Insulin Glulisine: An Evaluation of Its Pharmacodynamic Properties and Clinical Application

Helms, Kristen L.; Kelley, Kristi W.

doi:10.1345/aph.1e662

Cited by 20 publications

(11 citation statements)

References 27 publications

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“…Superiority in improvement of glycemic control and reduction of frequency hypoglycemia in our patients after using GLU as compared with previous Caucasian studies has some possible explanations. First, Japanese meals are known to traditionally have a higher carbohydrate energy ratio and a lower fat energy ratio than meals in Western countries.…”

Section: Discussionsupporting

confidence: 38%

Efficacy and safety of switching to insulin glulisine from other rapid‐acting insulin analogs in children with type 1 diabetes

Urakami

Kuwabara

Habu

et al. 2014

J of Diabetes Invest

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We investigated the efficacy and safety of switching to insulin glulisine (GLU) from other rapid-acting insulin analogs (Ra) in children with type 1 diabetes treated with multiple daily injections of insulin or continuous subcutaneous insulin infusion. A total of 26 children with type 1 diabetes were included. Ra in all of these patients was changed to GLU, and they were observed for a 6-month period after having previously finished treatment with other Ra. The mean glycated hemoglobin value decreased from 7.6 ± 1.0 to 7.4 ± 0.9% (P = 0.0034), and mean plasma glucose values after breakfast and supper also improved from 183 ± 50 to 153 ± 32 mg/dL (P = 0.0035), and from 203 ± 29 to 164 ± 23 mg/dL (P < 0.0001), respectively. Furthermore, the mean frequency of hypoglycemia was reduced from 7 ± 6 to 4 ± 4/month (P = 0.0004), while insulin doses and obesity degree were stable with statistically non-significant differences. In conclusion, switching to GLU might be a good treatment option for improving glycemic control in children with type 1 diabetes.

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Section: Discussionsupporting

confidence: 38%

Efficacy and safety of switching to insulin glulisine from other rapid‐acting insulin analogs in children with type 1 diabetes

Urakami

Kuwabara

Habu

et al. 2014

J of Diabetes Invest

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“…In the few direct reported comparisons of rapid‐acting analogues in clinical trials, they appear to show equivalent glycaemic control and frequency of hypoglycaemia [67–72]. During a 26‐week study in which 672 people with type 1 diabetes were randomized to insulin lispro or insulin glulisine, the mean change in HbA 1c was −0.1% (1 mmol/mol) in both treatment groups, and there was no difference in reported hypoglycaemia [67].…”

Section: Methodsmentioning

confidence: 99%

“…In another randomized comparison of insulin lispro and insulin glulisine, mean HbA 1c increased by 0.1% (1 mmol/mol) in the glulisine group (n = 132) and by 0.0% (0 mmol/mol) in the insulin lispro group (n = 135) with a similar safety profile after 28 weeks [68]. Comparisons between insulin aspart, insulin lispro and insulin glulisine when delivered by continuous subcutaneous insulin infusion in adults and children with type 1 diabetes indicate that the rapid‐acting analogues are equally effective at reducing blood glucose, and equally safe [69–73].…”

Section: Methodsmentioning

confidence: 99%

The pharmacokinetics and pharmacodynamics of rapid‐acting insulin analogues and their clinical consequences

