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Pirepemat is a small molecule drug under development for the prevention of falls in people with Parkinson's disease and Parkinson's disease dementia. It acts as an antagonist at serotonin 5-HT7 receptor and alpha-2 adrenergic receptor, with additional affinity for several other neurotransmitter receptors and transporters including sigma σ1 receptor, serotonin transporter (SERT), α2C-adrenergic receptor, α2A-adrenergic receptor, serotonin 5-HT2C receptor, serotonin 5-HT2A receptor, norepinephrine transporter (NET), κ-opioid receptor (KOR), and weakly at α1-adrenergic receptor. Pirepemat is described as a "cortical enhancer," increasing norepinephrine, dopamine, and acetylcholine levels in the cerebral cortex by antagonizing these targets. Its primary clinical focus is to improve balance and reduce falls in patients with Parkinson’s disease by strengthening nerve cell signaling in the prefrontal cortex. The drug has completed Phase I studies showing good tolerability and has advanced through Phase IIa/IIb trials demonstrating potential benefits on balance, cognitive function, postural dysfunction, psychiatric symptoms of Parkinson’s disease as well as reduced fall frequency[1][3][4][6].
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