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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

baSal BoluS Therapy in patIenTs With TypE 1 Diabetes Mellitus

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 1
Interventions
First Posted Date
2010-09-17
Last Posted Date
2014-03-17
Lead Sponsor
Sanofi
Target Recruit Count
206
Registration Number
NCT01204593
Locations
🇩🇿

Investigational Site Number 01202, Algiers, Algeria

🇦🇷

Investigational Site Number 03201, Caba, Argentina

🇿🇦

Investigational Site Number 12468, Benoni, South Africa

and more 40 locations

Intensive Insulin Glulisine Therapy in Patients With Type 2 Diabetes Inadequately Controlled With Basal Insulin and Oral Glucose-lowering Drugs

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 2
Interventions
First Posted Date
2010-09-16
Last Posted Date
2012-08-30
Lead Sponsor
Sanofi
Target Recruit Count
207
Registration Number
NCT01203111
Locations
🇻🇪

Administrative office, Caracas, Venezuela

Apidra Children & Adolescents Study

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 1
Interventions
First Posted Date
2010-09-15
Last Posted Date
2012-12-18
Lead Sponsor
Sanofi
Target Recruit Count
100
Registration Number
NCT01202474
Locations
🇷🇺

Administrative office, Moscow, Russian Federation

Safety/Efficacy Study of Subcutaneously Injected Prandial Insulins Compared to Insulin Lispro Alone in Patients With Type 2 Diabetes Mellitus

First Posted Date
2010-09-02
Last Posted Date
2014-08-20
Lead Sponsor
Halozyme Therapeutics
Target Recruit Count
132
Registration Number
NCT01194258
Locations
🇺🇸

Mercury Street Medical, Butte, Montana, United States

🇺🇸

UT Southwestern Medical Center at Dallas, Dallas, Texas, United States

🇺🇸

John Muir Physician Network Clinical Research Center, Concord, California, United States

and more 19 locations

Safety/Efficacy Study of Subcutaneously Injected Prandial Insulins Compared to Insulin Lispro Alone in Participants With Type 1 Diabetes Mellitus

First Posted Date
2010-09-02
Last Posted Date
2019-02-26
Lead Sponsor
Halozyme Therapeutics
Target Recruit Count
135
Registration Number
NCT01194245
Locations
🇺🇸

Mercury Street Medical, Butte, Montana, United States

🇺🇸

Mid-America Diabetes Associates, Wichita, Kansas, United States

🇺🇸

Rocky Mountain Diabetes and Osteoporosis Center, Idaho Falls, Idaho, United States

and more 16 locations

Pharmacodynamic and Pharmacokinetic Effects of Insulin Glulisine in Obese Subjects With Type 2 Diabetes After a Standard Meal in Comparison to Insulin Aspart

Phase 1
Completed
Conditions
Type 2 Diabetes Mellitus
Interventions
First Posted Date
2010-07-09
Last Posted Date
2010-07-16
Lead Sponsor
Sanofi
Target Recruit Count
37
Registration Number
NCT01159353
Locations
🇫🇷

Sanofi-Aventis Administrative Office, Paris, France

Diabetes in the Elderly: Prospective Study

Phase 4
Completed
Conditions
Diabetes
Hyperglycemia
Interventions
First Posted Date
2010-05-26
Last Posted Date
2014-12-31
Lead Sponsor
Guillermo Umpierrez
Target Recruit Count
150
Registration Number
NCT01131052
Locations
🇺🇸

Guillermo Umpierrez, Atlanta, Georgia, United States

Evaluation of the Safety and Efficacy of Insulin Glargine + Glulisine or Insulin Regular + NPH Insulin (Isophane Insulin) Use in Type 2 Diabetes Mellitus Patients With Moderate Renal Failure.

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 2
Interventions
Drug: NPH insulin (insulin isophane)
Drug: Regular insulin
First Posted Date
2010-05-13
Last Posted Date
2013-11-08
Lead Sponsor
Sanofi
Target Recruit Count
72
Registration Number
NCT01122979
Locations
🇧🇷

Investigational Site Number 076-013, São Paulo, Brazil

🇧🇷

Investigational Site Number 076-007, Curitiba, Brazil

🇧🇷

Investigational Site Number 076-005, São Paulo, Brazil

and more 7 locations

Insulins Glargine and gluLisine strAtegy Versus Premixed Insulin strAteGy: a cOmparative Study

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 2
Interventions
First Posted Date
2010-05-12
Last Posted Date
2013-04-04
Lead Sponsor
Sanofi
Target Recruit Count
934
Registration Number
NCT01121835
Locations
🇨🇴

Investigational Site Number 170003, Bucaramanga, Colombia

🇨🇴

Investigational Site Number 170004, Pereira, Colombia

🇨🇳

Investigational Site Number 156012, Haikou, China

and more 93 locations

Insulin Glargine for Diabetes Metabolism(DM)Type II Patients Under Enteral Nutrition

Phase 4
Terminated
Conditions
Diabetes Mellitus, Type 2
Interventions
First Posted Date
2010-03-05
Last Posted Date
2012-03-27
Lead Sponsor
Sanofi
Target Recruit Count
15
Registration Number
NCT01081938
Locations
🇧🇷

Sanofi-Aventis Investigational Site Number 076-007, Belo Horizonte, Brazil

🇧🇷

Sanofi-Aventis Investigational Site Number 076-004, Porto Alegre, Brazil

🇧🇷

Sanofi-Aventis Investigational Site Number 076-006, São José do Rio Preto, Brazil

and more 7 locations
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