Overview
Insulin glulisine is a short-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is typically prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas that promotes glucose metabolism. Insulin is released from the pancreas following a meal to promote the uptake of glucose from the blood into internal organs and tissues such as the liver, fat cells, and skeletal muscle. Absorption of glucose into cells allows for its transformation into glycogen or fat for storage. Insulin also inhibits hepatic glucose production, enhances protein synthesis, and inhibits lipolysis and proteolysis among many other functions. Insulin is an important treatment in the management of Type 1 Diabetes (T1D) which is caused by an autoimmune reaction that destroys the beta cells of the pancreas, resulting in the body not being able to produce or synthesize the insulin needed to manage circulating blood sugar levels. As a result, people with T1D rely primarily on exogenous forms of insulin, such as insulin glulisine, to lower glucose levels in the blood. Insulin is also used in the treatment of Type 2 Diabetes (T2D), another form of diabetes mellitus that is a slowly progressing metabolic disorder caused by a combination of genetic and lifestyle factors that promote chronically elevated blood sugar levels. Without treatment or improvement in non-pharmacological measures such as diet and exercise to lower blood glucose, high blood sugar eventually causes cellular resistance to endogenous insulin, and in the long term, damage to pancreatic islet cells. Insulin is typically prescribed later in the course of T2D, after trying several oral medications such as Metformin, Gliclazide, or Sitagliptin have been tried, when sufficient damage has been caused to pancreatic cells that the body is no longer able to produce insulin on its own. Marketed as the brand name product Apidra, insulin glulisine begins to exert its effects within 15 minutes of subcutaneous administration, while peak levels occur 30 to 90 minutes after administration. Due to its duration of action of around 5 hours, Apidra is considered "bolus insulin" as it provides high levels of insulin in a short period of time to mimic the release of endogenous insulin from the pancreas after meals. Bolus insulin is often combined with once daily, long-acting "basal insulin" such as Insulin detemir, Insulin degludec, and Insulin glargine to provide low concentrations of background insulin that can keep blood sugar stable between meals or overnight. Use of basal and bolus insulin together is intended to mimic the pancreas' production of endogenous insulin, with a goal of avoiding any periods of hypoglycemia. Insulin glulisine is a biosynthetic, rapid-acting human insulin analogue produced in a non-pathogenic laboratory strain of Escherichia coli (K12). This recombinant hormone differs from native human insulin in that the amino acid asparagine at position B3 is replaced by lysine and the lysine at position B29 is replaced by glutamic acid. These structural modifications decrease hexamer formation, stabilize insulin glulisine monomers and increase the rate of absorption and onset of action compared to human insulin. Without an adequate supply of insulin to promote absorption of glucose from the bloodstream, blood sugar levels can climb to dangerously high levels and can result in symptoms such as fatigue, headache, blurred vision, and increased thirst. If left untreated, the body starts to break down fat, instead of glucose, for energy which results in a build-up of ketone acids in the blood and a syndrome called ketoacidosis, which is a life-threatening medical emergency. In the long term, elevated blood sugar levels increase the risk of heart attack, stroke, and diabetic neuropathy.
