Sticky ABOUT TRESIBA (insulin degludec)

A little bit about insulin Tresiba/degludec from New Developments in the Use of Insulin Mixtures & Analogues for the Problem Diabetic:

Insulin Degludec
Insulin degludec (Tresiba, Novo Nordisk) is a new-generation, ultra-long-acting basal insulin analogue. This latest insulin analogue differs from other long-acting insulin preparations in having a longer half-life, flat time-action profile (less likely to cause hypoglycemia) and less day-to-day variability (less glycemic variability).19-21

Degludec is a neutral, soluble ultra-long-acting insulin that forms large soluble multihexamers at the subcutaneous injection site. Its molecular structure is similar to the human insulin amino acid sequence, apart from deletion of Threonine at position B30 and the addition of a 16-carbon fatty diacid attached to Lysine at position B29 via a glutamic acid spacer.

After SC administration, degludec results in the formation of a subcutaneous depot of soluble multihexamers that results in the slow release of insulin monomers into the systemic circulation. Insulin degludec has an onset of action of 30-90 minutes (similar to insulin glargine and insulin detemir). There is no peak in activity, due to the slow release into systemic circulation. The duration of action of insulin degludec is over 42 hours, unlike the 18 to 26 hours provided by current marketed long-acting insulins such as glargine and detemir. The large molecular size of the degludec multihexamers allows for continuous slow release of insulin with less pharmacodynamic variability and within-subject variability than is seen with the currently available insulin analogs.19-21

In studies in people with type 1 and type 2 diabetes, degludec was demonstrated to provide similar improvements in blood glucose control as glargine or detemir while also reducing the rate of overall and nocturnal hypoglycemia. One study found that degludec’s long duration of action makes it possible to dose the drug at different times each day (i.e., in the morning one day, the evening the next day, the morning the day after that) without sacrificing effectiveness and safety.

Although dosing at roughly the same time each day would make sense for most patients, having the flexibility to vary the time of day when needed could be positive for some patients. In addition, the daily injection time of degludec can be varied to extreme intervals of 24-40 hrs without compromising glycemic control or increasing the risk of hypoglycemia. Therefore, degludec represents an improvement over glargine or detemir that require dosing at the same time each day to maintain sufficient insulin levels in the body and to avoid hypoglycemia.

If all goes according to plan, both degludec and degludecPlus (see below) should be approved in both the US and Europe in the second half of 2012. Obviously, no clinical trials have yet been performed on diabetic cats or dogs. Insulin degludec could potentially provide us with a reliable once-a-day or once-every-other-day therapy for animals with diabetes.

 

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