109
ChEBI	CHEBI:77590
ATC	N06BA13
Molecular formula	C15H15NO2S
Molecular weight	273.4
InChIKey	YFGHCGITMMYXAQ-LJQANCHMSA-N

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

IUPAC name: 2-[(R)-benzhydrylsulfinyl]acetamide

ChEBI definition: A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness.

Pharmacological roles (ChEBI): central nervous system stimulant, eugeroic.

Also known as: Armodafinil, Armodafinilo, CEP-10952, CEP-10953, CRL-40982, Modafinil, (r)-, NSC-751850, NSC-758711, Nuvigil, R-(-)-modafinil, (R)-Modafinil, ARMODAFINIL

Patent coverage: 3,721 distinct patent families (14,479 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: D(2) dopamine receptor, D(3) dopamine receptor, Sodium-dependent dopamine transporter, Sodium-dependent dopamine transporter.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 6 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD2	8.68	IC50	2.1	nM	CHEMBL_ACT_16772099
SLC6A3	6.19	Ki	647	nM	CHEMBL_ACT_16772111
P23977	5.52	Ki	3050	nM	CHEMBL_ACT_16771904
P23977	5.49	Ki	3260	nM	CHEMBL_ACT_5208036
SLC6A3	5.18	IC50	6600	nM	CHEMBL_ACT_19151466

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

4 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
attention deficit-hyperactivity disorder	4	MONDO:0007743	EFO:0003888
obstructive sleep apnea syndrome	4	MONDO:0007147	EFO:0003918
sleep disorder	4	MONDO:0100081	EFO:0008568
narcolepsy	4	MONDO:0021107	MONDO:0021107

12 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
hypersomnia	3	MONDO:0005466	EFO:0005246
obesity disorder	3	MONDO:0011122	EFO:0001073
brain injury	3	MONDO:0043510	MONDO:0043510
depressive disorder	3	MONDO:0002050	MONDO:0002050
sleep apnea syndrome	3	MONDO:0005296	EFO:0003877
insomnia	2	MONDO:0013600	EFO:0004698
neoplasm	2	MONDO:0005070	EFO:0000616
stroke disorder	2	MONDO:0005098	EFO:0000712
glioma	2	MONDO:0021042	MONDO:0100342
multiple sclerosis	2	MONDO:0005301	MONDO:0005301
non-small cell lung carcinoma	1	MONDO:0005233	EFO:0003060
head and neck cancer	1	MONDO:0005627	EFO:0006859

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

Clinical trials

Total trials: 55.

