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Tirzepatide

Metabolic & Weight
MounjaroZepboundLY3298176

Overview

Tirzepatide, also known as Mounjaro, Zepbound, and LY3298176, is a novel synthetic peptide-based compound developed by Eli Lilly and Company. It is a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. The compound is synthesized through recombinant DNA technology, resulting in a molecule that combines the properties of both incretin hormones. Tirzepatide is designed to mimic the natural incretin hormones that play a role in glucose regulation and energy balance. Researchers have primarily investigated tirzepatide in the context of metabolic disorders, including type 2 diabetes and obesity. Clinical trials have demonstrated its efficacy in improving glycemic control and promoting weight loss in patients with type 2 diabetes. Additionally, studies have shown that tirzepatide can reduce cardiovascular risk factors, such as blood pressure and lipid levels. The mechanism of action of tirzepatide involves the activation of both GIP and GLP-1 receptors. This dual agonism enhances insulin secretion, suppresses glucagon release, and slows gastric emptying, leading to improved glucose homeostasis and reduced appetite. The pharmacokinetic profile of tirzepatide reveals a half-life of approximately 5 days when administered subcutaneously, allowing for once-weekly dosing. It exhibits high stability and bioavailability when delivered via this route. Current research on tirzepatide is focused on its long-term effects and potential applications in other metabolic conditions. It has received regulatory approval for the treatment of type 2 diabetes in several countries, with ongoing studies exploring its use in obesity management. The compound is not yet approved for use in all regions, and its regulatory status may vary globally.

Mechanism of Action

Tirzepatide acts as a dual agonist of the GIP and GLP-1 receptors, which are involved in the regulation of insulin secretion and appetite. By activating these receptors, tirzepatide enhances insulin release, reduces glucagon levels, and slows gastric emptying, contributing to improved glycemic control and weight loss.

Molecular Data

FormulaC225H348N48O68
Molecular Weight4813 g/mol
CAS Number2023788-19-2
PubChem CID166567236

Half-Life

Subcutaneous~5 days
IntravenousNot applicable
IntranasalNot applicable
OralPoor bioavailability

The long half-life supports once-weekly dosing for subcutaneous administration.

Storage

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Solubility

Tirzepatide is soluble in water and exhibits limited solubility in organic solvents such as acetonitrile and DMSO.

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Approved by the FDA for the treatment of type 2 diabetes. Not a controlled substance.

🇦🇺AU

Approved by the TGA for the treatment of type 2 diabetes.

🇬🇧UK

Approved by the MHRA for the treatment of type 2 diabetes.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

9 Research Publications

Tirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis.

Human

The New England journal of medicine · 2024

Researchers studied the effects of tirzepatide on a liver disease called metabolic dysfunction-associated steatohepatitis (MASH) in patients with moderate to severe fibrosis. They found that tirzepatide significantly improved the resolution of MASH and reduced liver fibrosis compared to a placebo over 52 weeks.

  • 44% of participants taking 5 mg of tirzepatide saw resolution of MASH without worsening fibrosis, compared to 10% in the placebo group.
  • 62% of participants taking 15 mg of tirzepatide achieved the same resolution, showing a significant benefit over placebo.
  • The most common side effects reported were mild to moderate gastrointestinal issues.
PubMed

Tirzepatide: A Review in Type 2 Diabetes.

Review

Drugs · 2024

Researchers reviewed the effectiveness of tirzepatide (Mounjaro) for managing type 2 diabetes. They found that many people with this condition struggle to meet their blood sugar and weight goals with existing treatments, highlighting the potential of tirzepatide as a promising option.

  • Researchers observed that tirzepatide may offer better blood sugar control compared to current diabetes medications.
  • The study noted that participants using tirzepatide experienced significant weight loss.
  • Researchers highlighted the need for more effective treatments for individuals who do not achieve their diabetes management goals.
PubMed

Continued Treatment With Tirzepatide for Maintenance of Weight Reduction in Adults With Obesity: The SURMOUNT-4 Randomized Clinical Trial.

Human

JAMA · 2024

Researchers studied the effects of tirzepatide on maintaining weight loss in adults with obesity. They found that participants who continued tirzepatide treatment maintained significantly more weight loss compared to those who switched to a placebo, with many participants keeping most of their weight off over the year.

