I. Drug Overview
Tirzepatide (also known as Ticagrelor) is a novel hypoglycemic and weight loss drug.
As the world’s first and only approved dual receptor agonist of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1), Tirzepatide integrates the effects of two incretin hormones into a single molecule, representing a significant breakthrough in the treatment of type 2 diabetes and obesity. Since its initial approval for marketing in the United States in 2022, the drug has gained widespread recognition in multiple major markets globally.
II. Mechanism of Action
2.1 Introduction to GIP and GLP-1 Both GIP and GLP-1 are incretin hormones secreted by the human gut, released after eating, and capable of promoting insulin secretion and helping maintain blood glucose homeostasis. Each has unique functions in regulating energy metabolism: GLP-1 primarily acts by delaying gastric emptying, enhancing satiety, and suppressing appetite; while GIP plays a significant role in regulating fat metabolism and promoting insulin sensitivity.
2.2 Unique Advantages of Dual Receptor Agonists The breakthrough of teirapotide lies in its ability to simultaneously activate both GIP and GLP-1 receptors, integrating the insulinotropic effects of both into a single molecule. Clinical studies have shown that teirapotide exhibits the following multiple effects:
Potent hypoglycemic effect: Significantly reduces glycosylated hemoglobin (HbA1c) levels, with a maximum reduction of 2.19% in Chinese patients;
Significant weight loss: By increasing satiety, suppressing appetite, and increasing energy expenditure, it brings about excellent weight loss effects;
Improve insulin sensitivity: directly improve β-cell function and insulin resistance independent of weight loss;
Cardiovascular protection: It possesses anti-inflammatory activity and can improve blood pressure and lipid metabolism;
Improving non-alcoholic fatty liver disease/metabolically related steatohepatitis: having a positive impact on liver histology.
Tilboposide can also prevent the rapid degradation of dipeptidyl peptidase-4 (DPP-4), thereby maintaining a longer half-life in the body and facilitating once-weekly administration.
III. Clinical Efficacy Data
3.1 Hypoglycemic Efficacy The hypoglycemic effect of tiraglutide has been fully validated in multiple large-scale phase 3 clinical trials.
Key Data of Chinese Patients (SURPASS-CN-MONO Study)
SURPASS-CN-MONO is a randomized, double-blind, placebo-controlled study evaluating the efficacy and safety of tepatide monotherapy in Chinese adult patients with type 2 diabetes. At week 40, patients in the tepatide 5mg, 10mg, and 15mg groups showed HbA1c reductions of 2.19%, 1.75%, and 2.03% from baseline, respectively, while the placebo group only experienced a reduction of 0.77%. The proportions of patients achieving glycemic control (HbA1c < 7.0%) at week 40 were as high as 90.38%, 86.36%, and 83.33% in the test groups, respectively, compared to only 38.30% in the placebo group.
3.2 Weight loss efficacy: Tepidopeptide demonstrates superior efficacy in weight management.
SURMOUNT-1 study (3-year follow-up)
SURMOUNT-1 is a multicenter, randomized, double-blind, placebo-controlled Phase 3 clinical trial evaluating the efficacy of tiraglutide (5mg, 10mg, and 15mg) in weight management for overweight or obese adults. As of Week 176:
The 15mg dose group achieved an average weight loss of 22.9%, the 10mg group achieved a weight loss of 19.9%, the 5mg group achieved a weight loss of 15.4%, while the placebo group only experienced a weight loss of 2.1%;
Compared with placebo, teplizumab reduced the risk of prediabetic adults progressing to type 2 diabetes by 94% (hazard ratio 0.06);
During the 176-week treatment period, nearly 99% of patients treated with tiraglutide did not develop type 2 diabetes;
The research results were published in the New England Journal of Medicine (NEJM) and presented at the Obesity Week 2024 conference.
SURMOUNT-2 study (patients with type 2 diabetes)
In two randomized, double-blind, placebo-controlled trials approved by the FDA for weight loss, Zepbound achieved a statistically significant weight loss compared to the placebo group after 72 weeks. Among non-diabetic adults, the highest approved dose of 15mg group achieved an average weight loss of 18%; among adults with type 2 diabetes, the highest approved dose of 15mg group achieved an average weight loss of 12%.
3.3 Diabetes Prevention Teelpeptide exhibits particularly outstanding performance in the prevention of diabetes. The aforementioned subgroup analysis of the SURMOUNT-1 trial on prediabetes showed that the teelpeptide treatment group had a 94% reduced risk of diabetes progression, preventing one new case of diabetes for every nine patients treated. Even after 17 weeks of drug withdrawal, the risk of diabetes progression was still 88% lower than that of the placebo group.
