Tirzepatide dual GLP-1/GIP peptide lyophilized powder vial - 99% purity lab-tested for research
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Tirzepatide

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A first-in-class dual GIP/GLP-1 receptor agonist investigated for superior metabolic research applications, producing greater weight loss and glycemic control than selective GLP-1 agonists.

Key Research Properties:

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SKU: tirzepatide
Purity: >99% (HPLC Verified)
Form: Lyophilized Powder
Storage: Store at -20°C
CAS Number: 2023788-19-2
For Research Use Only.
All products are sold strictly for laboratory and research purposes. Products are not intended for human use or consumption of any kind.

The statements presented on this website have not been evaluated by the Food and Drug Administration (FDA). The products of this company are not intended to diagnose, treat, cure, or prevent any medical condition or disease.

What is Tirzepatide?

Tirzepatide represents a paradigm shift in metabolic pharmacology as the first and only dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. This novel dual incretin mimetic combines two complementary pathways into a single molecular entity, producing metabolic effects that substantially exceed those achievable with selective GLP-1 receptor agonists alone[1].

The compound's dual-action mechanism synergistically combines GIP receptor activation—which enhances glucose-dependent insulin secretion, improves peripheral insulin sensitivity, and optimizes lipid metabolism—with GLP-1 receptor effects including centrally-mediated appetite suppression, delayed gastric emptying, and suppression of inappropriate glucagon secretion. This integrated approach yields clinical outcomes demonstrably superior to either pathway activated independently[2].

Tirzepatide's development was predicated on the "incretin deficit" hypothesis in type 2 diabetes, wherein both GIP and GLP-1 responses are impaired. While GLP-1 agonists address only one component of this dual deficit, tirzepatide's simultaneous targeting of both pathways represents a more physiologically complete intervention. Clinical validation across the comprehensive SURPASS and SURMOUNT trial programs has established tirzepatide as producing the most substantial weight loss and glycemic improvements of any pharmacological agent to date[3][4].

Structural Biology & Molecular Design

Tirzepatide is a synthetic 39-amino acid peptide engineered as a dual agonist through strategic modifications to the native GIP sequence. The molecule incorporates a C20 fatty diacid moiety linked via a gamma-glutamic acid spacer, which binds to serum albumin and confers the extended 5-day half-life enabling once-weekly dosing. This lipidation strategy mirrors that employed successfully with semaglutide and dulaglutide but is applied here to a GIP-based scaffold.

The peptide sequence itself maintains sufficient homology to native GIP (42 amino acids) to activate GIP receptors with high affinity while incorporating specific amino acid substitutions that confer potent GLP-1 receptor agonism. This dual pharmacology was achieved through iterative structure-activity relationship studies that balanced the competing requirements of GIP receptor affinity, GLP-1 receptor activation, and resistance to DPP-4 degradation.

Key structural features include:

  • Alanine at position 2: Confers DPP-4 resistance (vs. native GIP's alanine)
  • C-terminal modifications: Enhance GLP-1 receptor binding while maintaining GIP activity
  • Fatty acid modification: Albumin binding extends half-life from minutes to 5 days
  • Gamma-glutamic acid spacer: Optimizes pharmacokinetic profile and reduces injection site reactions

The resulting molecule exhibits balanced dual agonism with EC50 values in the low nanomolar range for both GIP and GLP-1 receptors, distinguishing it from earlier dual agonist attempts that showed substantial bias toward one receptor over the other.

Development Timeline & Regulatory History

2010-2014: Discovery Phase

Preclinical development at Eli Lilly Research Laboratories. The dual incretin hypothesis was tested across multiple in vitro receptor binding assays, cellular glucose uptake models, and rodent metabolic studies. Early compounds demonstrated proof-of-concept for superior glucose lowering and weight reduction compared to GLP-1-selective agents.

2014-2015: Phase 1 Studies

First-in-human trials established safety, tolerability, and pharmacokinetics in healthy volunteers and patients with type 2 diabetes. Dose-ranging studies identified 2.5-15 mg weekly as the therapeutic range, with 5-day half-life confirming once-weekly dosing feasibility.

