Dual GIP/GLP-1 Receptor Agonist
Tirzepatide is a first-in-class dual metabolic peptide that delivered 15 to 21% body weight reduction in clinical trials, outperforming every weight loss drug before it, with over half of participants losing more than 20% of their body weight. Its dual-receptor design reduces nausea compared to GLP-1 alone while simultaneously improving blood sugar, cholesterol, and liver fat.
Product
Research shows
Practical product identifiers and format details for professional review.
Content
30 mg
Format
Injectable
Composition
10 mg/ml per ml
Tirzepatide's GLP-1 agonism reduces appetite, slows gastric emptying, and improves glucose-stimulated insulin secretion. The GIP agonism component enhances fat storage regulation in adipocytes, improves insulin sensitivity in peripheral tissues, and attenuates the nausea associated with pure GLP-1 receptor agonism by balancing the emetic pathway. Together, the dual receptor engagement produces superior glycaemic control and substantially greater weight loss than GLP-1 monotherapy, while improving cardiovascular risk markers, triglycerides, and hepatic steatosis markers.
Based on published research and preclinical data. All benefits are documented under research-grade conditions.
Tirzepatide's simultaneous engagement of both GIP and GLP-1 receptors produces additive and potentially synergistic effects on glucose homeostasis. In the SURPASS-2 head-to-head trial against semaglutide 1 mg, all three tirzepatide doses achieved statistically superior HbA1c reductions, with the 15 mg dose producing a mean reduction of −2.30 percentage points versus −1.86 percentage points for semaglutide. Glucose-dependent insulin secretion is amplified by both receptor arms simultaneously, while glucagon suppression is maintained, yielding a dual brake on postprandial hyperglycaemia unachievable with GLP-1 monotherapy.
In the 72-week SURMOUNT-1 phase 3 trial in adults with obesity without type 2 diabetes, tirzepatide produced mean body weight reductions of 15.0%, 19.5%, and 20.9% at the 5, 10, and 15 mg doses respectively, versus 3.1% with placebo. More than 50% of participants on the 10 and 15 mg doses achieved ≥20% body weight reduction: an outcome previously associated only with bariatric surgery. These losses were durable throughout the 72-week observation period, with trajectory analysis indicating ongoing response at trial end.
Pure GLP-1 receptor agonism is associated with a high rate of nausea and vomiting attributed to area postrema activation and slowed gastric emptying. The co-activation of GIP receptors in tirzepatide appears to functionally counterbalance this emetic signalling. In SURMOUNT-1 to SURMOUNT-4 pooled analyses, gastrointestinal adverse event rates were comparable to or lower than those seen with semaglutide 2.4 mg despite greater weight loss efficacy, suggesting that GIP agonism meaningfully attenuates the nausea burden without reducing therapeutic potency.
GIP receptors are highly expressed on adipocytes, and tirzepatide's GIP agonism directly modulates lipid flux within fat depots. GIP receptor activation promotes insulin sensitisation in peripheral adipose tissue, enhances fatty acid re-esterification under fed conditions, and reduces ectopic lipid deposition. This adipocentric mechanism is distinct from GLP-1's primarily central and pancreatic actions, and together they shift adipose function toward healthier lipid partitioning, reducing circulating triglycerides and free fatty acids that contribute to cardiovascular and hepatic risk.
Post hoc analyses of the SURMOUNT-1 trial demonstrated that 72 weeks of tirzepatide treatment produced significant improvements in 10-year predicted ASCVD risk, with relative risk reductions of 16–23% compared to a 12.7% increase in the placebo arm. Reductions in systolic blood pressure, triglycerides, waist circumference, and fasting glucose each contribute independently to cardiovascular risk score improvement. The magnitude of these changes exceeds what is attributable to weight loss alone, suggesting direct vascular and metabolic effects of tirzepatide receptor engagement.
