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Insulin Tregopil

From PeptidePlaza, the free peptide reference · Entry #1188 · Metabolic · Sources fetched 2026-09-11 · Editorial standards

Insulin Tregopil (also known as Insulin tregopil [INN], Insuline tregopil, Insulina tregopilo, insulinum tregopilum) is a metabolic research peptide. Insulin Tregopil is an oral recombinant human insulin analog that acts as an insulin receptor agonist, currently in Phase 2 clinical trials for diabetes mellitus.

Insulin Tregopil is a synthetic peptide classified as an insulin receptor agonist. It is an ultra-fast acting oral recombinant human insulin analog. Its mechanism of action involves binding to and activating the insulin receptor, mimicking the effects of endogenous insulin. Insulin Tregopil is being investigated for its potential use in the treatment of diabetes mellitus, including both Type 1 and Type 2 diabetes. Clinical development has reached Phase 2 for diabetes mellitus generally, with Phase 1 studies specifically for Type 1 and Type 2 diabetes. Research has focused on its rapid absorption characteristics, pharmacodynamics, and efficacy as an oral prandial insulin analog.

1 Mechanism of action

Insulin receptor agonist (agonist)

Primary targets: Insulin receptor

2 Reported effects

Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.

2.1 Indicated / studied for

  • Diabetes Mellitus
  • Diabetes Mellitus, Type 1
  • Diabetes Mellitus, Type 2

3 Chemical and physical properties

CAS number874442-57-6
Molar mass6026 g/mol
Purity (typical)Not independently verified
Storage−20 °C, lyophilised powder, desiccated
SolubilitySterile water / bacteriostatic water
Receptors / targetsInsulin receptor

4 Research studies (7)

  1. Insulin Tregopil: An Ultra-Fast Oral Recombinant Human Insulin Analog: Preclinical and Clinical Development in Diabetes Mellitus
    Drugs (2023) · Review
  2. Enterically delivered insulin tregopil exhibits rapid absorption characteristics and a pharmacodynamic effect similar to human insulin in conscious dogs
    Diabetes, obesity & metabolism (2019)
  3. Efficacy and safety of Tregopil, a novel, ultra-rapid acting oral prandial insulin analog, as part of a basal-bolus regimen in type 2 diabetes: a randomized, active-controlled phase 2/3 study
    Expert opinion on pharmacotherapy (2022) · RCT
  4. Pharmacokinetics and Pharmacodynamics of Insulin Tregopil in Relation to Premeal Dosing Time, Between Meal Interval, and Meal Composition in Patients With Type 2 Diabetes Mellitus
    Clinical pharmacology in drug development (2020) · RCT
  5. Development and validation of an electrochemiluminescent ELISA for quantitation of oral insulin tregopil in diabetes mellitus serum
    Bioanalysis (2017)
  6. Impact of Insulin Tregopil and Its Permeation Enhancer on Pharmacokinetics of Metformin in Healthy Volunteers: Randomized, Open-Label, Placebo-Controlled, Crossover Study
    Clinical and translational science (2019) · RCT
  7. An open-label, multiple ascending dose trial of orally administered insulin Tregopil in patients with type 1 diabetes mellitus to evaluate its pharmacokinetics, pharmacodynamics, safety and tolerability
    Diabetes, obesity & metabolism (2025)

5 Safety and risk profile

5.1 Regulatory status

Insulin Tregopil is currently classified as Phase 2 clinical trials. It has no approved human indication in the United States; availability elsewhere does not imply demonstrated safety or efficacy.

Safety data disclaimer. Safety assessments are based on published literature and are for educational reference only. Clinical evidence varies significantly between peptides. Always consult primary research and current regulatory guidance.

6 Frequently asked questions

What is Insulin Tregopil?
Insulin Tregopil is an oral recombinant human insulin analog. It functions as an insulin receptor agonist, meaning it activates insulin receptors to help regulate blood sugar levels. It is currently undergoing clinical development for the treatment of diabetes mellitus.
What is Insulin Tregopil used for?
Insulin Tregopil is being studied for the treatment of diabetes mellitus, including both Type 1 and Type 2 diabetes. It is designed to be an ultra-rapid acting oral insulin analog to help manage blood glucose levels.
How does Insulin Tregopil work?
Insulin Tregopil works as an insulin receptor agonist. It binds to and activates insulin receptors on cells, which initiates a cascade of events that leads to glucose uptake from the blood and its utilization by the body's tissues, similar to natural insulin.
What is the regulatory status of Insulin Tregopil?
Insulin Tregopil is currently in Phase 2 clinical trials for diabetes mellitus. Phase 1 studies have also been conducted for Type 1 and Type 2 diabetes specifically, indicating ongoing research into its efficacy and safety.

7 References

  1. Insulin Tregopil — compound summary PubChem. View source
  2. Insulin Tregopil — molecule record ChEMBL. View source
  3. Insulin Tregopil — published literature (7 records) PubMed. View source

Entries that share a target, a mechanism, or a research area with Insulin Tregopil.

8 See also

For research reference only. Not medical advice. Peptides may be regulated or restricted in your jurisdiction. Entry validated by the PeptidePlaza Biomedical Research Desk; see editorial standards.