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Insulin Glulisine

Generic Name
Insulin Glulisine
Brand Names
Apidra
Drug Type
Biotech
CAS Number
207748-29-6
Unique Ingredient Identifier
7XIY785AZD
Background

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

Gulf, Lantus, Apidra Evaluation in Type 1 Diabetics Study

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 1
Interventions
First Posted Date
2007-10-04
Last Posted Date
2009-09-25
Lead Sponsor
Sanofi
Target Recruit Count
98
Registration Number
NCT00539448
Locations
🇦🇪

Sanofi-aventis administrative office, Dubai, United Arab Emirates

🇶🇦

Sanofi-Aventis Administrative Office, Doha, Qatar

Study of Safety and Effectiveness of Apidra® in Combination With Basal Insulin in Patients With Type 1 & 2 Diabetes Mellitus

Phase 4
Completed
Conditions
Diabetes Mellitus
First Posted Date
2007-09-10
Last Posted Date
2010-09-13
Lead Sponsor
Sanofi
Target Recruit Count
188
Registration Number
NCT00526513
Locations
🇪🇬

Sanofi-Aventis Administrative Office, Cairo, Egypt

APIDRA Registration Study

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 1
First Posted Date
2007-06-21
Last Posted Date
2009-03-16
Lead Sponsor
Sanofi
Target Recruit Count
45
Registration Number
NCT00489190
Locations
🇰🇿

Sanofi-Aventis, Almaty, Kazakhstan

Insulin Therapy in Chronic Obstructive Pulmonary Disease (COPD) Exacerbations

Not Applicable
Terminated
Conditions
Chronic Obstructive Pulmonary Disease
Hyperglycemia
Interventions
Procedure: Blood glucose monitoring
First Posted Date
2007-04-30
Last Posted Date
2009-10-02
Lead Sponsor
The Royal Bournemouth Hospital
Target Recruit Count
51
Registration Number
NCT00467636
Locations
🇬🇧

Royal Bournemouth Hospital, Bournemouth, Dorset, United Kingdom

Insulin Glulisine, Insulin Lispro and Insulin Glargine in Type 1 or 2 Diabetes Mellitus

Phase 3
Completed
Conditions
Diabetes Mellitus
Interventions
First Posted Date
2007-04-30
Last Posted Date
2009-09-15
Lead Sponsor
Sanofi
Target Recruit Count
485
Registration Number
NCT00467376
Locations
🇨🇳

Sanofi-Aventis, Beijing, China

Insulin Glulisine, Diabetes Mellitus Type 1

Phase 3
Completed
Conditions
Diabetes Mellitus, Type 1
Interventions
First Posted Date
2006-11-09
Last Posted Date
2009-09-18
Lead Sponsor
Sanofi
Target Recruit Count
104
Registration Number
NCT00397553
Locations
🇷🇺

Sanofi-Aventis, Moscow, Russian Federation

Insulin Glargine "All to Target" Trial

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 2
Interventions
First Posted Date
2006-10-04
Last Posted Date
2011-05-06
Lead Sponsor
Sanofi
Target Recruit Count
588
Registration Number
NCT00384085
Locations
🇺🇸

Sanofi-Aventis Administrative Office, Bridgewater, New Jersey, United States

Dose-Exposure-Response in Type 1 Diabetes Mellitus

Phase 1
Completed
Conditions
Diabetes Mellitus, Type I
First Posted Date
2006-08-24
Last Posted Date
2006-08-24
Lead Sponsor
Sanofi
Target Recruit Count
18
Registration Number
NCT00368394
Locations
🇩🇪

Sanofi-Aventis, Neuss, Germany

Insulin Glulisine in Type 2 Diabetic Patients

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 2
Interventions
First Posted Date
2006-08-07
Last Posted Date
2011-08-08
Lead Sponsor
Sanofi
Target Recruit Count
106
Registration Number
NCT00360698
Locations
🇷🇺

Sanofi-Aventis, Moscow, Russian Federation

🇬🇧

Sanofi-aventis, Guildford, United Kingdom

Insulin Glulisine in Healthy Lean and Obese Subjects

Phase 1
Completed
Conditions
Diabetes Mellitus
First Posted Date
2006-04-05
Last Posted Date
2009-12-07
Lead Sponsor
Sanofi
Registration Number
NCT00311077
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