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Hormone · Profile

Insulin (Regular)

Human Insulin · Humulin R · Novolin R · Regular Insulin

Insulin & Glucose RegulationApproved
MW
5808g/mol
Formula
C257H383N65O77S6

Insulin (Regular) is a peptide hormone produced by the beta cells of the pancreas, classified as a key regulator of glucose metabolism in the body. Researchers primarily study it to understand its pharmacokinetic and pharmacodynamic properties, particularly in relation to diabetes management. Key findings from recent studies indicate that biosimilar formulations of insulin, such as Biocon's Insulin-R, demonstrate pharmacokinetic and pharmacodynamic equivalence to established products like Humulin® R, suggesting comparable efficacy and safety profiles. Additionally, clinical evidence indicates that managing insulin dosing in hospitalized patients, especially those on concentrated formulations like U-500, poses challenges that require further investigation. Current research continues to explore the implications of insulin formulations and dosing strategies to optimize glycemic control in diverse patient populations.

Overview

Übersicht

Insulin (Regular), also known as Human Insulin, Humulin R, or Novolin R, is a synthetic form of the endogenous hormone insulin. It is produced through recombinant DNA technology, often utilizing Escherichia coli as a host for gene expression. This synthetic insulin belongs to the peptide hormone class and is structurally identical to human insulin, consisting of A and B chains linked by disulfide bonds. Researchers have focused on its production, purification, and clinical applications. The primary physiological role of insulin is to regulate glucose metabolism by facilitating cellular uptake of glucose, particularly in muscle and adipose tissues, thereby lowering blood glucose levels. Research areas include its pharmacokinetic and pharmacodynamic properties, equivalence studies with biosimilars, and its use in managing diabetes, including gestational diabetes and stress-induced hyperglycemia. Insulin acts by binding to the insulin receptor, a tyrosine kinase receptor, which triggers a cascade of downstream signaling pathways, including the PI3K-Akt pathway, leading to increased glucose uptake and glycogen synthesis. Pharmacokinetically, regular insulin has a relatively short half-life and is typically administered subcutaneously. It is absorbed into the bloodstream, where it exerts its effects over a few hours. Researchers have observed that its pharmacokinetic profile can vary based on the route of administration, with intravenous administration providing a more immediate effect. Clinically, regular insulin is used to manage blood glucose levels in patients with diabetes mellitus. It is approved by regulatory agencies such as the FDA and is available by prescription. Its use is guided by established clinical protocols, and it is considered a standard treatment for both type 1 and type 2 diabetes.

Chemical profile

Chemische Struktur

FormelC257H383N65O77S6
Molekulargewicht5808g/mol
CAS-Nummer11061-68-0
PubChem CID118984375
Mechanism

Wirkmechanismus

Insulin (Regular) acts on the insulin receptor, a transmembrane receptor with intrinsic tyrosine kinase activity. Upon binding, it initiates a signaling cascade involving the PI3K-Akt pathway, which promotes glucose uptake into cells and glycogen synthesis, thereby reducing blood glucose levels.

Mechanism

Signalweg

Insulin (Regular) primarily acts through the insulin receptor (IR), a receptor tyrosine kinase, which upon binding activates the insulin signaling pathway, including the phosphoinositide 3-kinase (PI3K)/Akt pathway and the mitogen-activated protein kinase (MAPK) pathway. This signaling cascade promotes glucose uptake by enhancing the translocation of glucose transporter type 4 (GLUT4) to the cell membrane, stimulates glycogen synthesis, and inhibits gluconeogenesis in the liver, thereby regulating glucose homeostasis. While the overall mechanism is well characterized, some aspects of insulin signaling and its interactions with other pathways remain to be fully elucidated.

Half-Life & Pharmacokinetics

ENEndogenous

Circulating half-life ~5-10 minutes

SCSubcutaneous

Approximately 4-6 hours

IMIntramuscular

Data limited

IVIntravenous

~10 minutes

POOral

Poor bioavailability due to first-pass metabolism

The pharmacokinetic profile varies significantly with the route of administration, with intravenous providing rapid onset and subcutaneous offering prolonged action.

Storage

Temperature

Refrigerate at 2-8C

Light

Protect from light

Form

Aqueous solution: use within 28 days after opening

Notes

Avoid freezing; discard if frozen.

