rivastigmine
Trade name: exelon
Approved
Apr 21, 2000
Rivastigmine (sold under the trade name Exelon) is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease. Rivastigmine, an acetylcholinesterase inhibitor, inhibits both butyrylcholinesterase and acetylcholinesterase (unlike donepezil, which selectively inhibits acetylcholinesterase). It is thought to work by inhibiting these cholinesterase enzymes, which would otherwise break down the brain neurotransmitter acetylcholine. Rivastigmine capsules, liquid solution, and patches are used for the treatment of mild to moderate dementia of the Alzheimer's type and for mild to moderate dementia related to Parkinson's disease. Rivastigmine has demonstrated treatment effects on the cognitive (thinking and memory), functional (activities of daily living) and behavioral problems commonly associated with Alzheimer's and Parkinson's disease dementia. In people with either type of dementia, rivastigmine has been shown to provide meaningful symptomatic effects that may allow patients to remain independent and ‘be themselves’ for longer. In particular, it appears to show marked treatment effects in patients showing a more aggressive course of the disease, such as those with younger-onset ages, poor nutritional status, or those experiencing symptoms such as delusions or hallucinations. Side effects may include nausea and vomiting, decreased appetite and weight loss. — NCATS
Clinical trial activity
84 trials · 80 clinical orgs · 21 marketing orgs
Earliest trial started Oct 1, 1998 (NCT00018278)
Timeline
2000s
- Apr 21, 2000
Novartis — Earliest FDA Approval
- Apr 21, 2000
Novartis — NDA Organization
- Jan 1, 2002
Earliest Phase 1 Sponsor(trial)
- Dec 21, 2005
Ranbaxy — Marketing Organization
- Jul 6, 2007
Sandoz — Marketing Organization
- Oct 22, 2007
Sun Pharmaceuticals — Marketing Organization
- Oct 31, 2007
Dr. Reddy's Laboratories — Marketing Organization
- Jan 1, 2008
Earliest Phase 2 Sponsor(trial)
- Jan 8, 2008
Watson Pharmaceuticals — Marketing Organization
2010s
- Jun 12, 2012
Alembic — Marketing Organization
- May 16, 2013
Apotex — Marketing Organization
- Aug 22, 2014
Macleods Pharmaceuticals, Ltd — Marketing Organization
- Aug 22, 2014
Neogen — Marketing Organization
- Jun 10, 2015
Orbion Pharms — Marketing Organization
- Jun 10, 2015
Orchid Pharma — Marketing Organization
- Aug 31, 2015
Alvogen — Marketing Organization
- Mar 25, 2016
Aurobindo Pharma — Marketing Organization
- Feb 13, 2017
Cadila Healthcare — Marketing Organization
- Sep 28, 2017
Chartwell Pharmaceuticals — Marketing Organization
- Jun 20, 2018
Mylan — Marketing Organization
- Jan 8, 2019
Amneal Pharmaceuticals — Marketing Organization
- Mar 4, 2019
Zydus Discovery DMCC — Marketing Organization
- Nov 26, 2019
Esteve Labs — Marketing Organization
2020s
- Sep 23, 2025
Yichang Humanwell Pharmaceutical Co.,Ltd — Marketing Organization
Indications
Approved for
Studied for
- Alzheimer Disease · Phase 4
- Anxiety Disorders · Phase 3
- Apathy · Phase 3
- Biological Availability · Early Phase 1
- Brain Injuries, Traumatic · Phase 4
- Central Nervous System Diseases · Phase 1
- Cholinergic Antagonists · Phase 2
- Cholinesterase Inhibitors · Phase 4
- Cocaine-Related Disorders · Phase 1
- Cognition Disorders · Phase 4
- Cognitive Dysfunction · Phase 4
- Delirium · Phase 4
- Dementia · Phase 3
