Tirzepatide (Mounjaro/Zepbound)

Overview
Mechanism of Action: Tirzepatide is a dual GIP (Glucose-dependent Insulinotropic Polypeptide) and GLP-1 (Glucagon-Like Peptide-1) receptor agonist. This means it acts on both the GIP and GLP-1 receptors, which are involved in insulin secretion and appetite regulation. By stimulating these receptors, tirzepatide enhances insulin secretion in response to meals, suppresses glucagon secretion, and slows gastric emptying, which can lead to reduced appetite and caloric intake.
Use in Diabetes Treatment: Tirzepatide is primarily used for the management of type 2 diabetes. It has been shown to effectively lower blood glucose levels and also contribute to significant weight loss in patients. Its dual action on GIP and GLP-1 receptors is thought to contribute to its effectiveness in controlling blood sugar levels.
Administration: Tirzepatide is administered through subcutaneous injection. The dosing frequency can vary depending on the formulation and the patient’s treatment plan.
Clinical Trials and Efficacy: Clinical trials have demonstrated that tirzepatide is effective in lowering HbA1c (a measure of blood sugar control over time) and aiding weight loss. It has been compared favorably with other GLP-1 receptor agonists and has shown significant benefits in terms of both glycemic control and weight reduction.
Side Effects: Common side effects of tirzepatide may include gastrointestinal symptoms such as nausea, diarrhea, reduced appetite, and vomiting. As with all medications, it’s essential for individuals to be aware of potential side effects and discuss them with their healthcare provider.
Approval and Availability: Tirzepatide had received regulatory approval in several regions, including the United States, for the treatment of type 2 diabetes. Its availability and specific indications can vary by region.
Potential for Weight Management: Given its significant effects on weight, tirzepatide is also being explored for use in weight management, similar to some GLP-1 receptor agonists like semaglutide.
Lilly is ramping up production - Big Time
Eli Lilly and Company is significantly investing in the manufacturing of tirzepatide. The company has announced plans to construct a new high-tech manufacturing site in Alzey, Rhineland-Palatinate, Germany, with an investment of $2.5 billion. This facility is intended to expand Lilly’s global parenteral (injectable) product and device manufacturing network, supporting increased demand for its medicines, including those for diabetes and obesity.
Additionally, Lilly has invested over $11 billion in its global manufacturing footprint over the past three years. This investment aims to ensure the safe and reliable supply of Lilly’s innovative medicines, addressing growth expected from potential new medicines to treat diabetes, obesity, Alzheimer’s disease, cancer, and autoimmune conditions.
Furthermore, the company plans to invest an additional $450 million to expand the capacity of a plant in North Carolina, U.S. This expansion is part of its efforts to boost production ahead of an expected increase in demand.
RECENT PAPERS from PubMed – November 11, 2023 – Tirzepatide and Cancer
- Survival Benefits of GLP-1 Receptor Agonists in Patients with Neuroendocrine Neoplasms: A Large-Scale Propensity-Matched Cohort Study May 14, 2025Background: Neuroendocrine neoplasms (NENs) represent a heterogeneous group of malignancies that consist of two major subtypes: neuroendocrine tumors (NETs) and neuroendocrine carcinomas (NECs). Glucagon-like peptide-1 receptor agonists (GLP-1Ra) have demonstrated favorable results in preclinical studies, but their impact on NEN outcomes remains unexplored. Methods: Using the TriNetX US Research Network, we identified adult patients with […]Manal S Fawzy
- Metformin use in prediabetes: A review of evidence and a focus on metabolic features among peri-menopausal women May 7, 2025The prevalence of prediabetes has more than doubled over the past two decades. Although hormones associated with the menstrual cycle may offer some protection against diabetes by enhancing insulin sensitivity and suppressing gluconeogenesis, the prevalence of diabetes among women remains high at 10.5%. Notably, among the perimenopausal population, the prevalence catches up to-and even surpasses-that […]Beth Shi Yu Lim
