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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

