Exelon (rivastigmine tartrate)

The following drug information is obtained from various newswires, published medical journal articles, and medical conference presentations.


Approval Status:

Approved April 2000

Specific Treatments:

Indicated for the treatment of mild to moderate dementia of the Alzheimer's type

Therapeutic Areas

General Information

Exelon has been approved in oral solution and capsule form for the treatment of mild to moderate Alzheimer's disease. This drug belongs to the class of drugs called cholinesterase inhibitors. Cholinesterase breaks down acetylcholine, a neurotransmitter which assists in human memory and cognition processes. By inhibiting cholinesterase, more acetylcholine available to the patient for memory and cognitive functioning. This is effective in treatment of Alzheimer's disease, since acetylcholine is at significantly lower levels in Alzheimer's patients than in normally functioning people.

Exelon has been shown to improve patients' performance in the three major domains of assessment of Alzheimer's: global functioning (such as activities of daily living), behavior, and cognition.

Another long term advantage to the drug is that it could treat symptoms early on in the deterioration process. Delaying the onset of the disease by five years in patients could save up to $50 billion in U.S. healthcare costs annually (half of the current annual cost).

Currently, 70 countries have approved Exelon for marketing.

Alzheimer's Disease is a neurodegenerative disease affecting up to 4 million adults in the U.S. and 10 million worldwide. Memory loss and other cognitive and behavior deteriorations are symptoms of the disease. As there is no current cure, Alzheimer's Disease is fatal.

Clinical Results

The safety and efficacy of Exelon was investigated in two placebo-controlled investigations. Participants, all Alzheimer's patients, were evaluated in terms of their cognitive performance using the Alzheimer's Disease Assessment Scale (ADAS-cog) and the Clinician's Interview Based Impression of Change (CIBIC-Plus). The ADAS-cog considers elements of memory, orientation, attention, reasoning, language and praxis. Improvement in global functioning was measured by the CIBIC-Plus. This instrument of evaluation considers overall patient cognition, behavior and functioning. The patient population for this study reflected a real world population, since most of the patients used concomitant medications to treat other conditions during the studies.

In a 26-week, U.S. study, patients were divided into three groups, each receiving 1-4 mg/day of Exelon, 6-12 mg/day of Exelon, or placebo. At the end of the treatment period, both ADAS-cog scores and CIBIC-Plus ratings for those treated in either dose-group of Exelon were significantly superior than scores of those who took placebo. Furthermore, the higher-dosage group had better ADAS-cog scores and CIBIC-Plus ratings than the lower-dosage group. Better scores in these assessments indicate greater improvement and less worsening in cognitive function (such as memory, recognition, ability to speak, and other symptoms of dementia) than the average placebo-treated patient.

In a 26-week, global study, patients were divided into similar groups. Results of this study also indicated that the 6-12 mg/day group showed significantly better ratings for CIBIC-Plus than placebo, and significantly better scores on the ADAS-cog scale, compared to placebo and the 1-4 mg/day group. However, the 1-4 mg/day treatment group did not improve significantly over placebo with either assessment tool.

To date, 5,300 patients have received Exelon in clinical research studies. This is considered the largest phase III program of an Alzheimer's treatment.

Side Effects

The following are the most common side effects of Exelon, as experienced by patients in clinical studies:

  • Nausea
  • Vomiting
  • Anorexia
  • Dyspepsia
  • Asthenia
  • Weight loss*

*26% of women, and 18% of men in the high-dose group

The above effects were experienced with greater frequency earlier in the treatment.

Mechanism of Action

Pathological changes in Dementia of the Alzheimer's type involve cholinergic neuronal pathways that project from the basal forebrain to the cerebral cortex and hippocampus. These pathways are thought to be intricately involved in memory, attention, learning, and other cognitive processes. While the precise mechanism of rivastigmine's action unknown, it is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. If this proposed mechanism is correct, Exelon's effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. There is no evidence that rivastigmine alters the course of the underlying dementing process. After a 6 mg dose of rivastigmine, anticholinesterase activity is present in CSF for about 10 hours, with a maximum inhibition of about 60% five hours after dosing.
(From FDA Label)

Additional Information

Visit the Novartis Pharmaceuticals U.S. web site to learn more about Exelon and about other products, research, and services provided by the company that developed this drug.

For more information about Alzheimer's Disease, visit Novartis's Alzheimer's Disease site: http://www.alzheimersdisease.com, designed to educate and support Alzheimer's patients' caregivers.

or visit the Alzheimer's Association web site, which provides information for patients, families, physicians, as well as recent research and glossary about Alzheimer's Disease.