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Insulin Glargine

Lantus · Toujeo · Basaglar · Long-acting insulin

Insulin & Glucose RegulationApproved
MW
6063g/mol
Formula
C267H404N72O78S6

Insulin glargine is a long-acting human insulin analogue produced in recombinant form, primarily synthesized in laboratories for therapeutic use in diabetes management. Researchers primarily study insulin glargine to evaluate its efficacy and safety in achieving glycemic control in individuals with type 1 and type 2 diabetes. Key findings from clinical studies indicate that insulin glargine provides a stable basal insulin level without pronounced peaks, resulting in lower rates of hypoglycemia compared to traditional intermediate-acting insulins. Additionally, concentrated formulations of insulin glargine have shown similar effectiveness in lowering blood glucose levels while potentially reducing the risk of hypoglycemic events. Current research continues to explore its immunogenicity and long-term outcomes in diverse populations, underscoring its clinical relevance in diabetes care.

Overview

Übersicht

Insulin glargine is a synthetic long-acting insulin analogue, produced through recombinant DNA technology. It belongs to the chemical class of insulin analogues and is designed to mimic the basal insulin secretion of the pancreas. Insulin glargine is available under various brand names, including Lantus, Toujeo, and Basaglar. Researchers have focused on its use in managing diabetes mellitus, particularly in providing a stable basal insulin level. The primary physiological role of insulin glargine is to regulate glucose metabolism by facilitating cellular glucose uptake, thereby lowering blood glucose levels. It is primarily used in the treatment of both type 1 and type 2 diabetes mellitus, where it helps maintain glycemic control by providing a consistent insulin level without pronounced peaks. Insulin glargine acts by binding to the insulin receptor, triggering a cascade of events that promote glucose uptake in muscle and fat tissues and inhibit hepatic glucose production. This mechanism of action is similar to endogenous insulin, but insulin glargine is designed to be released slowly over 24 hours, providing a steady insulin level. Pharmacokinetically, insulin glargine has a prolonged duration of action with no significant peak, and its time-action profile is relatively constant. It is administered subcutaneously, and its bioavailability and metabolism can vary among individuals. Clinically, insulin glargine is used as a basal insulin in diabetes management and is approved for use in adults and children with type 1 diabetes and adults with type 2 diabetes. It is well-tolerated and associated with a lower risk of hypoglycemia compared to some other insulin formulations. Regulatory agencies have approved insulin glargine for medical use, highlighting its importance in diabetes care.

Chemical profile

Chemische Struktur

Chemical structure of Insulin Glargine
FormelC267H404N72O78S6
Molekulargewicht6063g/mol
CAS-Nummer160337-95-1
PubChem CID118984454
Mechanism

Wirkmechanismus

Insulin glargine acts on the insulin receptor, initiating a signaling cascade that promotes glucose uptake in muscle and adipose tissues and inhibits hepatic glucose production. This results in decreased blood glucose levels, mimicking the action of endogenous insulin.

Mechanism

Signalweg

Insulin glargine binds to the insulin receptor (IR), activating the insulin receptor signaling pathway, which includes the phosphoinositide 3-kinase (PI3K)/Akt pathway and the mitogen-activated protein kinase (MAPK) pathway. This activation promotes glucose uptake in peripheral tissues, particularly muscle and adipose tissue, enhances glycogen synthesis, and inhibits gluconeogenesis in the liver, thereby contributing to improved glycemic control. The exact molecular mechanisms underlying its long-acting profile and peakless action remain incompletely understood.

Half-Life & Pharmacokinetics

Insulin glargine is designed for subcutaneous administration with a prolonged duration of action, providing a stable insulin level over 24 hours without a significant peak.

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

Insulin glargine is soluble in aqueous solutions, which is relevant for its formulation as an injectable solution.

Legal Status

🇩🇪DE

Verschreibungspflichtig (prescription only), not a controlled substance under BtMG.

🇺🇸US

FDA approved for prescription use, not scheduled by DEA.

🇦🇺AU

TGA Schedule 4 (prescription only medicine).

🇬🇧UK

Prescription only medicine (POM) under 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 long-term safety and efficacy of insulin glargine in diverse populations, particularly in those with concurrent diseases or varying comorbidities, as highlighted by the study on diabetic dogs. Further research is needed to explore the pharmacokinetics and individual variability in response to insulin glargine, particularly in cases of overdose, to better understand the implications for treatment protocols. Additionally, larger randomized controlled trials are necessary to investigate the immunogenicity of different formulations of insulin glargine and their impact on clinical outcomes across various demographics, including age and ethnicity.

