On Jul. 29, 2024, announces that the U.S. Food and Drug Administration (FDA) has granted approval for ZUNVEYL® (benzgalantamine) previously known as ALPHA-1062, for the treatment of mild-to-moderate Alzheimer’s disease.  Alzheimer’s disease (AD) is a progressive brain disorder that slowly destroys memory, thinking skills, and eventually the ability to do simple tasks, like carry on a conversation. AD is the most common form of dementia affecting nearly 7 million people, and is the leading cause of nursing home admissions and deaths, with 70% of all nursing home residents suffering with AD.

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 α-7 nicotinic acetylcholine and α4β2 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. Information about ZUNVEYL’S pivotal clinical studies are included further in this press release, and in the ZUNVEYL prescribing information.