armodafinil
Trade name: nuvigil
Approved
Jun 15, 2007
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. 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. Modafinil is indicated for the improvement of wakefulness in patients with excessive daytime sleepiness (EDS) associated with narcolepsy. — NCATS
Clinical trial activity
56 trials · 36 clinical orgs · 11 marketing orgs
Earliest trial started Jan 1, 2004 (NCT00078312)
Timeline
2000s
2010s
- Jun 1, 2012
Mylan — Marketing Organization
- Aug 29, 2012
Watson Pharmaceuticals — Marketing Organization
- Aug 29, 2012
Actavis — Marketing Organization
- Sep 24, 2014
Teva — Marketing Organization
- Nov 28, 2016
Lupin — Marketing Organization
- Nov 28, 2016
Natco Pharma — Marketing Organization
- Mar 6, 2018
Aurobindo Pharma — Marketing Organization
- Mar 25, 2019
Apotex — Marketing Organization
- Mar 25, 2019
Corepharma — Marketing Organization
- Mar 25, 2019
Amneal Pharmaceuticals — Marketing Organization
Indications
Studied for
- Apnea · Phase 3
- Binge-Eating Disorder · Phase 3
- Brain Injuries, Traumatic · Phase 3
- Brain Neoplasms · Phase 2
- Breast Neoplasms · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Cognition Disorders · Phase 2
- Depression · Phase 3
- Disorders of Excessive Somnolence · Phase 3
- Drug-Related Side Effects and Adverse Reactions · Phase 2
- Dysthymic Disorder · Phase 4
- Esophageal Neoplasms · Phase 2
- Fatigue · Phase 4
- Fibromyalgia · Phase 4
- Glioma · Phase 2
- Head and Neck Neoplasms · Phase 1/Phase 2
- Healthy Volunteers · Phase 1/Phase 2
- Hepatitis C · Phase 4
- HIV Infections · Phase 4
- Infant, Premature · Phase 3
- Lewy Body Disease · Phase 4
- Major Depressive Disorder · Phase 4
- Menopause · Phase 4
- Multiple Myeloma · Phase 3
- Multiple Sclerosis · Phase 2/Phase 3
- Neoplasms · Phase 2
- Nervous System Neoplasms · Phase 2
- Nocturia · Phase 2/Phase 3
- Obesity · Phase 3
- Overweight · Phase 3
- Paresis · Phase 2
- Psychotic Disorders · Phase 4
- Sarcoidosis · Phase 2/Phase 3
- Schizophrenia · Phase 4
- Sleep Apnea, Obstructive · Phase 4
- Sleep Apnea Syndromes · Phase 3
- Sleep Deprivation · Phase 2
- Sleep Disorders, Circadian Rhythm · Phase 3
- Sleep Disorders, Intrinsic · Phase 4
- Sleepiness · Phase 2/Phase 3
- Sleep Initiation and Maintenance Disorders · Phase 2/Phase 3
- Sleep Wake Disorders · Phase 4
- Stroke · Phase 2
Mechanism of action
- Dopamine transporterINHIBITOR
SLC6A3 inhibitor
Approval history
- approvedJun 15, 2007
Chemistry & pharmacology
SMILES
NC(=O)C[S@@+]([O-])C(C1=CC=CC=C1)C2=CC=CC=C2- Mol. weight
- 273.35 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaArmodafinil ↗
- NCATSV63XWA605I ↗
- ChEMBLCHEMBL1201192 ↗
Also known as
- (–)-2-[(r)-(diphenylmethyl)sulfinyl]acetamide
- (–)-2-[(r)-(diphenylmethyl)sulfinyl]acetamide
- 2-((r)-(diphenylmethyl)sulfinyl)acetamide
- armodafinil
- armodafinil
- armodafinil
- armodafinil
- armodafinil
- armodafinil
- armodafinil
- armodafinil
- armodafinil
- armodafinil
- armodanifil
- cep-10953
- cep-10953
- cep-10953
- nuvigil
- nuvigil
- nuvigil
- nuvigil
- nuvigil
- nuvigil
- nuvigil
- nuvigil
- r-modafinil
- r-modafinil
- r-modafinil
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02468856 | Phase 1 | May 21, 2017 | University of Florida |
| NCT02552303 | N/A | Apr 1, 2014 | Teva, University of Pennsylvania |
| NCT01781468 | Phase 3 | Jun 1, 2013 | Mayo Clinic, National Cancer Institute (NCI) |
