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molecules of the month

emraclidine

M4 positive allosteric modulator

Ph. II for schizophrenia

discovery not disclosed

Lancet, December 17, 2022

Cerevel Therapeutics, Cambridge, MA

emraclidine chemical structure mAChR positive allosteric modulator - Cerevel Therapeutics, Cambridge, MA
5 mins read

What is it? Emraclidine (CVL-231) is a selective positive allosteric modulator (PAM) of the cholinergic M4 muscarinic receptor (GCPR) and is the only selective M4 PAM in clinical development. The molecule was highlighted by Cerevel at JPM ‘23 as it has shown promising early results in schizophrenia with several Ph. II trials enrolling (NCT05443724, NCT05227703, NCT05227690), and is starting elderly healthy volunteer studies to support development in Alzheimer’s Disease psychosis (ADP) at 2-30 mg QD. The molecule demonstrates high brain penetration and target engagement based on PET studies in rhesus macaques using an M4 PAM radioligand ([11C]MK-6884). Why do we care? Schizophrenia affects an estimated 24 million people worldwide. For decades, treatments focused on modulating D2 dopamine receptors which are…


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