Tirzepatide is a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP, also known as: gastric inhibitory peptide) receptor and glucagon-like peptide-1 (GLP-1) receptor. Both GIP and GLP-1 are hormones secreted by the intestine and can promote insulin secretion. Tirzepatide combines two insulinotropic effects into a single molecule and represents a new class of drugs for the treatment of type 2 diabetes.

Tirzepatide (tirzepatide) is an innovative once-weekly glucose-dependent glucagon polypeptide (GIP)/glucagon-like peptide-1 (GLP-1) receptor agonist that selectively binds to and agonizes two natural enteroglucagon receptors, the GIP receptor and the GLP-1 receptor, to lower fasting and postprandial blood glucose levels in patients with type 2 diabetes mellitus (T2D). 2024On May 21, 2024, the drug was approved by the China National Drug Administration (NMPA) for adult T2D patients with poor glycemic control despite treatment with metformin and/or sulfonylureas based on dietary control and exercise.

The registration application for tirzepatide for the indication of long-term weight management in adults was based on the results of 26 clinical studies with tirzepatide, including the Chinese obese or overweight registry clinical trial SURmount-CN, which showed that at 52 weeks of treatment, the mean percentage change from baseline in body weight in the tirzepatide 10mg and 15mg treatment groups was -14.4% and -14.4%, respectively.were -14.4% and -19.9%, respectively, which was superior to the placebo group (-2.4%), and the proportion of patients achieving ≥5% weight loss was better in the tirzepatide group (10 mg, 91.4%; 15 mg, 92.7%) than in the placebo group (29.4%).In addition, the proportion of patients achieving ≥15% weight loss was also better in the tirzepatide group (10 mg, 48.6%; 15 mg, 72.1%) than in the placebo group (2.9%).

The overall safety profile of Tirzepatide is similar to that of known GLP-1 receptor agonists, with the most common adverse reactions being mild to moderate gastrointestinal adverse reactions, occurring primarily during dose-escalation periods, decreasing with continued administration, and tolerated and adhered to by the vast majority of patients.

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