First Phase 1 Trial Participant Receives HTL0016878, Heptares’ Therapy for Cognitive Impairment in Alzheimer’s

First Phase 1 Trial Participant Receives HTL0016878, Heptares’ Therapy for Cognitive Impairment in Alzheimer’s
The first participant in a Phase 1 clinical trial of HTL0016878 as a treatment for cognitive impairment in Alzheimer’s disease is receiving the therapy, according to its developer, Heptares Therapeutics. Heptares, a subsidiary of Japan’s Sosei Group Corporation, and Ireland-based Allergan are partnering in the trial under a treatment development and commercialization agreement they announced in April 2016. HTL0016878 is an agonist, or molecule that binds to a protein receptor to active it — in this case, the muscarinic receptor subtype M4. Muscarinic receptors are in a lot of body tissue. Together with nicotinic receptors, they are part of the cholinergic system — nerve cells or fibers that use acetylcholine as a  neurotransmitter. Researchers have linked impairment of the system with Alzheimer's-related dementia. Several studies have indicated that activating the M1 and M4 muscarinic receptors in the brain may be a way to treat the cognitive decline in Alzheimer's. But scientists have had trouble developing therapies that activate the M1 and M4 muscarinic receptors without also activating the M2 and M3 receptors, whose activation would be harmful. That has led to them
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