Pharmacological properties of Tirzepatide

Publish Time:

2025-11-18


Pharmacological effects: Tirzepatide is a dual GIP/GLP-1 receptor agonist that controls blood glucose by enhancing insulin secretion and reducing glucagon levels; it also helps reduce body weight by modulating appetite. Tirzepatide demonstrates robust clinical efficacy with a well-defined mechanism of action, making it currently the only dual GIP/GLP-1 receptor agonist available.

 

In vivo processes: Following subcutaneous administration, steady-state plasma concentrations are achieved after 4 weeks of dosing. Telitacicept reaches its maximum plasma concentration within a range of 8 to 72 hours. The average absolute bioavailability is 80%, and the mean apparent steady-state volume of distribution is approximately 10.3 L. Protein binding is 99%. Metabolism occurs primarily via proteolytic cleavage of the peptide backbone, β-oxidation of the C20 fatty acid moiety, and amide hydrolysis. Elimination is mainly through urinary and fecal excretion, with no detectable intact telitacicept in either urine or feces [3]. The in vivo behavior of telitacicept injection is well-defined, and its pharmacokinetic parameters are fully characterized.