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Innovative Medicines & Omics                                       Incretin mimetics in diabetes management



            4.6. Tirzepatide                                   resulting in a balanced dual agonist. Tirzepatide exhibits

            Tirzepatide (Figure 7) acts as a dual agonist, targeting both   comparable affinity for the GIP receptor to native GIP
            the GIP and GLP-1 receptors. It is marketed as Mounjaro   but binds to the GLP-1 receptor with about 5 times lower
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            for adults with T2DM to improve glycemic control and   affinity than native GLP-1.  This higher GIP receptor
            as Zepbound for overweight adults with weight-related   activity relative to GLP-1 receptor activity contributes to
            comorbidities (T2DM, hypertension, and dyslipidemia).   its dose-dependent reduction in HbA1c.
            By targeting multiple receptors, tirzepatide enhances   Mounjaro simultaneously targets the GIP and GLP-1
            insulin secretion and reduces glucagon levels, contributing   receptors, promoting insulin secretion and inhibiting
            to improved blood glucose management. In addition, it   glucagon release in a glucose-dependent manner. This
            aids in weight loss, which benefits individuals with obesity-  mechanism improves blood glucose control and reduces
            related health issues. The development of tirzepatide   post-meal glucose spikes. Treatment typically begins at
            involved introducing GLP-1 activity into the GIP sequence,   a dose of 2.5 mg once weekly for the first 4 weeks, after

























































                                               Figure 7. Chemical structure of tirzepatide
                                     Notes: Pink: C20 fatty acid diacidic moiety. Reproduced from Al Musaimi 12


            Volume 2 Issue 1 (2025)                         10                               doi: 10.36922/imo.4911
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