Anavex Life Sciences Corp (AVXL)

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Current Alzheimer’s Drugs vs. Anavex

Treatment for Mild to Moderate Alzheimer’s

Medications called cholinesterase inhibitors are prescribed for mild to moderate Alzheimer’s disease. These drugs may help delay or prevent symptoms from becoming worse for a limited time and may help control some behavioral symptoms. The medications are Razadyne® (galantamine), Exelon® (rivastigmine), and Aricept® (donepezil).

Scientists do not yet fully understand how cholinesterase inhibitors work to treat Alzheimer’s disease, but research indicates that they prevent the breakdown of acetylcholine, a brain chemical believed to be important for memory and thinking. As Alzheimer’s progresses, the brain produces less and less acetylcholine; therefore, cholinesterase inhibitors may eventually lose their effect.

https://www.nia.nih.gov/health/how-alzheimers-disease-treated

Interestingly, I can find no authoritative source that claims the three existing Alzheimer’s drugs, Razadyne® (galantamine), Exelon® (rivastigmine), and Aricept® (donepezil) work by restoration of neuron homeostasis resulting from their putative sigma-1 receptor agonism traits (if any). In each case, their recognized mechanism of action is suppression of acetylcholinesterase inhibitors, allowing elevated or normal concentrations of the neuron synapse molecule acetelycholine to be created or maintained. With this, normal neurotransmission across the synapse can occur, at least for a time.

But more importantly in regard to Anavex 2-73, none of the positive symptomatic outcomes of these three acetylcholinesterase inhibitors endures or persists. Each of them warns in the label information that the drugs will merely slow or temporarily stop symptomatic progression of Alzheimer’s. None provide lasting symptomatic relief, comparable in any way with the anecdotal results yet persisting in the Australian clinical participants.

Here is a summary of the five drugs FDA approved for Alzheimer’s treatment. None are claimed to be sigma-1 receptor agonists. They are either cholinesterase inhibitors or N-methyl D-aspartate (NMDA) antagonists.
https://www.nia.nih.gov/health/how-alzheimers-disease-treated

Notice the side effects of each. These were mild or absent in the Australian Anavex 2-73 trial.

Aricept® (donepezil) Cholinesterase inhibitor prescribed to treat symptoms of mild, moderate, and severe Alzheimer's Prevents the breakdown of acetylcholine in the brain. Nausea, vomiting, diarrhea, muscle cramps, fatigue, weight loss

Exelon® (rivastigmine) Cholinesterase inhibitor prescribed to treat symptoms of mild to moderate Alzheimer's (patch is also for severe Alzheimer's) Prevents the breakdown of acetylcholine and butyrylcholine (a brain chemical similar to acetylcholine) in the brain. Nausea, vomiting, diarrhea, weight loss, indigestion, muscle weakness

Namenda® (memantine) N-methyl D-aspartate (NMDA) antagonist prescribed to treat symptoms of moderate to severe Alzheimer's Blocks the toxic effects associated with excess glutamate and regulates glutamate activation. Dizziness, headache, diarrhea, constipation, confusion

Namzaric® (memantine extended-release and donepezil) NMDA antagonist and cholinesterase inhibitor prescribed to treat symptoms of moderate to severe Alzheimer’s (for patients stabilized on both memantine and donepezil taken separately) Blocks the toxic effects associated with excess glutamate and prevents the breakdown of acetylcholine in the brain. Headache, nausea, vomiting, diarrhea, dizziness

Razadyne® (galantamine) Cholinesterase inhibitor prescribed to treat symptoms of mild to moderate Alzheimer's Prevents the breakdown of acetylcholine and stimulates nicotinic receptors to release more acetylcholine in the brain. Nausea, vomiting, diarrhea, decreased appetite, dizziness, headache

It is stated on this National Institute on Aging webpage, “It is important to understand that none of these medications stops the disease itself. “

I can see no evidence that any of these existing drugs will out-compete Anavex 2-73, should it replicate the Australian results in the up-coming double-blind Phase 3 study. No evidence has been presented (only hope for such) that it won’t.