Phase distribution

Phase	Trials
PHASE3	19
PHASE2	12
PHASE4	9
Not specified	6
PHASE1/PHASE2	4
PHASE2/PHASE3	3
PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00373672	PHASE4	COMPLETED	Effects of Armodafinil on Cognition for Patients With Schizophrenia or Schizoaffective Disorder
NCT00518986	PHASE4	COMPLETED	Efficacy and Safety of Armodafinil for Adults With Excessive Sleepiness Obstructive Sleep Apnea/Hypopnea and Depression
NCT00678691	PHASE4	COMPLETED	An Eight Week, Double-Blind Efficacy Study of Armodafinil Augmentation to Alleviate Fibromyalgia Fatigue
NCT00711516	PHASE4	COMPLETED	Study to Evaluate Armodafinil Treatment in Improving Prefrontal Cortical Activation and Working Memory Performance
NCT00737204	PHASE4	COMPLETED	Effectiveness of Armodafinil for Treating Fatigue in Adults With HIV/AIDS
NCT01023672	PHASE4	COMPLETED	Pilot Study of Armodafinil in Patients With Dementia With Lewy Bodies
NCT01080807	PHASE4	COMPLETED	Efficacy and Tolerability of Armodafinil in Adults With Excessive Sleepiness Associated With Shift Work Disorder
NCT01460628	PHASE4	COMPLETED	Effect of Nuvigil on Fatigue
NCT01470651	PHASE4	TERMINATED	Armodafinil for Patients Starting Hepatitis C Virus Treatment
NCT00078312	PHASE3	COMPLETED	Armodafinil (CEP-10953) for Treatment of Narcolepsy, Obstructive Sleep Apnea/Hypopnea Syndrome, or Chronic Shift Work Sleep Disorder
NCT00078325	PHASE3	COMPLETED	Armodafinil (CEP-10953) in Treatment of Excessive Sleepiness Associated With Obstructive Sleep Apnea/Hypopnea Syndrome(OSAHS)
NCT00078377	PHASE3	COMPLETED	Safety and Efficacy Study of Armodafinil (CEP-10953) in the Treatment of Excessive Sleepiness Associated With Narcolepsy
NCT00079677	PHASE3	COMPLETED	Armodafinil (CEP-10953) in Treatment of Excessive Sleepiness Associated With Obstructive Sleep Apnea/Hypopnea (OSA/H) Syndrome
NCT00080288	PHASE3	COMPLETED	Safety/Efficacy Study With Armodafinil (CEP-10953) in Treatment of Excessive Sleepiness Associated With Chronic SWSD
NCT00228553	PHASE3	COMPLETED	Extension Study of the Safety and Efficacy of Armodafinil in the Treatment of Patients With Excessive Sleepiness
NCT00228566	PHASE3	COMPLETED	Study to Assess Patient Reported Outcomes With Armodafinil Treatment for Excessive Sleepiness in Adults With Narcolepsy or Obstructive Sleep Apnea/Hypopnea Syndrome
NCT00236080	PHASE3	COMPLETED	Study of the Efficacy and Multiple-Dose Plasma Concentration-Time Profiles of Armodafinil and PROVIGIL
NCT00555347	PHASE2/PHASE3	COMPLETED	Use of Armodafinil for Fatigue in Sarcoidosis
NCT00758498	PHASE3	COMPLETED	Study of the Effect of Armodafinil Treatment in Healthy Subjects With Excessive Sleepiness Associated With Jet Lag Disorder
NCT00893789	PHASE3	TERMINATED	Study to Evaluate the Efficacy and Safety of Armodafinil as Treatment for Patients With Excessive Sleepiness Associated With Mild or Moderate Closed Traumatic Brain Injury
NCT00981084	PHASE2/PHASE3	COMPLETED	Impact of Armodafinil on Neurocognition and Cognitive Fatigue in Multiple Sclerosis (MS)
NCT00983437	PHASE3	TERMINATED	Study to Evaluate the Safety, Tolerability, and Efficacy of Armodafinil as Treatment for Patients With Excessive Sleepiness Associated With Mild or Moderate Closed Traumatic Brain Injury
NCT01010789	PHASE3	COMPLETED	Armodafinil in Binge Eating Disorder (BED)
NCT01072630	PHASE3	COMPLETED	Study to Evaluate the Efficacy and Safety of Armodafinil Treatment as Adjunctive Therapy in Adults With Major Depression Associated With Bipolar I Disorder
NCT01072929	PHASE3	COMPLETED	A Study to Evaluate the Efficacy and Safety of Armodafinil Treatment as Adjunctive Therapy in Adults With Major Depression Associated With Bipolar I Disorder
NCT01121536	PHASE3	TERMINATED	Extension Study of the Safety and Efficacy of Armodafinil Treatment as Adjunctive Therapy in Adults With Major Depression Associated With Bipolar I Disorder