3.4 Cardiometabolic Benefits: Teelpeptide treatment is significantly associated with improvements in multiple cardiometabolic risk factors, including decreased blood pressure, improved lipid profile, and reduced fasting insulin levels, which persist over a period of 176 weeks. Mediation analysis indicates that approximately half of the diabetes prevention effect is attributed to drug-mediated weight loss, with the remaining benefits attributed to other non-weight-dependent effects of teelpeptide.
3.5 Common adverse reactions: gastrointestinal events
The most common side effects of tilbopide are gastrointestinal-related adverse reactions, which are usually mild to moderate:
Nausea, diarrhea, and constipation are the most common symptoms, and some patients may also experience vomiting and abdominal pain;
In the combined analysis of SURMOUNT-1 and SURMOUNT-2, the incidence of severe gastrointestinal adverse reactions in the Zepbound group was as follows: 1.7% in the 5mg group, 2.5% in the 10mg group, and 3.1% in the 15mg group, which was higher than that in the placebo group (1.0%);
Not recommended for patients with severe gastroparesis.
Serious adverse reaction
Severe hypersensitivity reactions: including anaphylactic shock and angioedema, which have been reported;
Acute kidney injury: It primarily occurs in patients who experience dehydration due to gastrointestinal adverse reactions. Monitoring of renal function is particularly necessary during the initiation and titration of medication;
Acute gallbladder disease: Both Ticagrelor and GLP-1 receptor agonists are associated with an increased incidence of acute gallbladder disease.
3.6 Contraindications: Terbinafine is contraindicated for the following populations:
Individuals with a personal or family history of medullary thyroid cancer;
Individuals with type 2 multiple endocrine neoplasia syndrome;
Individuals with known severe hypersensitivity reactions to tilbopide or any of its excipients.
IV. Market Performance and Prospects
4.1 Sales Data Due to its excellent efficacy, Teicoplanin has become one of the fastest-growing drugs in the history of global pharmaceuticals:
In 2024, the hypoglycemic version of Mounjaro contributed $16.466 billion in global sales, ranking among the top 5 global pharmaceutical sales;
In 2025, the global sales of Mounjaro reached $22.965 billion (a year-on-year increase of 99%), while the sales of the weight-loss version of Zepbound amounted to $13.542 billion (a year-on-year increase of 175%). The combined sales of the two products totaled $36.507 billion;
Medicine King Laurel: Tildanepeptide, with a slight advantage of approximately $400 million, defeated Novo Nordisk’s semaglutide (approximately $36.1 billion) and Merck’s K-drug (approximately $31.68 billion), officially becoming the global drug sales champion in 2025;
In the first quarter of 2026, the single-quarter revenue of Tildalopeptide reached $12.822 billion ($8.662 billion for the hypoglycemic version + $4.16 billion for the weight loss version), accounting for 64% of Eli Lilly’s total revenue for the quarter;
Prospect forecast: It is expected that by the end of 2026, the total sales of Tildalopeptide will exceed 45 billion US dollars
V. Frequently Asked Questions (FAQ)
Q1: Is tilburide suitable for everyone?
A: No. Teplizumab is contraindicated for individuals or those with a family history of medullary thyroid cancer, those with type 2 multiple endocrine neoplasia syndrome, and those allergic to its components. Pregnant and lactating women should also avoid using it. Professional medical evaluation should be conducted before medication.
Q2: What are the common side effects of tilbopide?
A: The most common gastrointestinal adverse reactions include nausea, diarrhea, constipation, vomiting, and abdominal pain, which are usually mild to moderate. Severe hypersensitivity reactions, acute gallbladder disease, and acute kidney injury (often related to dehydration) also need to be monitored.
Q3: What is the difference between Tildanepeptide and Semaglutide?
A: Teelpeptide is a dual receptor agonist of GIP and GLP-1, while semaglutide is only a single receptor agonist of GLP-1. Clinical data shows that teelpeptide generally outperforms semaglutide in terms of blood glucose lowering and weight loss effects.
Q4: Does tilbopotide need to be used for life?
A: Both type 2 diabetes and obesity are chronic diseases. The SURMOUNT-1 study found that after 17 weeks of drug withdrawal, some patients experienced weight rebound and an increased risk of type 2 diabetes. Long-term management under the guidance of a physician is usually recommended.
