The FDA approved oral to treat symptoms of mild-to-moderate Alzheimer's disease, Alpha Cognition announced on Monday.
A prodrug of galantamine and an acetylcholinesterase inhibitor (AChEI), benzgalantamine has a dual mechanism of action designed to eliminate drug absorption in the gastrointestinal (GI) tract and potentially improve tolerability.
Galantamine was as Razadyne to treat Alzheimer's symptoms. It is available in several generic formulations and sometimes is purchased as dietary supplements.
Galantamine is thought to work by elevating acetylcholine levels in the brain to improve memory and cognitive function. Unlike the recently approved anti-amyloid drugs lecanemab (Leqembi) and donanemab (Kisunla), galantamine is not designed to modify the Alzheimer's disease course.
Due to its prodrug properties, benzgalantamine is converted into the active moiety of galantamine after it passes through the GI tract. "We have always believed in the efficacy of galantamine but have been limited in its use due to tolerability issues," said Elaine Peskind, MD, of the University of Washington School of Medicine in Seattle, in an Alpha Cognition press release. "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."
Benzgalantamine's approval was based on data from three bioavailability studies that showed its bioequivalence and tolerability versus galantamine immediate-release tablets and extended-release capsules. GI adverse events (AEs) in benzgalantamine studies were less than 2% and no insomnia was observed, Alpha Cognition said.
for benzgalantamine states that AEs reported with galantamine tablets include nausea, vomiting, diarrhea, dizziness, headache, and decreased appetite. Warnings and precautions for galantamine include serious skin reactions, cardiovascular conduction effects, and pulmonary or bladder AEs. Galantamine may interfere with the activity of anticholinergic medications.
Benzgalantamine will be available by prescription in the first quarter of 2025, Alpha Cognition said.