70 Research Publications

1,211

Total Citations

45

Human/RCT

2.0

Avg. Influence

2024

Latest

Sort
Filter
#01

Similar efficacy and safety of LY2963016 insulin glargine and insulin glargine (Lantus®) in patients with type 2 diabetes who were insulin-naïve or previously treated with insulin glargine: a randomized, double-blind controlled trial (the ELEMENT 2 study).

HumanInfluence7.0
100
The study demonstrated that LY2963016 insulin glargine is non-inferior to Lantus in achieving glycemic control in patients with type 2 diabetes, with similar safety profiles.
#02

Evaluation of the carcinogenic potential of insulin glargine (LANTUS) in rats and mice.

AnimalInfluence7.0
97
The study demonstrated that insulin glargine did not show systemic carcinogenic potential in rats and mice, despite some localized tissue irritation observed.
#03

Evaluation of the reproductive toxicity and embryotoxicity of insulin glargine (LANTUS) in rats and rabbits.

AnimalInfluence1.0
84
Researchers observed that insulin glargine had no significant reproductive or embryotoxic effects in rats, with toxicity linked to hypoglycemia at high doses.
#04

Initiation of insulin glargine therapy in type 2 diabetes subjects suboptimally controlled on oral antidiabetic agents: results from the AT.LANTUS trial.

HumanInfluence1.0
72
Researchers observed significant reductions in HbA1c with low hypoglycemia risk when initiating insulin glargine therapy in human patients with type 2 diabetes on oral antidiabetic agents.
#05

No evidence for accumulation of insulin glargine (LANTUS): a multiple injection study in patients with Type 1 diabetes.

HumanInfluence1.0
68
The study demonstrated that there is no evidence of accumulation of insulin glargine after multiple injections in human patients with Type 1 diabetes.
#06

Effect of therapy with insulin glargine (lantus) on glycemic control in toddlers, children, and adolescents with diabetes.

Case ReportInfluence1.0
56
Researchers observed a significant reduction in HbA1c and hypoglycemia frequency in children and adolescents with diabetes after starting insulin glargine therapy, without increasing BMI or insulin requirements.
#07

Therapy with insulin glargine (Lantus) in toddlers, children and adolescents with type 1 diabetes.

HumanInfluence3.0
45
Researchers observed that insulin glargine significantly improved metabolic control in children and adolescents with type 1 diabetes without increasing severe hypoglycemic events.
#08

Insulin glargine in the treatment of type 1 and type 2 diabetes.

ReviewInfluence1.0
44
Researchers observed that insulin glargine provides a consistent plasma insulin level over 24 hours, leading to effective glycemic control and lower rates of hypoglycemia compared to traditional basal insulins.
#09

Insulin glargine: long-acting basal insulin analog for improved metabolic control.

ReviewInfluence4.0
40
The review highlighted that insulin glargine offers improved metabolic control and a better safety profile compared to traditional human insulins for basal therapy in diabetes management.
#10

Insulin glargine (Lantus).

Owens D R & Griffiths S · International journal of clinical practice · 2002

Review
38
Researchers observed that insulin glargine provides equivalent glycemic control to NPH insulin with a lower risk of hypoglycemia and higher treatment satisfaction in patients with type 1 and type 2 diabetes.

Key findings

  1. 01Insulin glargine offers consistent insulin levels without peaks, reducing the risk of low blood sugar.
  2. 02Patients using insulin glargine reported better fasting blood glucose levels and overall treatment satisfaction.
  3. 03It can be effectively combined with other insulin types or oral medications for better diabetes management.

Clinical Trials (24)

Preclinical
Phase I
Phase II
Phase III
Approved

24

Total Trials

16,958

Total Enrolled

The DURABLE Trial: Evaluating the Durability of Starter Insulin Regimens in Patients With Type 2 Diabetes (IOOV)

NCT00279201Phase 4COMPLETED
Sponsor

Eli Lilly and Company

Enrollment

2,091

Started

2005

Primary outcome

INITIATION: 24-Week Endpoint Glycosylated Hemoglobin (HbA1c)

Diabetes Mellitus, Type 2

Insulin Glargine "All to Target" Trial

NCT00384085Phase 4COMPLETED
Sponsor

Sanofi

Enrollment

588

Started

2006

Primary outcome

Percentage of Patients Achieving Glycosylated Hemoglobin A1c (HbA1c) < 7.0% at Week 60 (Lantus/Apidra-3 Versus Novolog Mix 70/30 - Intent To Treat (ITT) Population Without Good Clinical Practices (GCP) Noncompliant Sites)

