BPN14770 (Tetra Discovery Partners), an investigational drug that may improve memory, is being tested in a phase I safety trial funded by the National Institute of Neurological Disorders and Stroke and the National Institute on Aging, both part of the National Institutes of Health (NIH).
The compound is a first-in-class phosphodiesterase 4D negative allosteric modulator (PDE4D-NAM). PDE4D is an enzyme that plays a role in the formation of connections between brain cells. In addition, blocking PDE4D increases the activity of cyclic adenosine monophosphate, a protein that enhances learning and memory.
Another PDE4 inhibitor, rolipram (Schering AG), has been shown to improve cognitive performance in mouse models of Alzheimer’s disease, stroke, and traumatic brain injury. Although rolipram has been effective in these studies, it is not used clinically because of serious adverse effects. BPN14770 may be a possible treatment for dementia and Alzheimer’s disease with less potential for adverse effects than rolipram, according to the NIH.
The new phase I study will test the safety and pharmacokinetics of the compound in 48 healthy volunteers. If deemed safe, the next phase of testing will examine its effects on long-term memory and other aspects of cognition.
Future research studies may evaluate the effects of BPN14770 in Alzheimer’s patients as well as in those with mild cognitive impairment.
Source: NIH; December 30, 2015.