Wiki · Profile

Tirzepatide

Mounjaro · Zepbound · LY3298176

Metabolic & WeightApproved

MW: 4813g/mol
Formula: C225H348N48O68

Tirzepatide is a novel peptide that functions as a dual agonist for glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors, originally developed for the management of type 2 diabetes and obesity. Researchers primarily study tirzepatide for its efficacy in reducing blood glucose levels and body weight in individuals with type 2 diabetes and obesity. Key findings from recent studies indicate that tirzepatide significantly outperforms semaglutide in lowering HbA1c levels and promoting weight loss, with substantial reductions observed over extended treatment periods. Additionally, ongoing research is focused on assessing the cardiovascular safety and long-term effects of tirzepatide in diverse populations, including those with atherosclerotic cardiovascular disease. As of now, tirzepatide is undergoing extensive clinical trials to further evaluate its benefits and safety profile.

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 such as the cAMP/PKA pathway and the PI3K/Akt pathway, which enhance insulin secretion and promote glucose homeostasis. This dual action leads to increased insulin sensitivity, reduced glucagon secretion, and significant weight loss through appetite suppression and enhanced energy expenditure. While the precise molecular mechanisms underlying its effects on weight reduction and glycemic control are still being elucidated, its efficacy in modulating these pathways is well-established.

Research

84 Research Publications

16,033

Total Citations

Human/RCT

21.1

Avg. Influence

2025

Latest

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01Top

#01

Tirzepatide Once Weekly for the Treatment of Obesity.

HumanInfluence398.0

2720

The study demonstrated that once-weekly tirzepatide significantly reduced body weight in humans with obesity over 72 weeks 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

02Top

#02

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

Frías Juan P, et al. · The New England journal of medicine · 2021

HumanInfluence120.0

1358

Researchers observed that tirzepatide was superior to semaglutide in reducing HbA1c levels and body weight in humans with type 2 diabetes over 40 weeks.

Key findings

01Tirzepatide significantly reduced blood sugar levels more than semaglutide.
02Participants taking tirzepatide experienced greater weight loss compared to those on semaglutide.
03The most common side effects for both medications were mild to moderate gastrointestinal issues.

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

HumanInfluence61.0

719

Researchers observed that continued treatment with tirzepatide maintained weight loss in humans with obesity, while withdrawal led to substantial weight regain.

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

HumanInfluence51.0

692

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

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

#06

Obesity Management in Adults: A Review.

ReviewInfluence27.0

646

Researchers observed that comprehensive obesity management combining behavioral interventions and pharmacotherapy, including tirzepatide, can achieve significant weight loss and improve obesity-related health outcomes in humans.

PubMed

#07

Tirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity.

HumanInfluence47.0

602

The study demonstrated that tirzepatide treatment resulted in a lower risk of cardiovascular events and improved health status in patients with heart failure with preserved ejection fraction and obesity.

PubMed

#08

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 significantly reduced body weight in humans with obesity and type 2 diabetes compared to placebo over 72 weeks.

PubMed

#09

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

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.

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

#10

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.

PubMed

Safety

Safety & Handling

Research Gaps

The long-term cardiovascular safety and efficacy of tirzepatide compared to established treatments like dulaglutide are still unknown, as the ongoing SURPASS-CVOT trial has yet to report results. Additionally, the specific mechanisms by which tirzepatide influences weight reduction and diabetes progression remain unclear, necessitating further exploration into its pharmacodynamics and potential interactions with other metabolic pathways.

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
$309.00
Price/mg
$5.15/mg
View
Polaris PeptidesUS
50mg
$270.00
Price/mg
$5.40/mg
View
Polaris PeptidesUS
30mg
$225.00
Price/mg
$7.50/mg
View
Polaris PeptidesUS
10mg
$89.00
Price/mg
$8.90/mg
View
Polaris PeptidesUS
5mg
$55.00
Price/mg
$11.00/mg
View

Vendor	Amount	Price	Price/mg	Link
BESTPolaris PeptidesUS	60mg	$309.00	$5.15/mg	View
Polaris PeptidesUS	50mg	$270.00	$5.40/mg	View
Polaris PeptidesUS	30mg	$225.00	$7.50/mg	View
Polaris PeptidesUS	10mg	$89.00	$8.90/mg	View
Polaris PeptidesUS	5mg	$55.00	$11.00/mg	View

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Mechanism

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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