Diabetes Mellitus, Type 2

This Study Is To Determine If Inhaled Insulin Is Effective In Treating Type 2 Diabetes Mellitus

NCT00418522Phase 4COMPLETED
Sponsor

Pfizer

Enrollment

413

Started

2007

Primary outcome

Change From Baseline in Glycosylated Hemoglobin A1c (HbA1c) at Week 26 for the Per Protocol (PP) Population

Diabetes Mellitus, Type 2

Evaluation of the Safety and Efficacy of Insulin Glargine 300 U/ml (Gla-300) in Insulin-naïve Patients With Type 2 Diabetes Mellitus Uncontrolled on Oral Antihyperglycemic Drugs

NCT04980027Phase 4COMPLETED
Sponsor

Sanofi

Enrollment

228

Started

2021

Primary outcome

Percentage of participants with Treatment Emergent Adverse Events (TEAEs)

Type 2 Diabetes Mellitus

A Study to Investigate Safety and Efficacy of iGlarLixi in Adult Patients With Type 2 Diabetes Mellitus

NCT06716424Phase 4ACTIVE_NOT_RECRUITING
Sponsor

Sanofi

Enrollment

105

Started

2025

Primary outcome

Percentage of participants with treatment emergent adverse events (TEAEs) including serious adverse events (SAEs)

Type 2 Diabetes

Effects of Insulin in Perceived Mood Symptoms in Patients With Type 2 Diabetes

NCT00191178Phase 4COMPLETED
Sponsor

Eli Lilly and Company

Enrollment

60

Started

2003

Primary outcome

Compare twice-daily insulin lispro Low Mix therapy and once-daily insulin glargine therapy with respect to perceived mood on patient-rated questionnaires following chronic treatment administration in patients with type 2 diabetes

Type 2 Diabetes

Basal Bolus vs. Sliding Scale for Treatment of Diabetic Patients in Medical Wards

NCT01594060Phase 4COMPLETED
Sponsor

HaEmek Medical Center, Israel

Enrollment

36

Started

2012

Diabetes Mellitus Type 2

A Trial Comparing Cardiovascular Safety of Insulin Degludec Versus Insulin Glargine in Subjects With Type 2 Diabetes at High Risk of Cardiovascular Events

NCT01959529Phase 3COMPLETED
Sponsor

Novo Nordisk A/S

Enrollment

7,637

Started

2013

Primary outcome

Time From Randomisation to First Occurrence of a Major Adverse Cardiovascular Event (MACE): Cardiovascular Death, Non-fatal Myocardial Infarction, or Non-fatal Stroke

DiabetesDiabetes Mellitus, Type 2

Efficacy and Safety of Insulin Glargine/ Lixisenatide Fixed Ratio Combination Compared to Insulin Glargine Alone and Lixisenatide Alone on Top of Metformin in Patients With T2DM

NCT02058147Phase 3COMPLETED
Sponsor

Sanofi

Enrollment

1,170

Started

2014

Primary outcome

Change in HbA1c From Baseline to Week 30

Type 2 Diabetes

A Study of the Safety and Efficacy of Omarigliptin (MK-3102) Compared With Glimepiride in Participants With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Metformin (MK-3102-016)

NCT01682759Phase 3COMPLETED
Sponsor

Merck Sharp & Dohme LLC

Enrollment

751

Started

2012

Primary outcome

Change From Baseline in Hemoglobin A1C at Week 54

Type 2 Diabetes Mellitus

Randomized Sitagliptin Withdrawal Study (MK-0431-845)

NCT02738879Phase 3COMPLETED
Sponsor

Merck Sharp & Dohme LLC

Enrollment

746

Started

2016

Primary outcome

Change From Baseline in A1C at Week 30

Type 2 Diabetes Mellitus

Efficacy and Safety of the Insulin Glargine/Lixisenatide Fixed Ratio Combination (LixiLan) to Insulin Glargine Alone on Top of Oral Anti-diabetic Drugs (OADs) With Type 2 Diabetes in Japan

NCT02752828Phase 3COMPLETED
Sponsor

Sanofi

Enrollment

521

Started

2016

Primary outcome

Change from baseline in HbA1c

Type 2 Diabetes Mellitus

Comparison of SAR342434 to Humalog as the Rapid Acting Insulin in Adult Patients With Type 2 Diabetes Mellitus Also Using Insulin Glargine

