Tirzepatide — a dual GIP/GLP-1 receptor agonist — a new antidiabetic drug with potential metabolic activity in the treatment of type 2 diabetes

May 20, 2022Endokrynologia Polska

Tirzepatide, a new diabetes drug targeting two hormone receptors, with potential to improve metabolism in type 2 diabetes

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Abstract

Tirzepatide may reduce glycaemic levels and improve lipid metabolism in patients with type 2 diabetes mellitus.

Incretin hormones GLP-1 and GIP account for up to 65% of insulin secretion after meals.
Tirzepatide is a synthetic peptide designed to target both GIP and GLP-1 receptors.
This drug demonstrates dose-dependent effects on body weight and glycaemic control.
Tirzepatide could enhance insulin sensitivity in individuals with type 2 diabetes.
Weekly subcutaneous injections of tirzepatide may provide a novel treatment option for T2DM and related cardiometabolic issues.

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The incretin hormones glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are responsible for up to 65% of postprandial insulin secretion. Tirzepatide, developed by Eli Lilly, is a dual GIP/GLP-1 receptor agonist in the form of a synthetic linear peptide; its acylation technology allows it to bind to albumin, thus making it possible to dose the drug once a week. This review summarizes the key characteristics and pharmacokinetics of tirzepatide. The authors present the results of a phase 1, 2, and 3 clinical trial on the effects of tirzepatide on glycaemic and lipid control and the beneficial effects on body weight in a dose-dependent manner in patients with type 2 diabetes mellitus (T2DM). Tirzepatide has the ability to reduce glycaemic levels, improve insulin sensitivity, reduce body weight, and improve lipid metabolism, which is critically important in T2DM. Tirzepatide administered by weekly subcutaneous injections appears to be a promising drug for the treatment of T2DM as well as cardiometabolic disorders. The mechanism of action and safety profile of tirzepatide potentially fills important gaps in the current treatment of T2DM.

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Tirzepatide — a dual GIP/GLP-1 receptor agonist — a new antidiabetic drug with potential metabolic activity in the treatment of type 2 diabetes

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