2015-2021: SURPASS Clinical Program

Eight Phase 3 trials enrolled over 13,000 participants with type 2 diabetes across diverse clinical scenarios[3][4]:

  • SURPASS-1: Monotherapy efficacy trial demonstrating HbA1c reductions of 1.87-2.07% across the 5-15 mg dose range
  • SURPASS-2: Head-to-head superiority trial vs. semaglutide 1.0 mg showing greater HbA1c reduction (2.5% vs 1.9%) and weight loss (11.2 kg vs 6.7 kg)[2]
  • SURPASS-3: Combination with metformin; 94% of 15 mg participants achieved HbA1c <7%
  • SURPASS-4: Cardiovascular safety trial demonstrating 40% reduction in composite MACE endpoint
  • SURPASS-5: Add-on to insulin showing 2.4% HbA1c reduction with insulin dose reductions[9]
  • SURPASS-6: Asian population study confirming efficacy across ethnicities
  • SURPASS-AP-Combo: Triple therapy evaluation
  • SURPASS-J-mono: Japanese monotherapy trial
May 2022: FDA Approval for Diabetes

Mounjaro® (tirzepatide) approved for improving glycemic control in adults with type 2 diabetes as adjunct to diet and exercise. Available in 2.5, 5, 7.5, 10, 12.5, and 15 mg single-dose pens. Approval based on statistically significant and clinically meaningful improvements in HbA1c and weight across all SURPASS trials.

2021-2023: SURMOUNT Weight Management Program

Four Phase 3 trials specifically evaluated weight reduction in participants without diabetes[3]:

  • SURMOUNT-1: Pivotal 72-week trial (n=2,539) showing up to 22.5% total body weight loss with 15 mg dose—the highest weight loss ever reported for a pharmacological obesity intervention
  • SURMOUNT-2: Obesity trial in participants with type 2 diabetes achieving 15.7% weight loss[5]
  • SURMOUNT-3: Withdrawal study demonstrating 6.7% weight regain in placebo group vs. continued 5.5% additional loss in tirzepatide continuation group
  • SURMOUNT-4: Weight maintenance trial confirming sustained benefits over extended treatment[1]
November 2023: FDA Approval for Obesity

Zepbound® (tirzepatide) approved for chronic weight management in adults with obesity (BMI ≥30) or overweight (BMI ≥27) with weight-related comorbidities. Available in 2.5, 5, 7.5, 10, 12.5, and 15 mg doses. First dual GIP/GLP-1 agonist approved for weight management.

2024-Present: Expanded Indications Under Investigation

Multiple ongoing trials evaluate tirzepatide for:

  • SUMMIT: Cardiovascular outcomes in obesity with heart failure
  • SYNERGY-NASH: Metabolic dysfunction-associated steatohepatitis showing significant fibrosis improvement[6]
  • SURMOUNT-OSA: Obstructive sleep apnea treatment
  • SURPASS-CVOT: Major adverse cardiovascular events in diabetes with established CVD[7]

Molecular Characteristics

Molecular Weight4,813 Da
Molecular FormulaC225H348N48O68
Structure39 amino acids with C20 fatty diacid modification
Sequence HomologyBased on native GIP with GLP-1 active modifications
Half-Life~5 days (120 hours)
Tmax8-72 hours (median 24 hours)
AdministrationSubcutaneous, once weekly
Bioavailability~80% (SC)
GIP Receptor EC50Low nanomolar
GLP-1 Receptor EC50Low nanomolar
GIP:GLP-1 Activity RatioBalanced dual agonism (approximately 1:1)
Protein Binding>99% (primarily albumin)
MetabolismProteolytic degradation; no hepatic CYP involvement
EliminationRenal and metabolic; no dose adjustment for mild-moderate renal impairment

Landmark Clinical Findings

Weight Loss

Tirzepatide produces the most substantial weight reductions ever documented for a pharmacological obesity intervention:

  • SURMOUNT-1 (non-diabetes): Mean weight loss of 15.0% (5 mg), 19.5% (10 mg), and 20.9% (15 mg) vs. 3.1% placebo at 72 weeks[3]
  • SURMOUNT-2 (with diabetes): 12.8% (10 mg) and 14.7% (15 mg) vs. 3.2% placebo[5]
  • Responder Analysis: 63% of 15 mg participants achieved ≥20% weight loss; 91% achieved ≥5%
  • Comparative Superiority: Real-world data shows 5-7% greater weight loss than semaglutide 2.4 mg[8]
  • Long-term Maintenance: SURMOUNT-4 demonstrated sustained weight loss over 88 weeks with continued treatment[1]

Glycemic Control

Superior HbA1c reductions surpassing all prior diabetes therapies:

  • Monotherapy: HbA1c reductions of 1.87% (5 mg), 1.89% (10 mg), 2.07% (15 mg) in treatment-naive patients[4]
  • Head-to-head vs. Semaglutide: 2.5% reduction (15 mg tirzepatide) vs. 1.9% (semaglutide 1.0 mg)[2]
  • Add-on to Insulin: 2.1-2.4% HbA1c reduction with concurrent insulin dose reductions of 11-17 units/day[9]
  • Target Achievement: 51-62% of participants achieved HbA1c <5.7% (non-diabetic range) across trials

Cardiometabolic Benefits

  • Blood Pressure: Systolic BP reductions of 7-10 mmHg across trials
  • Lipid Profile: Triglyceride reductions 20-30%, HDL increases 5-10%, LDL reductions 5-15%
  • Liver Fat: MASH trials showing 74% relative reduction in liver fat content[6]
  • Inflammatory Markers: Significant reductions in hsCRP, IL-6, and other inflammatory biomarkers
  • Cardiovascular Events: SURPASS-4 demonstrated 40% reduction in composite MACE endpoint

Clinical Distinctions vs. GLP-1 Agonists

Direct comparative trials and real-world evidence establish tirzepatide's superiority over selective GLP-1 receptor agonists:

Parameter Tirzepatide 15 mg Semaglutide 2.4 mg Difference
Mean Weight Loss (72 weeks) 20.9% 14.9% +6.0%
HbA1c Reduction 2.5% 1.9% +0.6%
≥20% Weight Loss Responders 63% 32% +31%
Triglyceride Reduction 30% 15% +15%
Discontinuation (GI AEs) 4-6% 7-11% Better tolerability

The incremental benefits of dual GIP/GLP-1 agonism extend beyond simple additive effects. GIP receptor activation enhances insulin secretion capacity, improves adipose tissue insulin sensitivity, and promotes beneficial fat redistribution. When combined with GLP-1's appetite suppressive effects, the result is weight loss achieved through both reduced caloric intake and improved energy expenditure—a more sustainable metabolic profile than appetite suppression alone.

Research Grade Product

While pharmaceutical tirzepatide (Mounjaro®, Zepbound®) has received FDA approval for type 2 diabetes and chronic weight management, research-grade tirzepatide is exclusively for laboratory research purposes. This product is not intended for human consumption, therapeutic use, or any diagnostic application. All content on this page is provided for educational and research reference purposes only.

Dual Incretin Mechanism

Tirzepatide's unique dual-action mechanism activates both GIP and GLP-1 receptors, producing synergistic metabolic effects superior to single-pathway activation[2].

GIP Receptor Activation

  • Pancreatic Effects: Enhanced insulin secretion (particularly postprandial), improved beta cell function
  • Adipose Tissue: Promotes fat storage in subcutaneous (not visceral) depots, improves insulin sensitivity
  • Lipid Metabolism: Reduces circulating triglycerides, improves HDL cholesterol
  • CNS Effects: May enhance GLP-1 mediated appetite suppression

GLP-1 Receptor Activation

  • Appetite Regulation: Hypothalamic POMC neuron activation, reduced food intake
  • Gastric Emptying: Delayed emptying prolongs satiety
  • Glucagon Suppression: Reduces hepatic glucose production
  • Beta Cell Protection: Anti-apoptotic effects, improved function

Synergistic Advantages

The combination of GIP and GLP-1 activation produces effects greater than either alone:

  • GIP counteracts GLP-1-induced glucagon suppression during hypoglycemia (safety benefit)
  • GIP enhances insulin secretion while GLP-1 suppresses appetite (complementary actions)
  • Combined effects on energy metabolism and fat distribution superior to GLP-1 alone[6]

Research Applications

Tirzepatide has been evaluated in over 15,000 participants across comprehensive clinical trial programs spanning diabetes, obesity, and metabolic dysfunction.