NCT02294474Phase 3COMPLETED
Sponsor

Sanofi

Enrollment

505

Started

2015

Primary outcome

Change in HbA1c From Baseline to Week 26

Type 2 Diabetes Mellitus

Comparison of the Efficacy and Safety of Insulin Glargine/Lixisenatide Fixed Ratio Combination to Insulin Glargine in Patients With Type 2 Diabetes Insufficiently Controlled on Basal Insulin

NCT03798080Phase 3COMPLETED
Sponsor

Sanofi

Enrollment

426

Started

2019

Primary outcome

Change in HbA1c

Type 2 Diabetes Mellitus

Insulin Glargine Combination Therapies in Type II Diabetics

NCT00783744Phase 3COMPLETED
Sponsor

Sanofi

Enrollment

375

Started

2001

Primary outcome

Frequency of subjects with HbA1c ≤ 7.0 % and > 7.0 %

Diabetes Mellitus, Type 2

A Study of Dulaglutide in Japanese Participants With Type 2 Diabetes Mellitus

NCT01584232Phase 3COMPLETED
Sponsor

Eli Lilly and Company

Enrollment

361

Started

2012

Primary outcome

Change From Baseline in Glycosylated Hemoglobin (HbA1c) at 26 Weeks

Type 2 Diabetes Mellitus

Comparison of Insulin Detemir Plus Insulin Aspart Against Insulin Glargine Plus Insulin Aspart in Type 2 Diabetes

NCT00097084Phase 3COMPLETED
Sponsor

Novo Nordisk A/S

Enrollment

324

Started

2004

Primary outcome

HbA1c

DiabetesDiabetes Mellitus, Type 2

Efficacy and Safety of Soliqua Versus Lantus in Ethnically/Racially Diverse Patients With Type 2 Diabetes Mellitus Inadequately Controlled on Basal Insulin and Oral Antidiabetic Agents

NCT03434119Phase 3TERMINATED
Sponsor

Sanofi

Enrollment

241

Started

2018

Primary outcome

Change From Baseline in Glycated Hemoglobin (HbA1c) at Week 26

Type 2 Diabetes Mellitus

20 Week Bridging Study in Type II DM

NCT00563225Phase 3COMPLETED
Sponsor

Sanofi

Enrollment

90

Started

2002

Primary outcome

To evaluate safety & efficacy of Insulin glargine ( injection at bedtime, once a day) on the changes of HbA1c.

Diabetes Mellitus Type II

Trial to Compare NNC0123-0000-0338 in a Tablet Formulation and Insulin Glargine in Subjects With Type 2 Diabetes Currently Treated With Oral Antidiabetic Therapy

NCT02470039Phase 2COMPLETED
Sponsor

Novo Nordisk A/S

Enrollment

50

Started

2015

Primary outcome

Change in fasting plasma glucose (FPG)

DiabetesDiabetes Mellitus, Type 2

PK/PD Biosimilarity Study of Gan & Lee Insulin Glargine Injection vs.US & EU Lantus® in Type 1 Diabetes Mellitus Patients

NCT04236895Phase 1COMPLETED
Sponsor

Gan and Lee Pharmaceuticals, USA

Enrollment

114

Started

2018

Primary outcome

PK endpoint

Diabetes Mellitus, Type 1

A Trial Investigating the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Subcutaneous NNC0123-0338 in Healthy Subjects and in Subjects With Type 1 Diabetes Mellitus

NCT02220296Phase 1COMPLETED
Sponsor

Novo Nordisk A/S

Enrollment

62

Started

2014

Primary outcome

Incidence of adverse events

HealthyDiabetesDiabetes Mellitus, Type 1

A Trial Comparing the Effect of Exercise on Blood Glucose in Subjects With Type 1 Diabetes, Who Are Treated With Either Insulin Degludec or Insulin Glargine

NCT01704417Phase 1COMPLETED
Sponsor

Novo Nordisk A/S

Enrollment

40

Started

2012

Primary outcome

BGpre-exe - BGminimum,exe, difference between blood glucose concentration before exercise and the minimum blood glucose concentration observed during exercise

DiabetesDiabetes Mellitus, Type 1

A Study To Compare the Effects of Insulin Peglispro and Glargine on Insulin Sensitivity and Meal Time Insulin Requirements in Type 2 Diabetics

NCT02197520Phase 1COMPLETED
Sponsor

Eli Lilly and Company

Enrollment

24

Started

2014

Primary outcome

Pharmacodynamics (PD): Average Glucose Infusion Rate From Euglycemic 2-step Hyperinsulinemic Clamp (M-value)

Diabetes Mellitus, Type 2

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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