Solubility

Löslichkeit

Soluble in water, forming a clear solution suitable for injection.

Legal Status

🇩🇪DE

Prescription only (verschreibungspflichtig), not a controlled substance.

🇺🇸US

FDA approved, prescription required, not a controlled substance.

🇦🇺AU

TGA Schedule 4 (S4), prescription only.

🇬🇧UK

Prescription Only Medicine (POM), regulated by MHRA.

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.

Open Questions

Offene Forschungsfragen

Current evidence is limited regarding the optimal dosing strategies for hospitalized patients on U-500 insulin, as retrospective studies indicate significant hyperglycemia during admissions without clear guidance on effective inpatient dosing. Further research is needed to conduct larger randomized controlled trials (RCTs) that evaluate the safety and efficacy of different inpatient insulin dosing regimens in diverse patient populations, particularly those with obesity or complex comorbidities. Additionally, the potential benefits of human insulin in specific subsets of patients, such as those with gestational diabetes or during surgical stress, require further investigation to establish clear clinical guidelines.

30 Research Publications

1,775

Total Citations

17

Human/RCT

3.9

Avg. Influence

2022

Latest

Sort
Filter
#01

Expression in Escherichia coli of chemically synthesized genes for human insulin.

Goeddel D V, et al. · Proceedings of the National Academy of Sciences of the United States of America · 1979

AnimalInfluence9.0
804
Researchers observed successful cloning and purification of human insulin A and B chains in Escherichia coli, enabling further studies on insulin production.

Key findings

  1. 01Synthetic genes for human insulin were successfully cloned.
  2. 02Insulin peptides were purified from a precursor protein.
  3. 03The presence of insulin was confirmed using radioimmunoassay.
#02

Sequence of the human insulin gene.

In VitroInfluence9.0
491
The study demonstrated that the human insulin gene contains two intervening sequences, with potential regulatory regions identified in comparison to the rat insulin gene.
#03

Pre-meal insulin analogue insulin lispro vs Humulin R insulin treatment in young subjects with type 1 diabetes.

HumanInfluence2.0
103
The study demonstrated that insulin lispro significantly reduced hypoglycemic episodes and postprandial glucose excursions compared to regular human insulin in young subjects with type 1 diabetes.
#04

Evolution of insulin development: focus on key parameters.

ReviewInfluence4.0
57
The study demonstrated that despite advancements in insulin development, achieving optimal glycemic control and minimizing hypoglycemia in diabetes patients remains a significant challenge, necessitating further research on tailored insulin delivery strategies.
#05

Concentrated insulins: the new basal insulins.

Review
51
The review demonstrated that concentrated insulins like Humulin-R U500 provide longer action duration and reduced hypoglycemia risk compared to standard insulins.
#06

Allergic reactions to human insulin: a review of current knowledge and treatment options.

ReviewInfluence3.0
40
The review demonstrated that while the incidence of insulin allergy has decreased, it remains a significant issue that can be life-threatening, highlighting the need for effective treatment options.
#07

Human insulin: facile synthesis by modification of porcine insulin.

In Vitro
36
Researchers observed that human insulin can be synthesized from porcine insulin through a chemical modification process, allowing for large-scale production.
#08

Availability of insulin from total parenteral nutrition solutions.

In VitroInfluence2.0
34
Researchers observed that human insulin recovery from total parenteral nutrition solutions is significantly higher than previously reported, with minimal impact from lipid addition or specific amino acid formulations.
#09

Concise synthetic routes to human insulin.

In VitroInfluence1.0
30
Researchers observed concise synthetic routes for human insulin production, achieving high yields in a single workday.
#10

Equivalent Recombinant Human Insulin Preparations and their Place in Therapy.

Review
20
Researchers observed that recombinant human insulin formulations have established bioequivalence and are crucial for addressing global insulin supply needs.

Clinical Trials (13)

Preclinical
Phase I
Phase II
Phase III
Approved

13

Total Trials

1,258

Total Enrolled

Comparison on Efficacy and Safety of Three Inpatient Insulin Therapy in Type2 DM

NCT01855243COMPLETED
Sponsor

Cairo University

Enrollment

63

Started

2010

Primary outcome

Mean Daily Blood Glucose (BG) Concentration During Their Hospital Stay.

