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Discovery of MK-1462: GLP-1 and Glucagon Receptor Dual Agonist for the Treatment of Obesity and Diabetes

Cover of ACS Med Chem Letters Journal, Aug 2022, which features Discovery by IRBM

The IRBM peptide chemistry team is proud to announce a new publication in ACS Medicinal Chemistry Letters in collaboration with the outstanding drug discovery team at Merck & Co. (Kenilworth, NJ).
Concomitant activation of GLP1R and the glucagon receptor (GCGR) has been reported by Merck & Co and other groups to improve glucose metabolism and provide superior weight loss when compared to GLP1R agonism in preclinical species.

This study highlights chemistry structure−activity relationship optimization and summarizes in vivo efficacy studies toward the discovery of a once daily, balanced, dual GLP1R/GCGR peptide agonist -MK-1462.
Based on the overall preclinical characteristics including potency, selectivity, PK, in vivo efficacy, and safety, MK-1462 was nominated as a development candidate and has advanced into the clinic.

The details of this successful drug discovery collaboration can be found at the link

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