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Oral semaglutide – Rybelsus®, the first GLP-1 receptor agonist for oral use in clinical practice


Authors: David Karásek
Authors place of work: III. Interní klinika – nefrologická, revmatologická a endokrinologická, LF UP a FN Olomouc
Published in the journal: Vnitř Lék 2022; 68(2): 89-95
Category: Main Topic

Summary

Glucagon like peptide-1 receptor agonists (GLP-1 RA) are potent antidiabetic drugs associated with significant weight loss and minimal risk of hypoglycemia. Semaglutide is a GLP-1 RA with a proven cardiovascular benefit. It is currently also available in oral form, which is especially suitable for the treatment of the initial phase of type 2 diabetes. However, it is also effective at later initiation of therapy, in different diabetic populations. The PIONEER 6 trial demonstrated cardiovascular safety of oral semaglutide, its administration was accompanied by a significant reduction in cardiovascular and overall mortality.

Keywords:

type 2 diabetes – glycated hemoglobin – cardiovascular benefit – oral semaglutide


Zdroje

1. American Diabetes Association. 9. Pharmacologic Approaches to Glycemic Treatment: Standards of Medical Care in Diabetes-2021. Diabetes Care 2021;44(Suppl 1):S111-S124.

2. Rasmussen MF. The development of oral semaglutide, an oral GLP-1 analog, for the treatment of type 2 diabetes. Diabetol Int. 2020;11:76-86.

3. Baekdal TA, Thomsen M, Kupčová V et al. Pharmacokinetics, safety, and tolerability of oral semaglutide in subjects with hepatic impairment. J Clin Pharmacol 2018; 58:1314–1323.

4. Granhall C, Sřndergaard FL, Thomsen M et al. Pharmacokinetics, safety and tolerability of oral semaglutide in subjects with renal impairment. Clin Pharmacokinet 2018; 57:1571–1580.

5. Meier JJ, Granhall C, Hoevelmann U et al. Effect of upper gastrointestinal disease on the pharmacokinetics of oral semaglutide in subjects with type 2 diabetes. Diabetes.nd 2019; 68(Suppl 1):1013-P.

6. Bćkdal TA, Breitschaft A, Navarria A, Hansen CW. A randomized study investigating the effect of omeprazole on the pharmacokinetics of oral semaglutide. Expert Opin Drug Metab Toxicol. 2018;14:869–877.

7. Hauge C, Breitschaft A, Hartoft‑Nielsen ML et al. Effect of oral semaglutide on the pharmacokinetics of thyroxine after dosing of levothyroxine and the influence of co‑administered tablets on the pharmacokinetics of oral semaglutide in healthy subjects: an open‑ label, one‑sequence crossover, single‑ center, multiple‑dose, two‑part trial. Expert Opin Drug Metab Toxicol. 2021;17:1139-1148.

8. Davies M, Pieber TR, Hartoft‑Nielsen ML et al. Effect of oral semaglutide compared with placebo and subcutaneous semaglutide on glycemic control in patients with type 2 diabetes: a Randomized Clinical Trial. JAMA 2017;318:1460-1470.

9. Kim YG, Hahn S, Oh TJ et al. Differences in the HbA1c‑ lowering efficacy of glucagon‑like peptide-1 analogues between Asians and non‑Asians: a systematic review and meta‑analysis. Diabetes Obes Metab. 2014;16:900-909.

10. Aroda VR, Rosenstock J, Terauchi Y et al. PIONEER 1 Investigators. PIONEER 1: Randomized Clinical Trial of the Efficacy and Safety of Oral Semaglutide Monotherapy in Comparison With Placebo in Patients With Type 2 Diabetes. Diabetes Care. 2019;42:1724-1732.

11. Zinman B, Aroda VR, Buse JB et al. PIONEER 8 Investigators. Efficacy, Safety, and Tolerability of Oral Semaglutide Versus Placebo Added to Insulin With or Without Metformin in Patients With Type 2 Diabetes: The PIONEER 8 Trial. Diabetes Care 2019;42:2262-2271.