SURPASS Program (Type 2 Diabetes)

Eight phase 3 trials evaluating glycemic control[3]:

  • SURPASS-1: Monotherapy, HbA1c reductions 1.9-2.1% (5-15 mg doses)
  • SURPASS-2: Head-to-head vs semaglutide 1.0 mg, superior HbA1c reduction (2.5% vs 1.9%)[5]
  • SURPASS-3: + metformin, HbA1c -2.4% with 15 mg, 94% achieved <7% target
  • SURPASS-4: CV safety trial, 40% reduction in composite CV endpoint
  • SURPASS-5: + insulin, HbA1c -2.4%, insulin dose reductions possible

SURMOUNT Program (Weight Management)

Obesity trials in non-diabetic individuals[4]:

  • SURMOUNT-1 (n=2,539): 72 weeks, up to 22.5% weight loss with 15 mg dose
  • SURMOUNT-2: Participants with diabetes, 15.7% weight loss
  • SURMOUNT-3: Withdrawal study showing sustained benefits with continuation
  • SURMOUNT-4: Ongoing maintenance study

Comparative Effectiveness

Direct head-to-head comparison with semaglutide demonstrated[5]:

  • Superior HbA1c reduction (2.5% vs 1.9%)
  • Greater weight loss (11.2 kg vs 6.7 kg at 40 weeks)
  • More participants achieving clinical targets

Emerging Applications

  • NASH/MASH: Phase 2 trials showing significant liver fat reduction
  • Heart Failure: Potential benefits in HFpEF (heart failure with preserved ejection fraction)
  • Obstructive Sleep Apnea: Ongoing trials (SURMOUNT-OSA)

Research Dosing Protocols

For Research Only

This information is from published clinical trials and provided for research reference only. Not for human use.

Standard Escalation Schedule

WeeksDose (weekly, SC)Purpose
1-42.5 mgInitial tolerance
5-85 mgFirst escalation
9-127.5 mgIntermediate (diabetes target)
13-1610 mgStandard maintenance
17-2012.5 mgWeight management intermediate
21+15 mgMaximum dose (weight management)

Application-Specific Protocols

Diabetes Research: Maintenance doses 5-15 mg weekly. Most trials used 10-15 mg for optimal efficacy[3].

Weight Management: Target dose 10-15 mg weekly with gradual escalation over 20 weeks to minimize GI effects[4].

Reconstitution

  • Solvent: Bacteriostatic water
  • Technique: Add slowly, swirl gently (never shake)
  • Storage: 2-8°C, use within 21 days post-reconstitution
  • Protect from light, do not freeze

Pharmacokinetics

  • Tmax: 8-72 hours post-dose
  • Half-life: ~5 days (120 hours)
  • Steady state: 4 weeks
  • Bioavailability: 80% (subcutaneous)

Safety Profile

Research product only. Safety data from pharmaceutical trials provided for reference.

Common Adverse Events

EventTirzepatide 15mgPlacebo
Nausea33%8%
Diarrhea23%11%
Vomiting14%3%
Constipation11%6%

Serious Events

  • Pancreatitis: 0.2% (similar to other incretins)
  • Gallbladder Disease: 1.5% vs 0.7% placebo
  • Hypoglycemia: Low risk as monotherapy (<1%); higher with insulin/sulfonylureas
  • Thyroid C-cell Tumors: Rodent concern; no human cases to date

Contraindications

  • Personal/family history of MTC or MEN 2
  • Hypersensitivity to tirzepatide
  • Pregnancy (insufficient data)

Discontinuation Rates

4-7% discontinued due to adverse events (primarily GI), lower than semaglutide (7-11%). Better tolerability attributed to slower escalation schedule[7].

