FDA approves benzgalantamine for treatment of Alzheimer disease

A novel oral therapy, Zunveyl has a dual mechanism of action designed to eliminate drug absorption in the GI tract, potentially addressing certain tolerability issues with leading AD medications, combined with the efficacy and long-term benefit profile of galantamine. Tolerability affects therapy adherence, with data showing that 55% of AD patients discontinue their medication after one year, mainly due to GI side effects and insomnia. Medication discontinuation can cause risk to patients themselves, and dissatisfaction and burden among nursing home staff, physicians, and caregivers.

Zunveyl, a prodrug of AD treatment galantamine and an acetylcholinesterase inhibitor (AChEI), is postulated to exert its therapeutic effect by preventing the breakdown of acetylcholine, the important brain neurotransmitter involved in memory, motivation, and attention functions. It is also an allosteric potentiator of alpha-7 nicotinic acetylcholine and alpha4beta2 receptors. This action facilitates the release of acetylcholine from the presynaptic neurons, giving clinical significance to its dual mode of action. Zunveyl targets AD symptoms, to provide patients with long-lasting benefits to cognitive and global function and the ability to perform daily activities that are impaired by AD.

Galantamine, FDA-approved since 2001, has extensive and positive data related to long-term outcomes, demonstrating activity among multiple brain receptors, anti-inflammatory effects, and is associated with improved memory, attention, and a significantly lower risk of death. It also has the strongest effect on cognitive decline in the AChEI class of medications and demonstrated significant risk reduction of developing severe dementia. Due to its prodrug properties, Zunveyl is effectively converted into the active moiety of galantamine after it passes through the GI tract, therefore achieving the same therapeutic effects of galantamine. It was also uniquely designed to eliminate drug absorption in the GI tract, potentially addressing certain tolerability issues and has a CNS safety profile that includes no incidence of insomnia.

“I am very excited about the approval of Zuveyl, which we believe offers better tolerability for patients with Alzheimer's disease. We have always believed in the efficacy of galantamine but have been limited in its use due to tolerability issues. To now have an agent with the efficacy of galantamine, but that also offers the hope of better tolerability, will provide physicians a great option to treat patients,” said Elaine Peskind, MD, the Friends of Alzheimer’s Research Professor of Psychiatry at the University of Washington School of Medicine. “This advancement marks a meaningful step forward in improving the quality of life for those living with Alzheimer's and their families. As a geriatric psychiatrist specializing in Alzheimer’s disease, I am eager to incorporate this new treatment into our practice and see the positive difference it will make.”