| NCT01219673 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2013 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT01746043 | Phase 2 | Feb 1, 2013 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT01624480 | Phase 1 | Jul 1, 2012 | Teva |
| NCT01470651 | Phase 4 | Oct 1, 2011 | Cornell University, Icahn School of Medicine at Mount Sinai, Research Foundation for Mental Hygiene, Inc. |
| NCT01460628 | Phase 4 | Oct 1, 2011 | Harvard University, Teva |
| NCT02478580 | Phase 3 | Aug 1, 2011 | The University of Texas, Dallas |
| NCT01317550 | N/A | Jul 1, 2011 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT01431573 | N/A | Jul 1, 2011 | Columbia University |
| NCT01330446 | Phase 1/Phase 2 (Phase 2) | May 1, 2011 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT02151253 | Phase 2/Phase 3 (Phase 3) | May 1, 2011 | Duke University |
| NCT01169753 | N/A | May 1, 2011 | Cephalon, University of Texas at Houston |
| NCT01305408 | Phase 3 | Mar 1, 2011 | Cephalon |
| NCT01011218 | Phase 2/Phase 3 (Phase 3) | Jan 1, 2011 | National Cancer Institute (NCI), Stanford University |
| NCT01256905 | N/A | Dec 1, 2010 | Cephalon, New York University |
| NCT01400958 | Phase 2 | Dec 1, 2010 | Cephalon, University of South Florida |
| NCT01032200 | Phase 2 | Aug 1, 2010 | National Cancer Institute (NCI), Wake Forest University |
| NCT01160380 | Phase 3 | Jun 1, 2010 | Cephalon, James R. Berenson MD, Inc., Oncotherapeutics |
Organizations
Research & Development (36)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Cephalon | For profit | 31 | 22 | 4 | 2004 |
| National Cancer Institute (NCI) | Government | 9 | 1 | 3 | 2008 |
| University of Texas at Houston | Academic/Hospital | 6 | 6 | 2 | 2010 |
| Teva | For profit | 4 | 1 | 4 | 2008 |
| Harvard University | Academic/Hospital | 3 | 3 | 2 | 2007 |
| Columbia University | Academic/Hospital | 2 | 2 | 2 | 2008 |
| Mayo Clinic | Academic/Hospital | 2 | 1 | 2 | 2009 |
| University of Cincinnati | Academic/Hospital | 2 | 2 | 1 | 2007 |
| University of Pennsylvania | Academic/Hospital | 2 | 2 | 2 | 2009 |
| Brain & Behavior Research Foundation | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Burke Rehabilitation Hospital | Academic/Hospital | 1 | 1 | 1 | 2008 |
| Clinilabs | For profit | 1 | 0 | 1 | 2010 |
| Cornell University | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Dartmouth University | Academic/Hospital | 1 | 0 | 1 | 2008 |
| Duke University | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Icahn School of Medicine at Mount Sinai | Academic/Hospital | 1 | 0 | 1 | 2011 |
| James R. Berenson MD, Inc. | Academic/Hospital | 1 | 0 | 1 | 2010 |
| National Institute of Mental Health (NIMH) | Government | 1 | 0 | 1 | 2008 |
| National Institute on Aging (NIA) | Government | 1 | 0 | 1 | 2009 |
| New York University | Academic/Hospital | 1 | 1 | 1 | 2010 |
Marketing (12)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Actavis | For profit | MKTG | Aug 29, 2012 |
| Amneal Pharmaceuticals | For profit | MKTG | Mar 25, 2019 |
| Apotex | For profit | MKTG | Mar 25, 2019 |
| Apotex | For profit | SYN | Mar 25, 2019 |
| Aurobindo Pharma | For profit | MKTG | Mar 6, 2018 |
| Cephalon | For profit | NDA | Jun 15, 2007 |
| Corepharma | For profit | MKTG | Mar 25, 2019 |
| Lupin | For profit | MKTG | Nov 28, 2016 |
| Mylan | For profit | MKTG | Jun 1, 2012 |
| Natco Pharma | For profit | MKTG | Nov 28, 2016 |
| Teva | For profit | MKTG | Sep 24, 2014 |
| Watson Pharmaceuticals | For profit | MKTG | Aug 29, 2012 |