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Tirzepatide

Mounjaro · Zepbound · LY3298176

Metabolic & WeightApproved
From$5.15/mgCompare prices
MW
4813g/mol
Formula
C225H348N48O68

Tirzepatide is a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors, developed for the management of type 2 diabetes and obesity. Researchers primarily study tirzepatide for its potential to enhance glycemic control and promote weight loss in individuals with these conditions. Key findings from clinical trials indicate that participants receiving tirzepatide experienced significant reductions in body weight, with mean changes ranging from -12.3% to -19.7%, and a markedly lower incidence of type 2 diabetes compared to placebo groups. Additionally, studies suggest that tirzepatide may improve insulin sensitivity and reduce appetite more effectively than other treatments. Current research continues to explore its mechanisms of action and long-term effects on metabolic health.

Chemical Profile

Chemical Profile

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

Half-Life

SCSubcutaneous

~5 days

IVIntravenous

Not applicable

INIntranasal

Not applicable

POOral

Poor bioavailability

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

Mechanism

Mechanism of Action

Tirzepatide acts as a dual agonist for the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor, enhancing insulin secretion and promoting weight loss through distinct signaling pathways. It preferentially activates the GIP receptor, leading to increased cAMP production, while exhibiting biased agonism at the GLP-1 receptor that favors cAMP generation over β-arrestin recruitment, thus enhancing insulin secretion without promoting receptor internalization. Although the precise mechanisms underlying its effects on appetite regulation and metabolic adaptation remain incompletely understood, tirzepatide has been shown to reduce calorie intake and increase fat oxidation.

Research

119 Research Publications

13,787

Total Citations

53

Human/RCT

21.7

Avg. Influence

2025

Latest

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#01

Tirzepatide Once Weekly for the Treatment of Obesity.

HumanInfluence398.0
2720
The study demonstrated that tirzepatide led to substantial and sustained weight reductions in humans with obesity over 72 weeks compared to placebo.
5 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)176 weeks15 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)36 weeks15 mgsubcutaneous(human)36 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)ongoing5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#02

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

Aronne Louis J, et al. · JAMA · 2024

HumanInfluence61.0
719
Researchers observed that continued tirzepatide treatment in humans with obesity maintained significant weight loss compared to those switched to placebo.

Key findings

  1. 01Participants who continued tirzepatide maintained an average weight loss of 25.3% over 88 weeks, compared to 9.9% for those on placebo.
  2. 0289.5% of participants on tirzepatide maintained at least 80% of their weight loss, while only 16.6% of those on placebo did.
  3. 03The most common side effects were mild to moderate gastrointestinal issues, more frequent in the tirzepatide group.
5 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)176 weeks15 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)36 weeks15 mgsubcutaneous(human)36 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)ongoing5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#03

Tirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis.

Loomba Rohit, et al. · The New England journal of medicine · 2024

HumanInfluence51.0
692
The study demonstrated that tirzepatide was more effective than placebo in resolving metabolic dysfunction-associated steatohepatitis without worsening fibrosis in patients with moderate to severe liver fibrosis.

Key findings

  1. 0144% of participants taking 5 mg of tirzepatide saw resolution of MASH without worsening fibrosis, compared to 10% in the placebo group.
  2. 0262% of participants taking 15 mg of tirzepatide achieved the same resolution, showing a significant benefit over placebo.
  3. 03The most common side effects reported were mild to moderate gastrointestinal issues.
5 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)176 weeks15 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)36 weeks15 mgsubcutaneous(human)36 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)ongoing5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#04

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.

Rosenstock Julio, et al. · Lancet (London, England) · 2021

HumanInfluence68.0
670
Researchers observed that tirzepatide significantly improved glycemic control and body weight in humans with type 2 diabetes compared to placebo without increasing the risk of hypoglycemia.

Key findings

  1. 01Tirzepatide led to significant improvements in blood sugar control compared to a placebo.
  2. 02Participants experienced notable weight loss while using tirzepatide.
  3. 03The safety profile of tirzepatide was similar to existing GLP-1 receptor agonists, suggesting it could be a viable treatment option.
10 or 15 mgsubcutaneous(human)36 weeks5 mgsubcutaneous(human)176 weeks5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks
PubMed
#05

Tirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity.

HumanInfluence47.0
602
The study demonstrated that tirzepatide significantly reduced the risk of cardiovascular events and improved health status in patients with heart failure and obesity compared to placebo.
5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks2.5 mgsubcutaneous(human)4 weeks0.75 mgsubcutaneous(human)once per week
PubMed
#06

Tirzepatide once weekly for the treatment of obesity in people with type 2 diabetes (SURMOUNT-2): a double-blind, randomised, multicentre, placebo-controlled, phase 3 trial.

HumanInfluence65.0
553
The study demonstrated that tirzepatide resulted in significant weight loss in adults with obesity and type 2 diabetes compared to placebo over 72 weeks.
5 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)176 weeks15 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)36 weeks15 mgsubcutaneous(human)36 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)ongoing5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#07

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.

Dahl Dominik, et al. · JAMA · 2022

HumanInfluence35.0
505
The study demonstrated that adding tirzepatide to insulin glargine significantly improved glycemic control in patients with type 2 diabetes compared to placebo.

Key findings

  1. 01Participants using tirzepatide had an average decrease in blood sugar levels of up to 2.4% compared to 0.9% in the placebo group.
  2. 02Those treated with tirzepatide lost between 5.4 kg and 8.8 kg, while the placebo group gained 1.6 kg.
  3. 03A higher percentage of patients on tirzepatide achieved target blood sugar levels of less than 7% compared to those on placebo.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#08

Tirzepatide for the Treatment of Obstructive Sleep Apnea and Obesity.

HumanInfluence47.0
492
Researchers observed that tirzepatide significantly reduced the apnea-hypopnea index and body weight in humans with moderate-to-severe obstructive sleep apnea and obesity compared to placebo.
5 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)176 weeks15 mgsubcutaneous(human)176 weeks5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)36 weeks15 mgsubcutaneous(human)36 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#09

Once-weekly tirzepatide versus once-daily insulin degludec as add-on to metformin with or without SGLT2 inhibitors in patients with type 2 diabetes (SURPASS-3): a randomised, open-label, parallel-group, phase 3 trial.

HumanInfluence41.0
467
The study demonstrated that tirzepatide significantly reduced HbA1c and body weight compared to insulin degludec in human participants with type 2 diabetes at 52 weeks.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)36 weeks15 mgsubcutaneous(human)36 weeks5 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)176 weeks15 mgsubcutaneous(human)176 weeks5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)40 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks
PubMed
#10

Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist.

AnimalInfluence31.0
455
The study demonstrated that tirzepatide exhibits an imbalanced mechanism of action favoring GIP receptor engagement over GLP-1 receptor signaling, which may enhance insulin secretion in humans.
5 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)176 weeks15 mgsubcutaneous(human)176 weeks10 mgsubcutaneous(human)36 weeks15 mgsubcutaneous(human)36 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)ongoing5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
Safety

Safety & Handling

Research Gaps

The specific mechanisms by which GIP receptor agonism improves insulin secretion in type 2 diabetic patients remain unclear, particularly since previous studies have indicated that some patients may be unresponsive to GIP. Additionally, while the short-term efficacy and safety of tirzepatide have been established, the long-term effects and potential risks associated with prolonged use in diverse populations have not yet been thoroughly investigated.

Solubility

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

Storage & Handling

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

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

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.

Community Insights

Community Insights

Publications per Year

50 total
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Pricing

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer