Tirzepatide is a novel, once weekly, dual GIP/GLP-1 receptor agonist and is under development for the treatment of type 2 diabetes (T2D) and obesity.
Tirzepatide is a dual glucose-dependent insulinotropic polypeptide-GLP-1 receptor agonist. Its structure is primarily based on the glucose-dependent insulinotropic polypeptide amino acid sequence and includes a C20 fatty diacid moiety. Its half-life of approximately 5 days allows once-weekly subcutaneous administration. A phase 2b trial involving patients with type 2 diabetes showed that those who received tirzepatide had dose-dependent reductions in the glycated hemoglobin level and weight at 26 weeks.
Once-weekly injectable semaglutide, a selective GLP-1 receptor agonist, is approved for the treatment of type 2 diabetes at doses up to 1 mg. In trials involving patients who received semaglutide, the mean reductions in the glycated hemoglobin level have been reported to be as high as 1.8 percentage points and the mean reductions in body weight have been reported to be as high as 6.5 kg.
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