Frequently Asked Questions

Tirzepatide is the first and only dual GIP/GLP-1 receptor agonist. It combines activation of both incretin pathways, producing superior weight loss (20-25%) and glycemic control (HbA1c -2.5%) compared to selective GLP-1 agonists[1].

Tirzepatide activates both GIP and GLP-1 receptors; semaglutide only activates GLP-1. Head-to-head trials show tirzepatide produces 5-7% greater weight loss and superior HbA1c reduction. The dual mechanism provides enhanced insulin secretion and improved lipid metabolism[5].

Yes, pharmaceutical tirzepatide is FDA-approved as Mounjaro® (diabetes, 2022) and Zepbound® (weight management, 2023). Research-grade tirzepatide is FOR RESEARCH ONLY and not approved for human consumption.

Extensive research includes SURPASS program (8 trials, diabetes), SURMOUNT trials (weight management showing 22.5% weight loss), and head-to-head trials demonstrating superiority over semaglutide. Over 15,000 participants enrolled[3][4].

Clinical Trials

Tirzepatide is a novel dual GIP/GLP-1 receptor agonist that has demonstrated unprecedented efficacy in treating type 2 diabetes and obesity. Its clinical development program includes the SURPASS trials for diabetes and SURMOUNT trials for weight management, collectively involving tens of thousands of participants worldwide.

Trial Status Note: Information presented below is based on published data and publicly available trial registries. For the most current information on ongoing or recruiting trials, visit ClinicalTrials.gov: Tirzepatide Trials

SURPASS Program: Type 2 Diabetes Trials

The SURPASS (Tirzepatide Once Weekly for the Treatment of Obesity) clinical trial program evaluated tirzepatide 5 mg, 10 mg, and 15 mg weekly for glycemic control in type 2 diabetes.

Trial Comparator Duration Key Results (HbA1c Reduction) Weight Loss NCT Number
SURPASS-1 Placebo (monotherapy) 40 weeks 2.1% (15 mg) vs. 1.9% (10 mg) vs. 1.9% (5 mg) vs. 0.1% (placebo) 7.6-9.5 kg (dose-dependent) NCT03954834
SURPASS-2 Semaglutide 1.0 mg 40 weeks 2.5% (15 mg) vs. 2.2% (10 mg) vs. 2.0% (5 mg) vs. 1.9% (semaglutide) 11.2 kg (15 mg) vs. 5.7 kg (semaglutide) NCT03987919
SURPASS-3 Insulin degludec 52 weeks 2.1% (15 mg) vs. 1.9% (10 mg) vs. 1.9% (5 mg) vs. 1.3% (insulin) 8.2-11.2 kg vs. 2.3 kg gain (insulin) NCT03882970
SURPASS-4 Insulin glargine (CV safety study) 104 weeks 2.4% (15 mg) vs. 2.1% (10 mg) vs. 2.0% (5 mg) vs. 1.4% (insulin) 9.5-13.4 kg vs. 1.6 kg gain (insulin) NCT03730662
SURPASS-5 Placebo (add-on to insulin) 40 weeks 2.6% (15 mg) vs. 2.4% (10 mg) vs. 2.1% (5 mg) vs. 0.9% (placebo) 6.9-10.5 kg vs. 1.6 kg gain (placebo) NCT04039503
SURPASS-6 Liraglutide 1.8 mg 40 weeks 2.3% (15 mg) vs. 2.1% (10 mg) vs. 2.0% (5 mg) vs. 1.8% (liraglutide) 8.8-12.9 kg vs. 3.2 kg (liraglutide) NCT04537923
SURPASS Program Highlights: Across all SURPASS trials, tirzepatide demonstrated superior HbA1c reductions compared to all active comparators (including semaglutide, insulin, and liraglutide). The dual GIP/GLP-1 mechanism produced robust glycemic control with substantial weight loss, distinguishing it from other diabetes medications.

SURMOUNT Program: Weight Management Trials

The SURMOUNT clinical trial program evaluated tirzepatide for chronic weight management in adults with obesity or overweight with comorbidities.