Diabetes Mellitus (DM)

The Effect of Insulin on Protein Metabolism After Cardiac Surgery

Sponsor

McGill University Health Centre/Research Institute of the McGill University Health Centre

Enrollment

30

Started

2010

Primary outcome

Protein breakdown

Cardiac Surgery

Pilot Study to Evaluate a Method of Controlling High Blood Sugar in the Pediatric Intensive Care Unit

NCT00240149COMPLETED
Sponsor

Stanford University

Enrollment

0

Started

2005

Primary outcome

Specific Aim #1 Intervention): Randomized study of strict glucose control in a pediatric intensive care unit (PICU) using a discrete-closed-loop (DCL) insulin algorithm.

Hyperglycemia

Insulin for Hyperglycemia in Stroke Trial

NCT04834362Phase 4COMPLETED
Sponsor

National Institute of Neurosciences and Hospital, Dhaka

Enrollment

452

Started

2021

Primary outcome

Glycemic Control

HyperglycemiaStroke, Acute

Insulin Analogues and Severe Hypoglycaemia

NCT00346996Phase 4COMPLETED
Sponsor

Lise Tarnow

Enrollment

179

Started

2007

Primary outcome

Severe hypoglycaemia

Type 1 Diabetes

Insulin in Total Parenteral Nutrition

NCT02706119Phase 4COMPLETED
Sponsor

Fundación Pública Andaluza Progreso y Salud

Enrollment

163

Started

2016

Primary outcome

Basal blood glucose value before starting TPN

Diabetes Mellitus

Basal Bolus Versus Human Insulin in Hospitalized Patients With Diabetes in Paraguay

NCT02278913Phase 4COMPLETED
Sponsor

Universidad Nacional de Asunción

Enrollment

134

Started

2009

Primary outcome

Glycemic control

HyperglycemiaDiabetes

Comparison of Neutral Protamine Hagedorn (NPH) and Lantus Based Insulin Regimen in the Management of Hypoglycemia in the Hospitalized Patients in Noncritical Care Setting

NCT02189395Phase 4TERMINATED
Sponsor

Riverside University Health System Medical Center

Enrollment

52

Started

2013

Primary outcome

difference in glycemic control between treatment groups as measured by the mean daily blood glucose

Type 2 Diabetes Mellitus

Investigating the Accuracy of the Home Glucose Monitors in Hypoglycemia

NCT01013402Phase 4COMPLETED
Sponsor

Gulhane School of Medicine

Enrollment

51

Started

2008

Hypoglycemia

Effect of Glargine Insulin on Glucose Control in Hospitalized Patients Who Receive Tube Feedings

NCT00177398Phase 4COMPLETED
Sponsor

University of Pittsburgh

Enrollment

50

Started

2005

Primary outcome

The primary outcome to be studied is the frequency and severity of hyperglycemia and hypoglycemia in each group

Type 2 DiabetesHyperglycemia

Phase 2, Randomized, Open-Label, Crossover, PD/PK Study of a Novel Pram-Insulin Co-Formulation in Adults With T1D

NCT04074317Phase 2COMPLETED
Sponsor

Xeris Pharmaceuticals

Enrollment

18

Started

2019

Primary outcome

Area Under the Curve 0-180 Minutes for Plasma Glucose >180 mg/dL

Diabetes Mellitus, Type 1Insulin-dependent Diabetes Mellitus

AT278, NovoRapid® and Humulin® R (U500) in Glucose Clamp Study

NCT05754424Phase 1COMPLETED
Sponsor

Arecor Limited

Enrollment

41

Started

2023

Primary outcome

Area under the glucose infusion rate-time curve of insulin aspart

Diabetes Mellitus, Type 2

Comparative Glucose Clamp Study of Wockhardt's Insulin Human Regular for Injection and Novolin R, in Healthy Subjects.

NCT00596063Phase 1COMPLETED
Sponsor

Wockhardt

Enrollment

25

Started

2008

Primary outcome

The primary objective is to test for bioequivalence based on AUC0-12h and Cmax between Wockhardt's Insulin Human Regular for injection and Novolin® R

Diabetes Mellitus

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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