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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 for its role in managing blood glucose levels in individuals with diabetes mellitus. Key findings from recent studies indicate that pharmacokinetic and pharmacodynamic equivalence exists between biosimilar formulations of insulin, such as Biocon's Insulin-R and the US-licensed Humulin® R, suggesting comparable efficacy and safety profiles. Additionally, clinical evidence indicates that managing insulin dosing in hospitalized patients remains challenging, particularly for those on concentrated insulin formulations like U-500, where hyperglycemia is prevalent. Current research continues to explore the complexities of insulin therapy, focusing on optimizing dosing strategies and improving patient outcomes in various clinical settings.

Overview

Übersicht

Insulin (Regular), also known as Human Insulin, Humulin R, or Novolin R, is a synthetic form of the naturally occurring hormone insulin. It is produced using recombinant DNA technology, often in Escherichia coli, where synthetic genes for the insulin A and B chains are expressed and subsequently purified. This form of insulin is classified under the insulin & glucose regulation category and is used to manage blood glucose levels in individuals with diabetes. Researchers have developed biosimilar versions, such as Biocon's Insulin-R, which have been shown to be pharmacokinetically and pharmacodynamically equivalent to Humulin R in clinical studies. The primary physiological role of insulin is to regulate blood glucose levels by facilitating cellular uptake of glucose, thus playing a crucial role in the management of diabetes mellitus. Research areas include its use in managing gestational diabetes, stress-induced hyperglycemia, and as a basal insulin in high-dose insulin therapy for insulin-resistant patients. Insulin acts primarily through the insulin receptor, a transmembrane receptor that initiates a cascade of intracellular events leading to glucose uptake, glycogen synthesis, and lipid metabolism. Upon binding to its receptor, insulin activates the PI3K/AKT pathway, which is critical for its metabolic effects. Pharmacokinetically, regular insulin has a relatively rapid onset of action and a short duration, making it suitable for mealtime glucose control. It is typically administered subcutaneously, with a circulating half-life of approximately 4-6 hours. The metabolism of insulin occurs primarily in the liver and kidneys. Clinically, regular insulin is used to manage both type 1 and type 2 diabetes and is approved by regulatory agencies like the FDA. It is available by prescription and is considered a critical component of diabetes management protocols. Researchers continue to explore its use in various clinical scenarios, including its role in managing hyperglycemia in hospitalized patients.

Chemical profile

Chemische Struktur

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

Wirkmechanismus

Insulin acts on the insulin receptor, a tyrosine kinase receptor, triggering a signaling cascade that includes the activation of the PI3K/AKT pathway. This cascade facilitates glucose uptake by cells, promotes glycogen synthesis, and regulates lipid metabolism.

Mechanism

Signalweg

Insulin (Regular) primarily exerts its effects through binding to the insulin receptor (IR), a receptor tyrosine kinase, which activates the insulin signaling pathway, including the phosphoinositide 3-kinase (PI3K)/Akt pathway and the mitogen-activated protein kinase (MAPK) pathway. This activation leads to increased glucose uptake in peripheral tissues, particularly muscle and adipose tissue, by promoting the translocation of glucose transporter type 4 (GLUT4) to the cell membrane, as well as enhancing glycogen synthesis and lipid metabolism. The precise mechanisms underlying insulin's effects on various cellular processes are well characterized, but some aspects of its signaling may not be fully understood.

Half-Life & Pharmacokinetics

ENEndogenous

Circulating half-life ~4-6 minutes

SCSubcutaneous

~4-6 hours

IVIntravenous

~5-10 minutes

POOral

Poor bioavailability due to first-pass metabolism

The pharmacokinetic profile varies with different formulations; U500 has a longer duration of action compared to U100.

Storage

Temperature

Refrigerate at 2-8C

Light

Protect from light

Form

Aqueous solution: use within 28 days after opening

Notes

Do not freeze; discard if frozen.

Solubility

Löslichkeit

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

Legal Status

🇩🇪DE

Prescription-only medication (verschreibungspflichtig); not a controlled substance.

🇺🇸US

FDA-approved; prescription required; not a controlled substance.

🇦🇺AU

TGA Schedule 4 (S4) prescription-only medicine.

🇬🇧UK

Prescription-only medicine (POM) as per MHRA regulations.

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, particularly in relation to their home insulin requirements and the management of glycemic outcomes. Further research is needed to conduct larger randomized controlled trials (RCTs) that explore the long-term effects of concentrated insulins on glycemic control and hypoglycemia risk in diverse populations, including those with obesity and insulin resistance. Additionally, there is a need for studies that assess the efficacy of human insulin in specific patient subsets, such as those with gestational diabetes or those requiring insulin during stress, to better understand its role compared to older insulin preparations.

29 Research Publications

1,758

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
799
Researchers observed successful expression and purification of human insulin A and B chains in Escherichia coli using synthetic genes.

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
102
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
Researchers observed that despite significant advancements in insulin development, challenges in achieving optimal glycemic control and minimizing hypoglycemia persist, necessitating further studies for tailored insulin delivery strategies.
#05

Concentrated insulins: the new basal insulins.

Review
50
The review highlighted that concentrated insulins like Humulin-R U500 offer similar onset but longer duration of action compared to U100 regular insulin, potentially reducing hypoglycemia risk.
#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
The review provided an overview of bioequivalence studies for recombinant human insulin preparations, emphasizing their relevance in therapy today.

Clinical Trials (7)

Preclinical
Phase I
Phase II
Phase III
Approved

7

Total Trials

657

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)

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

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