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

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

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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