Indication
用于治疗成人糖尿病。
Associated Conditions
- Diabetes Mellitus
- Type 1 Diabetes Mellitus
- Hyperglycemia during critical illness
Research Report
A Comprehensive Clinical and Pharmacological Review of Insulin Glulisine (Apidra®): From Molecular Engineering to Clinical Practice
Section 1: Introduction and Drug Profile
1.1 Overview and Classification
Insulin glulisine is a rapid-acting, biosynthetic human insulin analog developed for the management of diabetes mellitus.[1] It is classified as a prandial or "bolus" insulin, specifically engineered to control postprandial glycemic excursions in individuals with Type 1 or Type 2 diabetes.[2] The drug is produced as a biotech product through recombinant DNA technology, utilizing a non-pathogenic laboratory strain of
Escherichia coli (K12) as the production organism.[2] Developed and marketed by Sanofi-Aventis, insulin glulisine is sold under the brand names Apidra® and Apidra SoloStar®, the latter referring to a prefilled disposable pen delivery system.[1] Its primary role in diabetes management is to mimic the physiological surge of endogenous insulin that occurs in response to a meal, thereby facilitating the cellular uptake and metabolism of glucose.[2]
1.2 Regulatory and Development History
The development of insulin glulisine by Sanofi-Aventis (formerly Aventis Pharmaceuticals Inc.) culminated in its initial approval by the U.S. Food and Drug Administration (FDA) on April 16, 2004, for the treatment of adults with Type 1 and Type 2 diabetes mellitus.[1] This marked the introduction of a third rapid-acting insulin analog to the market, offering clinicians and patients another option for mealtime insulin therapy.[10]
Following its initial approval, the clinical utility of insulin glulisine was systematically expanded through a series of subsequent regulatory milestones. This strategic approach to lifecycle management broadened its applicability across diverse patient populations and clinical settings. Key developments include:
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2019/10/11 | Phase 4 | UNKNOWN | Medical University of Warsaw | ||
2019/07/15 | Phase 4 | Completed | Medical University of Warsaw | ||
2017/12/02 | Phase 4 | Completed | |||
2017/11/01 | Phase 4 | Completed | Fundación Pública Andaluza para la Investigación de Málaga en Biomedicina y Salud | ||
2016/09/26 | Phase 4 | Completed | Kinderkrankenhaus auf der Bult | ||
2016/09/22 | Phase 1 | Completed | |||
2016/02/18 | Phase 4 | UNKNOWN | Medical University of Warsaw | ||
2015/07/21 | Phase 2 | Terminated | |||
2015/05/04 | Phase 1 | Completed | |||
2014/10/28 | Phase 4 | Completed | Medical University of Warsaw |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
sanofi-aventis U.S. LLC | 0088-2500 | SUBCUTANEOUS, INTRAVENOUS | 100 [iU] in 1 mL | 11/1/2022 | |
sanofi-aventis U.S. LLC | 0088-2502 | SUBCUTANEOUS | 100 [iU] in 1 mL | 11/1/2022 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
---|---|---|---|
Authorised | 9/27/2004 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
Apidra SoloStar 100 Units/ml Solution for injection in a pre-filled pen | SIN13432P | INJECTION, SOLUTION | 3.49 mg (100 Units) | 3/20/2008 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
---|---|---|---|---|---|
No NMPA approvals found for this drug. |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
---|---|---|---|---|---|
No PPB approvals found for this drug. |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
---|---|---|---|---|---|
APIDRA insulin glulisine (rbe) 100IU/mL 10mL injection vial | 99145 | Medicine | A | 5/2/2005 | |
APIDRA insulin glulisine (rbe) 100IU/mL 3mL injection cartridge | 99146 | Medicine | A | 5/2/2005 | |
APIDRA SOLOSTAR insulin glulisine (rbe) 100IU/mL 3mL solution for injection injector pen | 132816 | Medicine | A | 11/28/2006 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
---|---|---|---|---|---|
APIDRA | sanofi-aventis canada inc | 02279460 | Solution - Subcutaneous | 100 UNIT / ML | 9/22/2008 |
APIDRA | sanofi-aventis canada inc | 02279479 | Solution - Subcutaneous | 100 UNIT / ML | 10/1/2009 |
APIDRA | sanofi-aventis canada inc | 02279487 | Solution - Subcutaneous | 100 UNIT / ML | N/A |
APIDRA | sanofi-aventis canada inc | 02294346 | Solution - Subcutaneous | 100 UNIT / ML | 9/22/2008 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
---|---|---|---|---|---|
APIDRA 100 UNIDADES/ML SOLUCION INYECTABLE EN VIAL | 04285001 | SOLUCIÓN INYECTABLE | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Not Commercialized | |
APIDRA 100 UNIDADES/ML SOLUCION INYECTABLE EN CARTUCHO | 04285008 | SOLUCIÓN INYECTABLE EN CARTUCHO | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Commercialized | |
APIDRA 100 UNIDADES/ML,SOLOSTAR SOLUCION INYECTABLE EN PLUMA PRECARGADA | 04285032 | SOLUCIÓN INYECTABLE EN PLUMA PRECARGADA | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Commercialized | |
APIDRA 100 UNIDADES/ml OPTICLIK SOLUCION INYECTABLE EN CARTUCHO | 04285024 | SOLUCIÓN INYECTABLE EN CARTUCHO | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Not Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Philippines FDA approvals found for this drug. |
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Saudi SFDA approvals found for this drug. |
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Malaysia NPRA approvals found for this drug. |
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
---|---|---|---|---|---|
No UK EMC drug information found for this drug. |
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