Insulin degludec

Overview

Insulin degludec (INN/USAN) is an ultralong-acting basal insulin analogue that was developed by Novo under the brand name Tresiba. It is administered via subcutaneous injection to help control the blood sugar level of those with diabetes. It has a duration of action that lasts up to 42 hours (compared to 18 to 26 hours provided by other marketed long-acting insulins such as insulin glargine and insulin detemir), making it a once-daily basal insulin, that is one that provides a base insulin level, as opposed to the fast- and short-acting bolus insulins.[1–4] WP

Insulin degludec is a modified insulin that has one single amino acid deleted in comparison to human insulin, and is conjugated to hexadecanedioic acid via gamma-L-glutamyl spacer at the amino acid lysine at position B29. WP

It is included on the World Health Organization's List of Essential Medicines as an equivalent to insulin glargine. In 2023, it was the 152nd most commonly prescribed medication in the United States, with more than 3 million prescriptions.[5][6][7] WP

Uses, dosage and effects

Medical uses

Insulin degludec is indicated to improve glycemic control in people with diabetes.[8][9] WP

In a meta-analysis involving data from 3 randomized controlled trials having 1171 patients, thrice weekly insulin degludec had similar efficacy as daily insulin glargine injections with regards to the fasting blood glucose reduction, having similar safety and risk of low blood glucose (hypoglycaemia) profile. However the overall HbA1c reduction with thrice weekly insulin degludec injection was marginally lower than that of daily insulin glargine injections. Hence thrice weekly degludec injections can be considered in extremely needle prick phobic patients as a choice for basal insulin therapy.[10] WP

Risks and side effects

Side effects

A significant side effect of insulin therapy is hypoglycemia. A meta-analysis of clinical trials published in July 2012 found 39 to 47.9 events of hypoglycemia (defined as blood glucose <56 mg/dL) per patient year, with higher rates in the more concentrated degludec formulation. Rates of nocturnal hypoglycemia ranged from 3.7 to 5.1 events per patient year. A more recent Cochrane systematic review found there was no significant differences in rates of diurnal, nocturnal hypoglycemia or any other studies outcomes when using insulin degludec as compared to insulin glargine, insulin detemir and NPH insulin for the management of type 1 diabetes in either adults or children.[11][12] WP

Pharmacology

Mechanism of action

Insulin degludec is an ultra-long acting insulin that, unlike insulin glargine, is active at a physiologic pH. The addition of hexadecanedioic acid via an amide linkage to lysine at the B29 position allows for the formation of multi-hexamers in subcutaneous tissues. This allows for the formation of a subcutaneous depot that results in slow insulin release into the systemic circulation.[13][14] WP

Pharmacokinetics

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 reported as being longer than 24 hours.[11][13] WP

Because the half-life is longer than 24 hours, it is approved for daily dosing at any time each day - as long as more than 8 hours has elapsed since the previous dose. A missed dose is advised to be taken as soon as remembered, then return to a normal schedule.[15] WP

History

History

Insulin degludec has been filed for registration in the United States. After the completion of additional cardiac safety studies requested by the US Food and Drug Administration (FDA) in February 2013, it received FDA approval in September 2015 and marketing began in January 2016.[16–19] WP

Chemistry

Harm reduction information

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Sources

1. Journal / agency Committee for Medicinal Products for Human Use. Summary of opinion 1 (initial authorisation): Tresiba. 18 October 2012
2. Journal / agency Klein O, Lynge J, Endahl L, Damholt B, Nosek L, Heise T. Albumin-bound basal insulin analogues (insulin detemir and NN344): comparable time-action profiles but less variability than insulin glargine in type 2 diabetes. Diabetes, Obesity & Metabolism. May 2007. doi:10.1111/j.1463-1326.2006.00685.x · PMID 17391154
3. Journal / agency Haahr H, Heise T. A review of the pharmacological properties of insulin degludec and their clinical relevance. Clinical Pharmacokinetics. September 2014. doi:10.1007/s40262-014-0165-y · PMID 25179915 · PMC4156782
4. Other Tresiba Summary of product characteristics
5. Other The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). 2023
6. Other Top 300 of 2023
7. Other Insulin Degludec Drug Usage Statistics, United States, 2014 - 2023
8. Journal / agency Tresiba- insulin degludec injection, solution. 1 July 2022
9. Journal / agency Tresiba EPAR. 17 September 2018
10. Journal / agency Kamrul-Hasan AB, Borozan S, Fernandez CJ, Dutta D, Nagendra L, Pappachan JM. Thrice-Weekly Insulin Degludec Versus Once-Daily Insulin Glargine in Insulin-Naïve Patients With Type 2 Diabetes Mellitus: A Systematic Review and Meta-Analysis. British Journal of Hospital Medicine. July 2025. doi:10.12968/hmed.2024.0716 · PMID 40705560
11. Journal / agency Wang F, Surh J, Kaur M. Insulin degludec as an ultralong-acting basal insulin once a day: a systematic review. Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy. 2012. doi:10.2147/DMSO.S21979 · PMID 22826637 · PMC3402007
12. Journal / agency Hemmingsen B, Metzendorf MI, Richter B. (Ultra-)long-acting insulin analogues for people with type 1 diabetes mellitus. The Cochrane Database of Systematic Reviews. March 2021. doi:10.1002/14651858.cd013498.pub2 · PMID 33662147 · PMC8094220
13. Journal / agency Nasrallah SN, Reynolds LR. Insulin Degludec, The New Generation Basal Insulin or Just another Basal Insulin?. Clinical Medicine Insights. Endocrinology and Diabetes. 2012. doi:10.4137/CMED.S9494 · PMID 22879797 · PMC3411522
14. Journal / agency Robinson JD, Neumiller JJ, Campbell RK. Can a new ultra-long-acting insulin analogue improve patient care? Investigating the potential role of insulin degludec. Drugs. December 2012. doi:10.2165/11642240-000000000-00000 · PMID 23145524
15. Other Duration of Action
16. Other R&D Pipeline
17. Other Hirschler B. New Novo insulin fails to knock out rival Sanofi. 27 October 2010
18. Journal / agency FDA approves two new drug treatments for diabetes mellitus
19. Other Novo Nordisk Launches Tresiba (insulin degludec injection 200 Units/mL) in the United States

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