12. Mosenzon O, Blicher TM, Rosenlund S et al. PIONEER 5 Investigators. Efficacy and safety of oral semaglutide in patients with type 2 diabetes and moderate renal impairment (PIONEER 5): a placebo‑ controlled, randomised, phase 3a trial. Lancet Diabetes Endocrinol 2019; 7:515-527. Erratum in: Lancet Diabetes Endocrinol 2019;7:e21.

13. Rosenstock J, Allison D, Birkenfeld AL et al. Effect of additional oral semaglutide vs sitagliptin on glycated hemoglobin in adults with type 2 diabetes uncontrolled with metformin alone or with sulfonylurea: the PIONEER 3 randomized clinical trial. JAMA. 2019; 321:1466-1480.

14. Buse JB, Bode BW, Mertens A, Cho YM et al. PIONEER 7 investigators. Long‑term efficacy and safety of oral semaglutide and the effect of switching from sitagliptin to oral semaglutide in patients with type 2 diabetes: a 52-week, randomized, open‑ label extension of the PIONEER 7 trial. BMJ Open Diabetes Res Care 2020;8:e001649.

15. Rodbard HW, Rosenstock J, Canani LH et al. Oral semaglutide versus empagliflozin in patients with type 2 diabetes uncontrolled on metformin: the PIONEER 2 trial. Diabetes Care 2019;42:2272-2281.

16. Pratley R, Amod A, Hoff ST et al. Oral semaglutide versus subcutaneous liraglutide and placebo in type 2 diabetes (PIONEER 4): a randomised, double-blind, phase 3a trial. Lancet 2019;394:39-50.

17. Husain M, Birkenfeld AL, Donsmark M et al. PIONEER 6 Investigators. Oral Semaglutide and Cardiovascular Outcomes in Patients with Type 2 Diabetes. N Engl J Med 2019;381:841-851.

18. Marso SP, Bain SC, Consoli A et al. SUSTAIN-6 Investigators. Semaglutide and Cardiovascular Outcomes in Patients with Type 2 Diabetes. N Engl J Med 2016;375:1834-1844.

19. Holst JJ, Gromada J. Role of incretin hormones in the regulation of insulin secretion in diabetic and nondiabetic humans. Am J Physiol Endocrinol Metab 2004;287:E199-206.

20. Sharma A, Verma S. Mechanisms by Which Glucagon‑Like‑Peptide- 1 Receptor Agonists and Sodium‑Glucose Cotransporter-2 Inhibitors Reduce Cardiovascular Risk in Adults With Type 2 Diabetes Mellitus. Can J Diabetes. 2020;44:93-102.

21. Rakipovski G, Rolin B, Nøhr J et al. The GLP-1 Analogs Liraglutide and Semaglutide Reduce Atherosclerosis in ApoE-/- and LDLr-/- Mice by a Mechanism That Includes Inflammatory Pathways. JACC Basic Transl Sci 2018;3:844-857.

22. Buse JB, Wexler DJ, Tsapas A et al. 2019 Update to: Management of Hyperglycemia in Type 2 Diabetes, 2018. A Consensus Report by the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD). Diabetes Care 2020; 43:487-493.

23. Dahl K, Brooks A, Almazedi F et al. Oral semaglutide improves postprandial glucose and lipid metabolism, and delays gastric emptying, in subjects with type 2 diabetes. Diabetes Obes Metab 2021;23:1594-1603.

24. Hjerpsted JB, Flint A, Brooks A et al. Semaglutide improves postprandial glucose and lipid metabolism, and delays first‑hour gastric emptying in subjects with obesity. Diabetes Obes Metab 2018;20:610-619.

25. Vergès B, Charbonnel B. After the LEADER trial and SUSTAIN-6, how do we explain the cardiovascular benefits of some GLP-1 receptor agonists? Diabetes Metab 2017; 43 Suppl 1:2S3-2S12.

Štítky
Diabetology Endocrinology Internal medicine
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