- The Potential Role of GLP1-RAs Against Anticancer-Drug Cardiotoxicity: A Scoping Review April 26, 2025Background: GLP1 receptor agonists (GLP1-RAs) have become a central component in the treatment of type 2 diabetes mellitus (T2DM) and are gaining prominence in the cardiovascular field. Semaglutide and other GLP1-RA molecules possess cardioprotective properties. Cardiotoxicity, a term used to refer to cardiovascular disease caused by anticancer treatment, is a collection of common and severe […]Filippo Biondi
- National trends in prescription drug expenditures and projections for 2025 April 22, 2025CONCLUSION: For 2025, we expect overall prescription drug spending to rise by 9.0 to 11.0%, whereas in clinics and hospitals we anticipate an 11.0% to 13.0% increase and a 2.0% to 4.0% increase, respectively, compared to 2024. These national estimates of future pharmaceutical expenditure growth may not be representative of any health system because of […]Eric M Tichy
- Real-world evidence on the utilization, clinical and comparative effectiveness, and adverse effects of newer GLP-1RA-based weight-loss therapies April 8, 2025Glucagon-like peptide-1 receptor agonists (GLP-1RAs) have emerged as key agents for weight management, based on their marked efficacy as observed in randomized controlled trials. While still limited, real-world studies on GLP-1RA use in populations with obesity are increasingly available. This narrative review discusses contemporary real-world evidence demonstrating the utilization, clinical and comparative effectiveness, and adverse […]Reimar W Thomsen
- Tirzepatide in the NHS: The known unknowns of treating obesity at a national scale April 8, 2025No abstractAshley Kieran Clift
- In adults with HF with preserved ejection fraction and obesity, tirzepatide reduced a composite of CV death or worsening HF at 2 y March 31, 2025GIM/FP/GP: [Formula: see text] Cardiology: [Formula: see text] Endocrinology: [Formula: see text].Leslie A Ynalvez
- The Novel Dual GIP and GLP-1 Receptor Agonist Tirzepatide Attenuates Colon Cancer Development by Regulating Glucose Metabolism March 24, 2025Colorectal cancer (CRC) is a leading cause of cancer mortality while diabetes is a recognized risk factor for CRC. Here we report that tirzepatide (TZP), a novel polypeptide/glucagon-like peptide 1 receptor (GIPR/GLP-1R) agonist for the treatment of diabetes, has a role in attenuating CRC growth. TZP significantly inhibited colon cancer cell proliferation promoted apoptosis in […]Yikai Zhang
- Exploring Connections Between Weight-Loss Medications and Thyroid Cancer: A Look at the FDA Adverse Event Reporting System Database March 8, 2025CONCLUSION: The study, based on data from the FAERS database, suggests a potential association between GLP-1 receptor agonists and an increased thyroid cancer risk. These findings underscore the importance of further research and continuous safety monitoring when prescribing these medications for obesity management.Christophe Abi Zeid Daou
- Glucagon-like peptide-1 receptor agonists: a new pharmacological treatment option for psychiatric illnesses? March 5, 2025Albiglutide, dulaglutide, exenatide, liraglutide, lixisenatide, orforglipron and semaglutide are glucagon-like peptide‑1 (GLP-1) receptor agonists. Tirzepatide targets not only GLP‑1 but also glucose-dependent insulinotropic peptide (GIP) receptors and retatrutide is a triple GLP‑1, GIP and glucagon receptor agonist. The GLP‑1 receptor agonists increase insulin release but suppress glucagon release. They slow down the emptying of the […]Hubertus Himmerich
- Regional trends and disparities in newer GLP1 receptor agonist initiation among real-world adult patients eligible for obesity treatment March 4, 2025CONCLUSIONS: The initiation of newer AOMs among overweight and obese populations remains low, but uptake has increased exponentially since 2022. Our findings reveal significant disparities in obesity care, highlighting the importance of addressing inequities in AOM access to improve obesity outcomes.Rotana M Radwan
- Tirzepatide alleviates doxorubicin-induced cardiotoxicity via inhibiting HRD1-mediated Nrf2 ubiquitination March 4, 2025CONCLUSIONS: Our study suggested that TZP attenuated oxidative stress and cardiomyocyte apoptosis by modulating HRD1-mediated Nrf2 expression and activity, thereby protecting against the cardiotoxic effects exerted by DOX. These results supported that TZP might be a promising therapeutic option for reducing chemotherapy-related cardiotoxicity.Dan Yang
