Background of Insulin Degludec
Insulin degludec is a revolutionary development in the field of Diabetes management, providing improved metabolic control, simplified design, and potentially less hypoglycemia. It is an ultra-long-acting basal insulin analog that has a steepened flat pharmacodynamic profile large, thus enhancing its duration of action.
The Discovery of Insulin Degludec
Insulin degludec was developed by the pharmaceutical company Novo Nordisk and was approved for use in Europe in 2013 and America in 2015. This innovative insulin analog was engineered by linking a 16-carbon fatty acid chain to the B30 amino acid of the insulin molecule through a process referred to as acylation. This modification enables insulin degludec to form soluble multi-hexamers within the subcutaneous injection site, contributing to its stable, protracted action.
Gene Locus and Protein Structure
The native human insulin protein is a small hormone consisting of an A-chain and a B-chain linked together by two disulfide bonds. Insulin degludec mimics this structure with the B30 threonine being substituted with a glutamic acid, onto which a 16-carbon fatty-diacyl chain is attached. This allows it to form multi-hexamers under subcutaneous fat, slowing its absorption and making its effective duration of action longer than 42 hours.
Function of Insulin Degludec
Insulin degludec mimics the function of natural insulin by lowering blood glucose levels. It acts as a substitute for endogenous insulin and is primarily used for the treatment of diabetes mellitus, specifically in patients who require insulin for the control of high blood sugar. Similar to endogenous insulin, it aids the intake of sugar by the cells, stopping them from producing more sugar and reprocessing the sugar available, effectively lowering sugar levels in the blood.
Insulin Degludec-Related Signaling Pathways
Insulin degludec operates via the insulin receptor signaling pathway. After subcutaneous injection, it binds with the insulin receptor, setting off a chain of biochemical processes. The insulin receptor has both an alpha and beta component. While the former is responsible for insulin binding, the latter has tyrosine kinase activity. On insulin binding, autophosphorylation of the receptor takes place, which further activates numerous intracellular processes. This results in increased protein synthesis, cellular proliferation, and transcription modification.
Related Diseases and Role in Disease
Insulin degludec is important in the management of both type 1 and type 2 diabetes. Its prolonged action reduces the risk of hypoglycemia, making degludec a preferred choice over other basal insulins for patients who experience fluctuating blood glucose levels. It helps manage these diseases by providing a stable, persistent insulin level, subsequently reducing blood sugar levels.
Application in Medicine
Beyond just diabetes management, insulin degludec is being investigated for use in other medical applications. Owing to its predictable and consistent glucose-lowering effect, it may also be useful in preventing or managing other conditions associated with hyperglycemia, including, but not limited to, heart disease, obesity, and polycystic ovary syndrome (PCOS).
Drug Candidates Related to Insulin Degludec
Tresiba, Ryzodeg, and Xultophy are some of the drug candidates related to insulin degludec. Tresiba and Ryzodeg are used in the management of diabetes in adults, adolescents, and children aged one year and above. Xultophy is a combination of insulin degludec and liraglutide and is used for the treatment of adults with type 2 diabetes.
In conclusion, insulin degludec proves evidence of the advancements in insulin therapy, facilitating individualized patient management with its extended duration of action and stable profile. Ongoing research promises the potential application in other health conditions, making insulin degludec an important subject of study in current diabetes therapeutics and beyond.