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MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate.

ABSTRACT: Identification of ligands that selectively activate the M1 muscarinic signaling pathway has been sought for decades to treat a range of neurological and cognitive disorders. Herein, we describe the optimization efforts focused on addressing key physicochemical and safety properties, ultimately leading to the clinical candidate MK-7622, a highly selective positive allosteric modulator of the M1 muscarinic receptor that has entered Phase II studies in patients with Alzheimer's disease.

SUBMITTER: Beshore DC 

PROVIDER: S-EPMC6047034 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature

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Identification of ligands that selectively activate the M<sub>1</sub> muscarinic signaling pathway has been sought for decades to treat a range of neurological and cognitive disorders. Herein, we describe the optimization efforts focused on addressing key physicochemical and safety properties, ultimately leading to the clinical candidate MK-7622, a highly selective positive allosteric modulator of the M<sub>1</sub> muscarinic receptor that has entered Phase II studies in patients with Alzheimer'  ...[more]

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