- Treatment of obesity: will incretin agonists make bariatric surgery a thing of the past? February 21, 2025The prevalence of obesity continues to increase worldwide. Obesity is associated with an increased risk of cardiometabolic and other diseases, reduced quality of life and shortened life expectancy. Highly effective therapies are required to achieve meaningful and sustained weight reduction to prevent, slow or reverse disease associated with obesity. Bariatric surgery is a highly effective […]Siehoon Lah
- Renal effects and safety of tirzepatide in subjects with and without diabetes: A systematic review and meta-analysis February 17, 2025CONCLUSION: Short-term data from RCTs with low RoB suggests that tirzepatide positively impacts UACR without detrimental effects on eGFR in subjects with T2D and obesity without T2D, with a reassuring renal safety profile. Larger RCTs are warranted to prove the longer-term renal benefits of tirzepatide, which might also prevent eGFR decline and worsening of CKD.Abm Kamrul-Hasan
- Nutrient-Stimulating Hormone-Based Therapies for Obesity February 7, 2025Obesity is a chronic disease with an increasing worldwide prevalence. Improving obesity is of paramount importance given its association with conditions such as type 2 diabetes, cardiovascular disease, and cancer among others. In the last decade, a new class of highly efficacious medications called nutrient-stimulating hormone (NuSH) therapies has emerged. This article highlights the effectiveness […]Cagney Cristancho
- Appendicitis After Initiation of Tirzepatide February 5, 2025Tirzepatide is a GLP1/GIP receptor agonist that is used to treat type 2 diabetes and promote weight loss. Common side effects of Tirzepatide include nausea, vomiting, and diarrhea. More severe side effects include pancreatitis, cholelithiasis, thyroid cancer, and cholecystitis. With the increased use of these medications, additional side effects are being discovered. Delayed gastric emptying […]Garrett Chan
- Association of long-term weight management pharmacotherapy with multiple health outcomes: an umbrella review and evidence map January 26, 2025CONCLUSIONS: This umbrella review identified significant beneficial associations between pharmacotherapies and anthropometric measures, lipid profile, blood pressure, glycemic profile, and quality-of-life outcomes in individuals with overweight or obesity. In addition, the umbrella review highlighted safety considerations. The findings affirm the efficacy of the six pharmacotherapies in promoting weight loss in this demographic. Further clinical trials […]Ting-Ting Lu
- Tirzepatide and Cancer Risk in Individuals with and without Diabetes: A Systematic Review and Meta-Analysis January 15, 2025CONCLUSION: Tirzepatide use in RCTs over 26 to 72 weeks did not increase overall or specific cancer risk.A B M Kamrul-Hasan
- Adropin/Tirzepatide Combination Mitigates Cardiac Metabolic Aberrations in a Rat Model of Polycystic Ovarian Syndrome, Implicating the Role of the AKT/GSK3beta/NF-kappaB/NLRP3 Pathway January 11, 2025Polycystic ovarian syndrome (PCOS) is a multifaceted metabolic and hormonal disorder in females of reproductive age, frequently associated with cardiac disturbances. This research aimed to explore the protective potential of adropin and/or tirzepatide (Tirze) on cardiometabolic aberrations in the letrozole-induced PCOS model. Female Wistar non-pregnant rats were allotted into five groups: CON; PCOS; PCOS + […]Islam Ibrahim Hegab
- Exploring the molecular mechanisms of tirzepatide in alleviating metabolic dysfunction-associated fatty liver in mice through integration of metabolomics, lipidomics, and proteomics January 10, 2025Clinical studies have suggested that tirzepatide may also possess hepatoprotective effects; however, the molecular mechanisms underlying this association remain unclear. In our study, we performed biochemical analyses of serum and histopathological examinations of liver tissue in mice. To preliminarily explore the molecular mechanisms of tirzepatide on metabolic dysfunction-associated fatty liver disease (MAFLD), liquid chromatography-mass spectrometry […]Jinliang Liang