Compared with drugs that only target GLP-1R, tirzepatide is the first new generation of weight loss and hypoglycemic drugs that simultaneously targets GLP-1R/GIPR. It has better weight loss and hypoglycemic effects than single-target drugs. This medicine is not suitable for people with type 1 diabetes, pancreatitis, or children under 18 years of age. The affinity of tirzepatide to GIPR is significantly lower than that of GIP, and its cAMP activity is roughly equivalent to that of GIP. Compared with the first-generation GLP-1R agonists, tirzepatide acts as a GLP-1/GIP dual receptor agonist, and many residues in the peptide backbone are changed to obtain GIPR activating activity.
In a 2022 study, Tirzepatide was tested in 2,539 adults with complications from obesity and a body mass index (BMI) of 30 kg/m2 or 27 kg/m2. The results showed that Tirzepatide had comparable weight loss effects to bariatric surgery.
Previous phase 3 clinical trials showed that after 72 weeks of tirzepatide treatment, subjects in the 15 mg dose group lost an average of 22.5% of their body weight. This is the first drug with an average weight loss effect of more than 20% in Phase 3 clinical trials, and it is also the best drug with the best weight loss effect to date.
Traditionally, treatments for obesity have focused on dietary and lifestyle changes, such as reducing caloric intake and increasing exercise. Clinically, the development and use of anti-obesity drugs or weight loss drugs has been highly anticipated for many years. The emergence of tirzepatide for weight loss has brought unlimited possibilities for humans to use multi-targeted agonists to combat obesity and diabetes.
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Reference
[1].Karagiannis T, Avgerinos I, Liakos A, et al. Management of type 2 diabetes with the dual GIP/GLP-1 receptor agonist tirzepatide: a systematic review and meta-analysis[J]. Diabetologia,2022,65(8):1251-1261.