Tirzepatide produces clinically meaningful reductions in liver fat content in individuals with metabolic dysfunction-associated steatotic liver disease (MASLD). In an analysis of Japanese patients with obesity and MASLD, 77% showed disease improvement at 72 weeks versus 10% in the placebo group, with significant reductions in ALT, AST, and hepatic fat fraction on MRI. The mechanism involves reduced hepatic de novo lipogenesis, suppressed hepatic glucagon receptor activity, and direct hepatic GIP receptor engagement reducing fatty acid uptake.
SURMOUNT-1 body composition analyses confirmed the reduction is predominantly from fat mass rather than lean mass. Fat mass decreased significantly across all dose groups while fat-free mass was largely preserved, particularly with adequate dietary protein intake. This preservation of lean mass during energy deficit is clinically important for maintaining resting metabolic rate, functional capacity, and avoiding the sarcopenic obesity phenotype: a key differentiator from historical caloric restriction strategies that result in proportionate lean mass loss.
Explore selected publications and registered trials on Tirzepatide, with links to the original sources.
5 publications from the research library.
Evidence type
Publication and key finding
Source
Evidence type
Human randomized study
Direct Tirzepatide randomized obesity trial
Publication and key finding
In SURMOUNT-1, weekly tirzepatide reduced mean body weight by 15.0% to 20.9% at 72 weeks versus 3.1% with placebo.
The New England journal of medicine
Evidence type
Human randomized study
Direct Tirzepatide phase 3 diabetes-and-obesity trial
Publication and key finding
In adults with obesity and type 2 diabetes, tirzepatide reduced mean body weight by 12.8% to 14.7% at 72 weeks versus 3.2% with placebo.
Lancet (London, England)
Evidence type
Human randomized study
Direct Tirzepatide randomized maintenance trial
Publication and key finding
After a 20.9% lead-in weight reduction, continued tirzepatide produced further loss while switching to placebo led to substantial weight regain.
JAMA
Evidence type
Human randomized study
Direct Tirzepatide long-term diabetes-prevention trial
Publication and key finding
Over three years, tirzepatide produced sustained weight reduction and markedly lowered progression from prediabetes to type 2 diabetes versus placebo.
The New England journal of medicine
Evidence type
Evidence synthesis
Tirzepatide randomized-trial evidence synthesis
Publication and key finding
A network meta-analysis of 28 randomized trials compared tirzepatide with semaglutide and ranked higher tirzepatide doses among the strongest options for HbA1c and weight reduction.
Diabetologia
5 selected studies from the wider trial library, in the order chosen for this product.
NCT05564039
NCT05706506
NCT04255433
NCT04184622
NCT03730662
Follow the product-specific protocol below with qualified professional guidance. For preparation, handling and pen guidance, review the manual.
Labbieux pens are designed for 30 to 31 administrations of 10 clicks. With daily use, this corresponds to approximately one month. We recommend starting with 5 clicks and building up to 10 clicks per administration. More sensitive people may use fewer clicks.
Before using our pens, consult the manual.
The most common adverse effects of tirzepatide are gastrointestinal in nature and include nausea, diarrhoea, vomiting, and constipation. These are typically dose-dependent, most pronounced during dose titration, and generally transient, resolving within weeks of dose stabilisation. In SURMOUNT-1, nausea was reported in approximately 28–40% of tirzepatide-treated participants versus 16% in the placebo arm, with the majority rating events as mild to moderate in severity. Serious gastrointestinal adverse events were infrequent (<2%). Hypoglycaemia risk is low as a monotherapy agent due to the glucose-dependent mechanism of insulin secretion; however, risk increases when combined with sulphonylureas or insulin. Rare but notable risks include pancreatitis, gallbladder disease (including cholelithiasis, occurring in ~2.5% of participants: attributable partly to rapid weight loss), and a potential class-related thyroid C-cell tumour risk identified in preclinical carcinogenicity research. Tirzepatide is contraindicated in individuals with a personal or family history of medullary thyroid carcinoma or Multiple Endocrine Neoplasia syndrome type 2. Injection-site reactions are uncommon. Resting heart-rate elevation of 2–4 bpm has been observed, consistent with GLP-1 class effects.
This public COA documents one selected production batch and is updated annually. It is not the COA for our latest available batch. Every batch has its own documentation, and partners can request the latest batch COA from our team.
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