[ Pharmaceutical Sciences Asia - ONLINE ]
Print ISSN 2586-8195 E-ISSN 2586-8470
[ Journal Abbreviation: Pharm.Sci.Asia ]
Mahidol University Journal of Pharmaceutical Sciences
  FORMER NAME   "Mahidol University Journal of Pharmaceutical Sciences" Published Since 1974

 
Abstracts

DOI: https://doi.org/10.14456/mujps.2017.1Pharm Sci Asia 2017; 44(1), 1-21
 

New ultra-long-acting basal insulin: Insulin degludec

N.J. Paw, N. Suksomboon*

- Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand


Long-acting basal insulin analogs were introduced in clinical practice for more than 10 years ago and designed to provide basal insulin requirement for both Type 1 (T1DM) and Type 2 (T2DM) diabetes mellitus. However, there has been a concern with the existing basal insulin such as insulin glargine 100U (IGla 100U) and insulin determir (IDet) because of the risk of hypoglycemia, weight gain, management complexity and rigid dosing schedule associated with their pharmacokinetic and pharmacodynamic properties. Recently, US Food and Drug Administration (FDA) approved new long-acting basal insulin analog, insulin degludec (IDeg) in 2015. IDeg was derived from human insulin by removal of B30 threonine amino acid residue and acylating the DesB30 at the LysB29 with hexadecandioic acid via a gamma-L-glutamic acid spacer. IDeg has long half-life, providing flat, peakless and stable blood glucose lowering effect when injected once daily. Clinical studies have shown that IDeg is not superior to IGla 100U in antihyperglycemic efficacy but it has significant lower hypoglycemic episode. Moreover, IDeg has less blood glucose variability and broad dosing window with flexible dosing interval. Coformulation of IDeg with Insulin Aspart (IAsp) and Glucagon-like-peptide receptor agonist (GLP-1 agonist) have been designed for basal-bolus administration. They have a benefit of improvement in glycated haemoglobin and reduce the number of daily doses. Overall, IDeg, with its unique pharmacokinetic properties, will provide effective glycemic control while minimizing the risk of hypoglycemia.


Keyword:

Long-acting-basal insulin, Insulin Degludec, Type 1 diabetes mellitus, Type 2 diabetes mellitus, Coformulation, Hypoglycemia




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