NCT01160380	PHASE3	COMPLETED	A Study of the Effectiveness of Armodafinil to Treat Cancer-Related Fatigue in Patients With Multiple Myeloma
NCT01305408	PHASE3	COMPLETED	Study to Evaluate the Efficacy and Safety of Armodafinil Treatment (150 mg/Day) as Adjunctive Therapy in Adults With Major Depression Associated With Bipolar I Disorder
NCT01781468	PHASE3	COMPLETED	Armodafinil in Reducing Cancer-Related Fatigue in Patients With High Grade Glioma
NCT02151253	PHASE2/PHASE3	COMPLETED	Cross-over Study of Armodafinil Treatment of Daytime Sleepiness Associated With Treated Nocturia
NCT02478580	PHASE3	COMPLETED	Armodafinil (Nuvigil), Postoperative Recovery of OSA (Obstructive Sleep Apnea) and Obese Patients
NCT00481195	PHASE2	COMPLETED	Armodafinil Treatment as Adjunctive Therapy in Adults With Major Depression Associated With Bipolar I Disorder
NCT00487942	PHASE2	COMPLETED	Efficacy and Safety of Armodafinil as Adjunctive Therapy in Schizophrenic Adults With Cognitive Deficits
NCT00592943	PHASE1/PHASE2	COMPLETED	PET Study Examining the Dopaminergic Activity of Armodafinil in Adults
NCT00766467	PHASE2	COMPLETED	A Randomized Placebo-Controlled Trial of Armodafinil (Nuvigil) for Fatigue in Patients With Malignant Gliomas
NCT00772005	PHASE2	COMPLETED	Study to Evaluate the Efficacy and Safety of Armodafinil as Adjunctive Therapy in Adults With Schizophrenia
NCT00825227	PHASE2	TERMINATED	Safety and Efficacy of Armodafinil for Fatigue Associated With Taxanes Alone or in Combination With Other Agents
NCT01011218	PHASE2	COMPLETED	Management of Insomnia in Breast Cancer Patients
NCT01019187	PHASE2	COMPLETED	Cognitive Behavioral Therapy With or Without Armodafinil in Treating Cancer Survivors With Insomnia and Fatigue After Chemotherapy
NCT01032200	PHASE2	COMPLETED	Armodafinil in Treating Fatigue Caused By Radiation Therapy in Patients With Primary Brain Tumors
NCT01048983	PHASE1/PHASE2	WITHDRAWN	Reducing Symptom Burden - Non Small Cell Lung Cancer (NSCLC)
NCT01091974	PHASE2	COMPLETED	Cognitive Behavioral Therapy +/- Armodafinil for Insomnia and Fatigue Following Chemotherapy
NCT01096680	PHASE2	COMPLETED	Pharmacodynamic Profile of SPD489 in Healthy Adult Males Undergoing a Nocturnal Period of Acute Sleep Loss
NCT01219673	PHASE1/PHASE2	TERMINATED	Symptom Burden in Head and Neck Cancer
NCT01330446	PHASE1/PHASE2	COMPLETED	Single Agent Armodafinil for Patient-Reported Fatigue Following Radiation Therapy for Head and Neck Cancer
NCT01746043	PHASE2	COMPLETED	A Phase II Study of Minocycline and Armodafinil for Reducing the Symptom Burden Produced by Chemoradiation Treatment for Esophageal Cancer
NCT01896128	PHASE2	COMPLETED	Combining Armodafinil With Neuro-rehabilitation to Improve Neurological Recovery and Reduce Disability Post-Stroke
NCT01624480	PHASE1	COMPLETED	Study to Evaluate the Pharmacokinetics, Pharmacodynamics, and Safety of Armodafinil in Children and Adolescents With Excessive Sleepiness Associated With Narcolepsy
NCT02468856	PHASE1	COMPLETED	Effect of Armodafinil on Simulated Driving
NCT01044004	Not specified	WITHDRAWN	Evaluate the Efficacy of Armodafinil for Patients With B-cell Lymphoma and Severe Fatigue
NCT01169753	Not specified	TERMINATED	Nuvigil in Treatment of Cancer-Related Fatigue in Chronic Myeloid Leukemia Patients
NCT01256905	Not specified	WITHDRAWN	Attention Modulation for Treatment of Parkinson’s Disease and Dementia With Lewy Bodies
NCT01317550	Not specified	COMPLETED	A Study for Reducing Symptom Burden Produced by Chemoradiation Treatment for Non Small Cell Lung Cancer by Minocycline and Armodafinil
NCT01792583	Not specified	TERMINATED	The Nuvigil and Provigil Pregnancy Registry
NCT02552303	Not specified	COMPLETED	The Treatment of Insomnia Comorbid With Sleep Disordered Breathing Using Armodafinil and/or Cognitive Behavioral Therapy for Insomnia

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).