- Dementia, Vascular · Phase 3
- Depression · Phase 3
- Depressive Disorder · Phase 4
- Down Syndrome · Phase 1/Phase 2
- Healthy Volunteers · Phase 4
- HIV Infections · Phase 4
- Hypotension, Orthostatic · Phase 1
- Lewy Body Disease · Phase 2
- Methamphetamine · Phase 1
- Multiple Sclerosis · Phase 4
- Neurobehavioral Manifestations · Phase 3
- Parkinson Disease · Phase 4
- Postoperative Cognitive Complications · Phase 4
- Psychophysiologic Disorders · Phase 3
- Pure Autonomic Failure · Phase 1
- Schizophrenia · Phase 3
- Stroke · Phase 4
- Substance-Related Disorders · Phase 1
- Supranuclear Palsy, Progressive · Phase 3
- Therapeutic Equivalency · Phase 1
Mechanism of action
- Cholinesterases; ACHE & BCHEINHIBITOR
Cholinesterases; ACHE & BCHE inhibitor
Approval history
- approvedApr 21, 2000
Chemistry & pharmacology
SMILES
CCN(C)C(=O)Oc1cccc([C@H](C)N(C)C)c1- Mol. weight
- 250.34 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral, Topical
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
Yes
Sources
- ChEMBLCHEMBL636 ↗
- WikipediaRivastigmine ↗
- NCATSPKI06M3IW0 ↗
- ChEMBLCHEMBL215645 ↗
- ChEMBLCHEMBL1201092 ↗
Also known as
- alzest
- eluden
- ena713
- ena713
- ena-713
- ena-713
- erastig
- exelon
- exelon
- exelon
- exelon
- kerstipon
- m-((s)-1-(dimethylamino)ethyl)phenyl ethylmethylcarbamate
- m-((s)-1-(dimethylamino)ethyl)phenyl ethylmethylcarbamate
- nimvastid
- nimvastid
- prometax
- prometax
- prometax
- prometax
- prometax
- prometax
- rivastigamine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine
- rivastigmine hexal
- rivastigmine hydrogen tartrate
- rivastigmine hydrogen tartrate
- rivastigmine tartrate
- rivastigmine tartrate
- rivastigmine tartrate
- rivastigmine tartrate
- (s)-3-(1-(dimethylamino)ethyl)phenyl ethylmethylcarbamate
- (s)-3-(1-(dimethylamino)ethyl)phenyl ethylmethylcarbamate
- sdz-212-713
- sdz-212-713
- sdz-ena-713
- sdz-ena-713
- somniton
- s-rivastigmine
- voleze
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06382649 | Phase 2 | Nov 30, 2025 | American Academy of Clinical Toxicology, Washington University in St. Louis |
| NCT07208344 | Early Phase 1 (Phase 1) | Jul 31, 2025 | Anhui Medical University |
| NCT06399679 | Phase 2 | Nov 4, 2024 | American Academy of Clinical Toxicology, Washington University in St. Louis |
| NCT06537076 | Phase 2 | Jan 1, 2024 | AriBio Co., Ltd., Samjin Pharmaceutical Co., Ltd., Yonsei University |
| NCT05853341 | Phase 1 | May 2, 2023 | Luye Pharma, SocraMetrics GmbH, SocraTec R&D GmbH |
| NCT05883124 | Phase 1 | Apr 17, 2023 | SocraTec R&D GmbH |
| NCT05768126 | Phase 4 | Sep 29, 2021 | St. Antonius Hospital, Nieuwegein, Tergooi Hospital, University of Groningen, Utrecht University, ZonMw: The Netherlands Organisation for Health Research and Development |
| NCT04226248 | Phase 3 | Jan 2, 2020 | University of Bath, University of Bristol |
| NCT04189666 | Phase 1/Phase 2 (Phase 2) | Nov 18, 2019 | Ain Shams University |
| NCT03915626 | Early Phase 1 (Phase 1) | Jul 1, 2019 | Food and Drug Administration, University of Maryland, University of Maryland, Baltimore County |
| NCT03957174 | N/A | Jun 30, 2019 | University of Oxford |
| NCT03840837 | Phase 4 | May 2, 2019 | National Institute on Aging (NIA), University of Maryland |
| NCT03659435 | Phase 1 | Aug 22, 2018 | SocraMetrics GmbH, SocraTec R&D GmbH |
