Evidence Grade A — Regulatory approved. 2082 published studies. 219 registered clinical trials.
Medically reviewed by a licensed medical professional
Loading...
Tirzepatide (sold as Mounjaro for diabetes and Zepbound for weight management) is a once-weekly injection that activates two gut hormone receptors simultaneously — GIP and GLP-1 — making it the first dual-action treatment in its class. It has produced the largest weight loss of any approved medication: an average of 22.5% body weight in clinical trials at the highest dose.
Tirzepatide is also known by these brand and alternate names:
2,082 published studies: 1112 human, 64 animal, 38 in-vitro, 732 reviews
Tirzepatide is marketed as Mounjaro for type 2 diabetes (approved May 2022) and Zepbound for weight management (approved November 2023), with a further approval for obstructive sleep apnoea in people with obesity (December 2024). It was developed by Eli Lilly and is the first medication to target both GIP and GLP-1 receptors.
In clinical trials, patients taking the highest dose lost an average of 22.5% of their body weight, and a head-to-head study showed it was significantly more effective than semaglutide for weight loss (20.2% versus 13.7%). A three-year extension study showed sustained weight loss of approximately 20% with continued use, and a separate trial found it reduced progression to type 2 diabetes by 94% in people with prediabetes. Trials are now underway for chronic kidney disease and cardiovascular outcomes. The most common side effects are gastrointestinal, including nausea and diarrhoea, which tend to improve over time.
Your body uses two key hormones after eating — GIP and GLP-1 — to control blood sugar and appetite. Most similar medications only target one of these. Tirzepatide is designed to activate both at the same time, which produces a combined effect greater than either hormone alone. It triggers insulin release when blood sugar is high, suppresses the hormone that raises blood sugar, slows stomach emptying so you feel full longer, and reduces appetite through signals to the brain. This dual approach is why it achieves greater weight loss and blood sugar improvements than single-target treatments.
Tirzepatide's clinical evidence is extensive. In a head-to-head study against semaglutide, it achieved 20.2% weight loss versus 13.7%. A three-year extension study showed sustained weight loss of approximately 20% with continued use. The SURMOUNT-3 trial found it reduced progression from prediabetes to type 2 diabetes by 94% — one of the most striking preventive results in metabolic medicine. It has also received approval for obstructive sleep apnoea in people with obesity. Active trials are investigating tirzepatide for chronic kidney disease and cardiovascular outcomes. A Phase II trial showed resolution of fatty liver disease (MASH) in 73% of patients at the highest dose. Side effects are predominantly gastrointestinal (nausea, diarrhoea, vomiting), tend to improve over time, and a thyroid tumour boxed warning exists based on animal data. Most weight is regained after stopping treatment, consistent with the class. A numerically higher rate of cardiovascular death was noted in one trial but was not statistically significant.
PeptideTrace tracks 219 registered clinical trials for Tirzepatide sourced from ClinicalTrials.gov.
Tirzepatide for the Treatment of Concurrent Type 1 Diabetes and Overweight or Obesity
Trial of Tirzepatide for the Treatment of Cannabis Use Disorder
Effectiveness of Combined GLP-1/GIP Dual Agonist Therapy and Structured Exercise on Skeletal Muscle Morphology, Quality, and Physical Function in Overweight and Obese Individuals
Safety and Efficacy of NA-931 and Tirzepatide in Adults Who Are Overweight or Obese
The Effect of Exercise and Tirzepatide on Weight and Health Outcomes (EXER-MED)
FDA ORIG 1
EMA Marketing Authorisation
FDA SUPPL 6
FDA SUPPL 2
FDA ORIG 1
FDA SUPPL 3
FDA SUPPL 19
FDA SUPPL 6
FDA SUPPL 15
FDA SUPPL 11
FDA SUPPL 5
FDA SUPPL 15
FDA SUPPL 22
FDA SUPPL 10
Health Canada Market Authorisation
FDA SUPPL 13
FDA SUPPL 20
FDA SUPPL 31
FDA SUPPL 31
FDA SUPPL 34
FDA SUPPL 39
FDA SUPPL 37
FDA SUPPL 41
FDA SUPPL 2
FDA SUPPL 9
FDA SUPPL 42
Tirzepatide is a 39-amino-acid synthetic peptide engineered as a dual GIP and GLP-1 receptor agonist. It contains a C20 unsaturated fatty diacid chain for albumin binding, producing a half-life of approximately 5 days and enabling once-weekly subcutaneous dosing. It is an imbalanced dual agonist with equal affinity for the GIP receptor relative to native GIP but approximately 5-fold weaker affinity at GLP-1R compared to native GLP-1.