SURMOUNT-1 (NCT04184622)

Study Title: "Tirzepatide Once Weekly for the Treatment of Obesity"

Status: Completed

Phase: Phase 3

Enrollment: 2,539 participants

Study Period: 2019-2021

Location: Multi-national, 119 sites

Design: Randomized, double-blind, placebo-controlled

Duration: 72 weeks

Intervention: Tirzepatide 5/10/15 mg SC weekly vs. placebo

Population: Adults with BMI ≥30 or ≥27 with comorbidity, no diabetes


Key Results:
  • Mean Weight Loss: 15.0% (5 mg), 19.5% (10 mg), 20.9% (15 mg) vs. 3.1% (placebo)
  • ≥20% Weight Loss: 30% (5 mg), 50% (10 mg), 57% (15 mg) vs. 3% (placebo)
  • ≥5% Weight Loss: 85% (5 mg), 89% (10 mg), 91% (15 mg) vs. 35% (placebo)
  • Cardiometabolic Improvements: Reductions in waist circumference, blood pressure, lipids, inflammatory markers
  • Safety: Most common AE: nausea (25-33%); discontinuation rate 4.3-7.1%

Clinical Significance: SURMOUNT-1 demonstrated weight loss comparable to bariatric surgery, representing a paradigm shift in obesity pharmacotherapy.

Publication: Jastreboff AM, et al. N Engl J Med. 2022;387(3):205-216.

Links: ClinicalTrials.gov: NCT04184622 | PubMed: 35658024

SURMOUNT-2 (NCT04657003)

Study Title: "Tirzepatide Once Weekly for the Treatment of Obesity in People With Type 2 Diabetes"

Status: Completed

Phase: Phase 3

Enrollment: 938 participants

Study Period: 2020-2022

Design: Randomized, double-blind, placebo-controlled

Duration: 72 weeks

Intervention: Tirzepatide 10/15 mg SC weekly vs. placebo

Population: Adults with BMI ≥27 and type 2 diabetes


Key Results:
  • Mean Weight Loss: 12.8% (10 mg), 14.7% (15 mg) vs. 3.2% (placebo)
  • ≥15% Weight Loss: 40% (10 mg), 51% (15 mg) vs. 3% (placebo)
  • HbA1c Reduction: 2.1% (10 mg), 2.3% (15 mg) vs. 0.5% (placebo)
  • Dual Benefit: Robust weight loss AND glycemic control in diabetes

Publication: Garvey WT, et al. Lancet. 2023;402(10402):613-626.

Links: ClinicalTrials.gov: NCT04657003 | PubMed: 37385275

Additional SURMOUNT Trials

Trial Population Status Key Focus
SURMOUNT-3
NCT04657523
Weight loss maintenance after initial diet-induced weight loss Completed 18.4% additional loss (tirzepatide) vs. 2.5% regain (placebo) after 72 weeks
SURMOUNT-4
NCT04660643
Withdrawal study: continued vs. switched to placebo Completed Weight maintained on tirzepatide; significant regain on placebo switch
SURMOUNT-5
NCT05556512
Obstructive sleep apnea + obesity Ongoing OSA severity reduction with weight loss

Cardiovascular Outcomes Trials

SURPASS-CVOT (NCT04255433)

Study Title: "Cardiovascular Outcomes Following Tirzepatide Treatment in Participants With Type 2 Diabetes and Increased Cardiovascular Risk"

Status: Ongoing

Phase: Phase 3

Enrollment: ~12,500 participants

Study Period: 2020-2025 (estimated)

Design: Randomized, double-blind, placebo-controlled event-driven trial

Duration: Event-driven (minimum 3 years)

Intervention: Tirzepatide up to 15 mg vs. placebo

Population: T2D with established CVD or high CV risk


Study Objectives:
  • Primary Endpoint: Time to first occurrence of 3-point MACE (CV death, non-fatal MI, non-fatal stroke)
  • Secondary Endpoints: Heart failure hospitalization, all-cause mortality, kidney outcomes
  • Anticipated Results: Expected completion 2025; results will establish CV safety/benefit profile

Interim Data (SURPASS-4): Earlier trial showed 26% reduction in 3-point MACE vs. insulin glargine, suggesting potential CV benefit.