| NCT03573050 | Phase 1 | May 16, 2018 | SocraMetrics GmbH, SocraTec R&D GmbH |
| NCT03454646 | Phase 4 | Mar 15, 2018 | University of Bordeaux |
| NCT02989402 | Phase 4 | May 31, 2017 | Novartis |
| NCT02703636 | Phase 4 | May 10, 2016 | Novartis |
| NCT02839642 | Phase 3 | May 1, 2016 | Aix-University of Marseille |
| NCT02444637 | Phase 4 | Apr 1, 2015 | National Neuroscience Institute |
| NCT02374567 | Phase 3 | Jan 1, 2015 | Gottfried Wilhelm Leibniz Universität Hannover |
Organizations
Research & Development (80)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Novartis | For profit | 37 | 29 | 3 | 1999 |
| SocraTec R&D GmbH | For profit | 4 | 3 | 1 | 2018 |
| National Institute on Drug Abuse (NIDA) | Government | 3 | 1 | 1 | 2006 |
| Ono Pharmaceuticals | For profit | 3 | 0 | 2 | 2007 |
| SocraMetrics GmbH | For profit | 3 | 0 | 1 | 2018 |
| Utrecht University | Academic/Hospital | 3 | 3 | 2 | 2008 |
| ZonMw: The Netherlands Organisation for Health Research and Development | Academic/Hospital | 3 | 0 | 1 | 2008 |
| American Academy of Clinical Toxicology | Academic/Hospital | 2 | 0 | 1 | 2024 |
| Baylor University | Academic/Hospital | 2 | 2 | 1 | 2009 |
| Department of Veteran Affairs | Government | 2 | 2 | 2 | 1998 |
| Dr. Reddy's Laboratories | For profit | 2 | 2 | 1 | 2004 |
| National Neuroscience Institute | Government | 2 | 1 | 1 | 2006 |
| New York University | Academic/Hospital | 2 | 1 | 2 | 1999 |
| SFBC Anapharm | For profit | 2 | 0 | 1 | 2004 |
| University of Groningen | Academic/Hospital | 2 | 0 | 1 | 2013 |
| University of Maryland | Academic/Hospital | 2 | 2 | 2 | 2019 |
| University of Munster | Academic/Hospital | 2 | 2 | 1 | 2004 |
| Washington University in St. Louis | Academic/Hospital | 2 | 2 | 1 | 2024 |
| Ain Shams University | Academic/Hospital | 1 | 1 | 1 | 2019 |
| Aix-University of Marseille | Academic/Hospital | 1 | 1 | 1 | 2016 |
Marketing (25)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Alembic | For profit | MKTG | Jun 12, 2012 |
| Alvogen | For profit | MKTG | Aug 31, 2015 |
| Alvogen | For profit | SYN | Aug 31, 2015 |
| Amneal Pharmaceuticals | For profit | MKTG | Jan 8, 2019 |
| Apotex | For profit | MKTG | May 16, 2013 |
| Aurobindo Pharma | For profit | MKTG | Mar 25, 2016 |
| Aurobindo Pharma | For profit | SYN | Mar 25, 2016 |
| Cadila Healthcare | For profit | MKTG | Feb 13, 2017 |
| Chartwell Pharmaceuticals | For profit | MKTG | Sep 28, 2017 |
| Dr. Reddy's Laboratories | For profit | MKTG | Oct 31, 2007 |
| Esteve Labs | For profit | MKTG | Nov 26, 2019 |
| Macleods Pharmaceuticals, Ltd | For profit | MKTG | Aug 22, 2014 |
| Mylan | For profit | MKTG | Jun 20, 2018 |
| Neogen | For profit | MKTG | Aug 22, 2014 |
| Novartis | For profit | NDA | Apr 21, 2000 |
| Orbion Pharms | For profit | MKTG | Jun 10, 2015 |
| Orchid Pharma | For profit | MKTG | Jun 10, 2015 |
| Ranbaxy | For profit | MKTG | Dec 21, 2005 |
| Sandoz | For profit | MKTG | Jul 6, 2007 |
| Sun Pharmaceuticals | For profit | MKTG | Oct 22, 2007 |
| Sun Pharmaceuticals | For profit | SYN | Oct 22, 2007 |
| Watson Pharmaceuticals | For profit | MKTG | Jan 8, 2008 |
| Yichang Humanwell Pharmaceutical Co.,Ltd | For profit | MKTG | Sep 23, 2025 |
| Zydus Discovery DMCC | For profit | MKTG | Mar 4, 2019 |
| Zydus Discovery DMCC | For profit | SYN | Mar 4, 2019 |