MK-7622: A First-in-Class M 1 Positive Allosteric Modulator Development Candidate

Identification of ligands that selectively activate the M 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 leadin...

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Published inACS medicinal chemistry letters Vol. 9; no. 7; pp. 652 - 656
Main Authors Beshore, Douglas C, N Di Marco, Christina, Chang, Ronald K, Greshock, Thomas J, Ma, Lei, Wittmann, Marion, Seager, Matthew A, Koeplinger, Kenneth A, Thompson, Charles D, Fuerst, Joy, Hartman, George D, Bilodeau, Mark T, Ray, William J, Kuduk, Scott D
Format Journal Article
LanguageEnglish
Published United States 12.07.2018
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Summary:Identification of ligands that selectively activate the M 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 muscarinic receptor that has entered Phase II studies in patients with Alzheimer's disease.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.8b00095