  • Participants who continued tirzepatide maintained an average weight loss of 25.3% over 88 weeks, compared to 9.9% for those on placebo.
  • 89.5% of participants on tirzepatide maintained at least 80% of their weight loss, while only 16.6% of those on placebo did.
  • The most common side effects were mild to moderate gastrointestinal issues, more frequent in the tirzepatide group.
PubMed

Comparison of tirzepatide and dulaglutide on major adverse cardiovascular events in participants with type 2 diabetes and atherosclerotic cardiovascular disease: SURPASS-CVOT design and baseline characteristics.

Human

American heart journal · 2024

Researchers studied the effects of tirzepatide, a new diabetes medication, on heart health in people with type 2 diabetes and existing heart disease. This research involved over 13,000 participants and aims to compare the cardiovascular safety and effectiveness of tirzepatide with another diabetes medication called dulaglutide.

  • The study included participants aged 40 and older with type 2 diabetes and a history of heart disease.
  • Researchers observed that the average participant was 64 years old and had been living with diabetes for nearly 15 years.
  • The trial aims to provide conclusive evidence regarding the cardiovascular safety of tirzepatide compared to dulaglutide.
PubMed

New Drug: Tirzepatide (Mounjaro

Human

The Senior care pharmacist · 2023

Researchers studied a new drug called tirzepatide (Mounjaro) for managing type 2 diabetes, which affects millions of Americans. They found that tirzepatide effectively lowers blood sugar levels and promotes weight loss, with side effects similar to existing treatments.

  • Researchers observed that tirzepatide significantly lowers blood glucose levels in patients with type 2 diabetes.
  • The study found that tirzepatide also leads to notable weight loss among participants.
  • Adverse effects of tirzepatide were comparable to those of other GLP-1 receptor agonists.
PubMed

Tirzepatide: A Systematic Update.

Review

International journal of molecular sciences · 2022

Researchers observed that Tirzepatide, a new medication, effectively controls blood sugar levels by targeting specific hormones that stimulate insulin release. The study highlighted its additional benefits, including improved blood pressure and reduced cholesterol levels. Tirzepatide has recently been approved for use in diabetes management, with ongoing research exploring its potential in other health areas.

  • Tirzepatide combines the effects of two hormones to help regulate blood sugar levels.
  • The medication has shown positive effects on blood pressure and cholesterol levels.
  • It has been approved for diabetes treatment and is being studied for other potential health applications.
PubMed

Effect of Subcutaneous Tirzepatide vs Placebo Added to Titrated Insulin Glargine on Glycemic Control in Patients With Type 2 Diabetes: The SURPASS-5 Randomized Clinical Trial.

Human

JAMA · 2022

Researchers found that adding tirzepatide to insulin glargine significantly improved blood sugar control in adults with type 2 diabetes who were not adequately managing their condition. After 40 weeks, participants receiving tirzepatide experienced greater reductions in blood sugar levels and weight compared to those receiving a placebo.

  • Participants using tirzepatide had an average decrease in blood sugar levels of up to 2.4% compared to 0.9% in the placebo group.
  • Those treated with tirzepatide lost between 5.4 kg and 8.8 kg, while the placebo group gained 1.6 kg.
  • A higher percentage of patients on tirzepatide achieved target blood sugar levels of less than 7% compared to those on placebo.
PubMed

Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes.

Human

The New England journal of medicine · 2021

Researchers found that tirzepatide, a new medication for type 2 diabetes, was more effective than semaglutide in lowering blood sugar levels over 40 weeks. The study involved nearly 1,900 participants and showed that tirzepatide also led to greater weight loss compared to semaglutide. Both medications had similar side effects, primarily mild gastrointestinal issues.

  • Tirzepatide significantly reduced blood sugar levels more than semaglutide.
  • Participants taking tirzepatide experienced greater weight loss compared to those on semaglutide.
  • The most common side effects for both medications were mild to moderate gastrointestinal issues.
PubMed

Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial.

Human

Lancet (London, England) · 2021

Researchers studied the effects of a new medication called tirzepatide on adults with type 2 diabetes who were not achieving control through diet and exercise alone. They found that tirzepatide significantly improved blood sugar levels and reduced body weight without increasing the risk of low blood sugar.

  • Tirzepatide led to significant improvements in blood sugar control compared to a placebo.
  • Participants experienced notable weight loss while using tirzepatide.
  • The safety profile of tirzepatide was similar to existing GLP-1 receptor agonists, suggesting it could be a viable treatment option.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.