Tirzepatide co-activates both GIPR and GLP-1R, producing synergistic enhancement of glucose-dependent insulin secretion, glucagon regulation, appetite suppression, and delayed gastric emptying. It displays biased agonism at GLP-1R, favoring cAMP signaling over β-arrestin recruitment, which may reduce receptor desensitization and improve sustained efficacy. The dual incretin mechanism engages non-overlapping hypothalamic and brainstem receptor populations, and GIP receptor activation may independently decrease food intake and increase energy expenditure. This dual agonism achieves greater metabolic effects than pure GLP-1 receptor agonism alone.
Tirzepatide is marketed as Mounjaro (type 2 diabetes, approved May 13, 2022), Zepbound (chronic weight management, approved November 8, 2023; moderate-to-severe OSA with obesity, approved December 2024). In the SURMOUNT-1 trial (N=2,539), tirzepatide 15 mg achieved 22.5% mean weight loss versus 2.4% with placebo over 72 weeks. SURMOUNT-5 showed superiority over semaglutide 2.4 mg (20.2% vs 13.7%). The SURPASS program demonstrated HbA1c reductions up to 2.30% with the 15 mg dose. In SURPASS-2, all tirzepatide doses were superior to semaglutide 1.0 mg for glycemic control. The SURPASS-CVOT trial (N=13,299) met noninferiority versus dulaglutide for cardiovascular outcomes but did not achieve superiority (MACE HR 0.92). The SUMMIT trial in heart failure with preserved ejection fraction showed a 38% reduction in cardiovascular death or worsening HF (HR 0.62).
Compare prices from 20 vendor listings
View pricing data across vendors and countries for Tirzepatide
Semaglutide is one of the most extensively studied peptide medications available today, with clinical trial data spanning over 50,000 patients. It is sold as Ozempic for type 2 diabetes (approved 2017), Rybelsus as an oral tablet for diabetes (approved 2019), and Wegovy for weight management (approved 2021). Wegovy has since received additional approvals for reducing heart attack and stroke risk, for use in adolescents aged 12 and older, and for liver disease related to obesity. In clinical trials, patients taking Wegovy lost an average of 14.9% of their body weight over 68 weeks, and the SELECT trial demonstrated a 20% reduction in major cardiovascular events such as heart attack and stroke. Research is now exploring its potential in early Alzheimer's disease. The main side effects are gastrointestinal, particularly nausea, and a key limitation is that most weight tends to return after stopping treatment.
Bimagrumab is in Phase II/III development (not yet approved). A Phase II trial (75 patients with type 2 diabetes and obesity) showed 20.5% fat mass reduction with 3.6% lean mass increase — essentially reshaping body composition without net appetite suppression. The BELIEVE Phase IIb trial (507 patients) showed that bimagrumab plus semaglutide achieved 22% weight loss with the weight lost being 88% fat — significantly better body composition than semaglutide alone. Bimagrumab is not a peptide. Its strategic significance is as a combination partner to address the muscle loss problem inherent in weight loss with current obesity drugs. Eli Lilly's acquisition positions it alongside tirzepatide.
Pemvidutide is in Phase II/III development (not yet approved). In the MOMENTUM Phase II trial (391 patients, 48 weeks), the 2.4 mg dose achieved 15.6% weight loss. Body composition analysis showed 78% of weight lost was fat mass, with only 22% lean mass — a favourable ratio. A Phase IIb MASH trial (212 patients) showed MASH resolution in up to 75% of patients at the highest dose. Pemvidutide's balanced receptor profile and no-titration dosing regimen represent potential practical advantages. The high rate of MASH resolution in Phase II positions it as a candidate for liver disease indications alongside obesity.
Evidence Reviews
Timelines
Deep Dives
This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
