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Tirzepatide

Mounjaro · Zepbound · LY3298176

Metabolic & WeightApproved

MW: 4813g/mol
Formula: C225H348N48O68

Tirzepatide is a novel peptide classified as a dual glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1 receptor agonist, developed for the management of obesity and type 2 diabetes. Researchers primarily study tirzepatide for its potential to induce significant weight loss and improve metabolic health in individuals with obesity and related conditions. Key findings from clinical trials indicate that participants receiving tirzepatide experienced substantial weight reductions, with some studies reporting mean weight losses of up to 20.9% over 72 weeks, and a markedly lower incidence of type 2 diabetes compared to placebo groups. Additionally, ongoing research continues to explore its long-term safety and efficacy, particularly in diverse populations and various comorbidities.

Chemical Profile

Chemical Structure

Formula	C225H348N48O68
Molecular Weight	4813 g/mol
CAS Number	2023788-19-2
PubChem CID	166567236

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, activating signaling pathways that enhance insulin secretion, suppress glucagon release, and promote satiety. This dual action leads to improved glycemic control and significant weight reduction through mechanisms involving the cAMP/PKA pathway and downstream effects on metabolic processes such as increased lipolysis and reduced appetite. While the overall mechanism is well-characterized, some aspects of its long-term effects on weight maintenance and metabolic health are still being elucidated.

Research

47 Research Publications

11,144

Total Citations

Human/RCT

22.5

Avg. Influence

2025

Latest

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01Top

#01

Tirzepatide Once Weekly for the Treatment of Obesity.

HumanInfluence312.0

2312

Researchers observed that tirzepatide provided substantial and sustained weight reductions in adults with obesity over 72 weeks compared to placebo, with significant improvements in cardiometabolic measures.

10 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 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks

PubMed

02Top

#02

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

01Tirzepatide led to significant improvements in blood sugar control compared to a placebo.
02Participants experienced notable weight loss while using tirzepatide.
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

03Top

#03

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

HumanInfluence45.0

606

The study demonstrated that continued treatment with tirzepatide significantly maintained weight loss in adults with obesity compared to placebo, with 89.5% of participants retaining at least 80% of their initial weight loss.

Key findings

01Participants who continued tirzepatide maintained an average weight loss of 25.3% over 88 weeks, compared to 9.9% for those on placebo.
0289.5% of participants on tirzepatide maintained at least 80% of their weight loss, while only 16.6% of those on placebo did.
03The most common side effects were mild to moderate gastrointestinal issues, more frequent in the tirzepatide group.

PubMed

#04

Tirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis.

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

HumanInfluence42.0

552

Researchers observed that tirzepatide was more effective than placebo in resolving metabolic dysfunction-associated steatohepatitis without worsening fibrosis in patients with moderate or severe fibrosis.

Key findings

0144% of participants taking 5 mg of tirzepatide saw resolution of MASH without worsening fibrosis, compared to 10% in the placebo group.
0262% of participants taking 15 mg of tirzepatide achieved the same resolution, showing a significant benefit over placebo.
03The most common side effects reported were mild to moderate gastrointestinal issues.

PubMed

#05

Tirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity.

HumanInfluence41.0

532

Researchers observed that tirzepatide treatment significantly reduced the risk of cardiovascular events and improved health status in patients with heart failure with preserved ejection fraction and obesity compared to placebo.

PubMed

#06

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

HumanInfluence34.0

489

The study demonstrated that adding tirzepatide to insulin glargine significantly improved glycemic control in humans with type 2 diabetes after 40 weeks.

Key findings

01Participants using tirzepatide had an average decrease in blood sugar levels of up to 2.4% compared to 0.9% in the placebo group.
02Those treated with tirzepatide lost between 5.4 kg and 8.8 kg, while the placebo group gained 1.6 kg.
03A higher percentage of patients on tirzepatide achieved target blood sugar levels of less than 7% compared to those on placebo.

PubMed

#07

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.

HumanInfluence52.0

479

The study demonstrated that tirzepatide resulted in significant weight loss in adults with obesity and type 2 diabetes over 72 weeks compared to placebo, with a favorable safety profile.

PubMed

#08

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

#09

Tirzepatide for the Treatment of Obstructive Sleep Apnea and Obesity.

HumanInfluence43.0

443

The study demonstrated that tirzepatide significantly reduced the apnea-hypopnea index and body weight in individuals with moderate-to-severe obstructive sleep apnea and obesity compared to placebo.

PubMed

#10

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

In VitroInfluence28.0

412

The study demonstrated that tirzepatide exhibits an imbalanced pharmacological profile favoring GIP receptor engagement, which may enhance its efficacy in metabolic control compared to selective GLP-1 receptor agonists.

PubMed

Safety

Safety & Handling

Research Gaps

The long-term effects of tirzepatide beyond the 3-year mark remain unclear, particularly regarding its impact on weight maintenance and the risk of developing type 2 diabetes after treatment cessation. Additionally, the specific mechanisms by which tirzepatide influences obstructive sleep apnea and its associated cardiovascular risks have not been fully elucidated in human trials.

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

🇩🇪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

Publications per Year

50 total

Pricing

Price Comparison

BESTPolaris PeptidesUS
60mg
$360.00
Price/mg
$6.00/mg
View
Polaris PeptidesUS
50mg
$320.00
Price/mg
$6.40/mg
View
Polaris PeptidesUS
30mg
$250.00
Price/mg
$8.33/mg
View
Polaris PeptidesUS
10mg
$99.00
Price/mg
$9.90/mg
View
Polaris PeptidesUS
5mg
$55.00
Price/mg
$11.00/mg
View

Vendor	Amount	Price	Price/mg	Link
BESTPolaris PeptidesUS	60mg	$360.00	$6.00/mg	View
Polaris PeptidesUS	50mg	$320.00	$6.40/mg	View
Polaris PeptidesUS	30mg	$250.00	$8.33/mg	View
Polaris PeptidesUS	10mg	$99.00	$9.90/mg	View
Polaris PeptidesUS	5mg	$55.00	$11.00/mg	View

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Mechanism

Tools

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Mechanism

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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