Benzgalantamine gluconate Usage And Synthesis

Description

Benzgalantamine is a prodrug of galantamine. Gastrointestinal adverse effects are the most frequently reported side effects in patients undergoing treatment with cholinesterase inhibitors, including galantamine, and are often a reason for treatment discontinuation. As a prodrug, benzagalantamine remains inert as it passes through the stomach, thereby avoiding many of the gastrointestinal effects associated with peripheral cholinesterase inhibition.
Benzgalantamine was approved by the FDA in July 2024 for the treatment of mild-to-moderate dementia in Alzheimer's patients.

Chemical Properties

Benzgalantamine gluconate is derived from the dried flowers of Lycoris radiata (family Amaryllidaceae, formerly classified as Liliaceae/Lycoraceae). It occurs as a white or off-white crystalline powder, odorless with a bitter taste. It is soluble in water, slightly soluble in ethanol, almost insoluble in acetone, trichloromethane and ether.

Uses

On July 29, 2024, the U.S. FDA approved Alpha Cognition's oral extended-release drug Zunveyl (benzgalantamine) for the treatment of mild-to-moderate Alzheimer's disease (AD).
Zunveyl represents the second oral Alzheimer's therapy approved by the FDA in the past decade, following the 2014 approval of the memantine/donepezil combination.
As a prodrug of galantamine (an acetylcholinesterase inhibitor), Zunveyl remains pharmacologically inert during gastric passage, thereby minimizing the gastrointestinal side effects - including nausea, vomiting and loss of appetite - commonly associated with the parent drug.

References

[1] CHARLOTTE BAKKER. Safety, pharmacokinetics, and pharmacodynamics of Gln-1062, a prodrug of galantamine[J]. Alzheimer”s and Dementia: Translational Research and Clinical Interventions, 2020, 6 1. DOI:10.1002/trc2.12093.
[2] https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/218549s000lbl.pdf
[3] https://www.fiercepharma.com/pharma/alpha-cognition-passes-commercial-threshold-fda-nod-delayed-release-alzheimers-drug
[4] Benzgalantamine (Zunveyl) for Alzheimer’s disease.[J]. Medical Letter on Drugs and Therapeutics, 2025, 67 1726: 59-60. DOI:10.58347/tml.2025.1726b.