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2012

Diabetes Obesity Metabolism

179

152

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Postprandial glucose excursions can inhibit achievement of good glycaemic control, and possibly have a specific effect on the risk of vascular comorbidities. Rapid-acting analogues control these excursions better than human insulin because their pharmacokinetic/pharmacodynamic (PK/PD) profile is closer to that of meal-time endogenous insulin secretion. Review of the findings of PK/PD studies and clinical trials suggests that the three marketed rapid-acting analogues--insulin lispro, insulin aspart and insulin glulisine--are equally efficacious and safe. In comparison with human insulin when using the same basal insulin, they provide comparable glycaemic control with a reduced risk of hypoglycaemia, although the combination of rapid-acting and basal analogues reduces glycated haemoglobin (HbA(1c)) more than human meal-time insulin combined with neutral protamine Hagedorn (NPH) insulin. Some studies have suggested that insulin glulisine has a slightly faster onset of action compared with insulin lispro or insulin aspart, but this has not been translated into demonstrable clinical benefit. Treatment satisfaction in patients with diabetes has been higher when therapy with a rapid-acting analogue is used instead of human insulin, perhaps due to differences in advised timing of injection. The largest benefits in efficacy, hypoglycaemia incidence, treatment satisfaction and quality of life have occurred when patients receive an all-analogue meal-time plus basal regimen as compared with an all-human insulin regimen. No new safety issues have been identified with the marketed rapid-acting analogues, and their insulin-like growth factor 1 receptor affinity and mitogenic activity are comparable to human insulin.

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“…Whereas mutational disruption of structure generally represents a straightforward task, a specific subset of such substitutions was sought based on three functional criteria: compatibility with high‐affinity binding to the insulin receptor, retention of native biological activity in vivo , and amenability to stable pharmaceutical formulation. There are three such rapid‐acting analogs in current use (Table 1B); in chronological order of clinical introduction, these are insulin lispro (the active component of Humalog®; Eli Lilly and Co., Indianapolis, IN), 22 insulin aspart (NovoLog®; Novo‐Nordisk), 23,24 and insulin glulisine (Apidra®; Sanofi‐Aventis) 25,26 . These products have been proven safe and effective in multi‐injection regimens 7,27 and for use in continuous subcutaneous infusion devices (insulin pumps) 28 .…”

Section: Insulin and Analogsmentioning

confidence: 99%

Insulin analogs for the treatment of diabetes mellitus: therapeutic applications of protein engineering

Berenson

Weiss

Wan

et al. 2011

Annals of the New York Academy of Sciences

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The engineering of insulin analogs represents a triumph of structure-based protein design. A framework has been provided by structures of insulin hexamers. Containing a zinc-coordinated trimer of dimers, such structures represent a storage form of the active insulin monomer. Initial studies focused on destabilization of subunit interfaces. Because disassembly facilitates capillary absorption, such targeted destabilization enabled development of rapid-acting insulin analogs. Converse efforts were undertaken to stabilize the insulin hexamer and promote higher-order self-assembly within the subcutaneous depot toward the goal of enhanced basal glycemic control with reduced risk of hypoglycemia. Current products either operate through isoelectric precipitation (insulin glargine, the active component of Lantus®; Sanofi-Aventis) or employ an albumin-binding acyl tether (insulin detemir, the active component of Levemir®; Novo-Nordisk). To further improve pharmacokinetic properties, modified approaches are presently under investigation. Novel strategies have recently been proposed based on subcutaneous supramolecular assembly coupled to (a) large-scale allosteric reorganization of the insulin hexamer (the TR transition), (b) pH-dependent binding of zinc ions to engineered His-X3-His sites at hexamer surfaces, or (c) the long-range vision of glucose-responsive polymers for regulated hormone release. Such designs share with wild-type insulin and current insulin products a susceptibility to degradation above room temperature, and so their delivery, storage, and use require the infrastructure of an affluent society. Given the global dimensions of the therapeutic supply chain, we envisage that concurrent engineering of ultra-stable protein analog formulations would benefit underprivileged patients in the developing world.

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Insulin Glulisine: An Evaluation of Its Pharmacodynamic Properties and Clinical Application

Cited by 20 publications

References 27 publications

Efficacy and safety of switching to insulin glulisine from other rapid‐acting insulin analogs in children with type 1 diabetes

Efficacy and safety of switching to insulin glulisine from other rapid‐acting insulin analogs in children with type 1 diabetes

The pharmacokinetics and pharmacodynamics of rapid‐acting insulin analogues and their clinical consequences

Insulin analogs for the treatment of diabetes mellitus: therapeutic applications of protein engineering

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