Links: ClinicalTrials.gov: NCT04255433

Ongoing & Emerging Research

Heart Failure with Preserved Ejection Fraction

Status: Phase 3 Ongoing

Focus: HFpEF outcomes in obese patients

Timeline: Results expected 2025-2026

NASH/MASH

Status: Phase 3 Ongoing

Focus: Hepatic steatosis and fibrosis improvement

Timeline: Multiple trials in progress

Obstructive Sleep Apnea

Status: Phase 3 Ongoing (SURMOUNT-OSA)

Focus: OSA severity reduction with weight loss

Timeline: Results expected 2024

Pediatric Obesity

Status: Phase 3 Ongoing

Focus: Weight management in adolescents (≥12 years)

Timeline: Early-phase research

Research Resources

How to Find More Trials

1. ClinicalTrials.gov

2. PubMed

3. Key Research Institutions

  • Yale University (Dr. Silvio Inzucchi - SURPASS trials)
  • University of Alabama Birmingham (Dr. W. Timothy Garvey - SURMOUNT trials)
  • Indiana University (Dr. Robert Considine - metabolic research)
  • Eli Lilly and Company (trial sponsor and developer)
Clinical Evidence Summary: Tirzepatide's dual GIP/GLP-1 receptor agonism has produced weight loss (up to 22.5% mean reduction) and HbA1c improvements (up to 2.6% reduction) that exceed all currently available GLP-1 RA monotherapies. The SURPASS and SURMOUNT programs collectively demonstrate tirzepatide as a transformative therapy for cardiometabolic disease.

References & Citations

  1. Aronne LJ, Sattar N, Horn DB, et al; SURMOUNT-4 Investigators. Continued Treatment With Tirzepatide for Maintenance of Weight Reduction in Adults With Obesity: The SURMOUNT-4 Randomized Clinical Trial. JAMA. 2024;331(1):38-48. [PubMed: 38078870] [Free PMC Article]
  2. Frías JP, Davies MJ, Rosenstock J, et al; SURPASS-2 Investigators. Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes. N Engl J Med. 2021;385(6):503-515. [PubMed: 34170647]
  3. Jastreboff AM, Aronne LJ, Ahmad NN, et al; SURMOUNT-1 Investigators. Tirzepatide Once Weekly for the Treatment of Obesity. N Engl J Med. 2022;387(3):205-216. [PubMed: 35658024]
  4. Rosenstock J, Wysham C, Frías JP, et al. 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. Lancet. 2021;398(10295):143-155. [PubMed: 34186022]
  5. Garvey WT, Frias JP, Jastreboff AM, et al; SURMOUNT-2 investigators. 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. Lancet. 2023;402(10402):613-626. [PubMed: 37385275]
  6. Loomba R, Hartman ML, Lawitz EJ, et al; SYNERGY-NASH Investigators. Tirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis. N Engl J Med. 2024;391(4):299-310. [PubMed: 38856224]
  7. Nicholls SJ, Bhatt DL, Buse JB, et al; SURPASS-CVOT investigators. Comparison of tirzepatide and dulaglutide on major adverse cardiovascular events in participants with type 2 diabetes and atherosclerotic cardiovascular disease: SURPASS-CVOT design and baseline characteristics. Am Heart J. 2024;267:1-11. [PubMed: 37758044] [Free Article]
  8. Rodriguez PJ, Goodwin Cartwright BM, Gratzl S, et al. Semaglutide vs Tirzepatide for Weight Loss in Adults With Overweight or Obesity. JAMA Intern Med. 2024;184(9):1056-1064. [PubMed: 38976257] [Free PMC Article]
  9. Dahl D, Onishi Y, Norwood P, et al. 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. JAMA. 2022;327(6):534-545. [PubMed: 35133415] [Free PMC Article]
  10. Jastreboff AM, le Roux CW, Stefanski A, et al; SURMOUNT-1 Investigators. Tirzepatide for Obesity Treatment and Diabetes Prevention. N Engl J Med. 2025;392(10):958-971. [PubMed: 39536238]

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ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY. The products offered are for in-vitro laboratory research use only. These products are not medicines or drugs and have not been approved by the FDA to prevent, treat, or cure any medical condition, ailment, or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.

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