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Pharmacokinetics and Clinical Implications of Semaglutide: A New Glucagon-Like Peptide (GLP)-1 Receptor Agonist

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Abstract

Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) came to market in the year 2005, as a new therapeutic classification, for clinical use in the management of type 2 diabetes mellitus (T2DM). Since 2005, there have been six approved products on the market, with the newest product being semaglutide (Novo Nordisk). Several studies have been conducted and completed evaluating its pharmacokinetics as a once-weekly subcutaneous injection. As a dose of 0.5 or 1 mg, semaglutide has a half-life of 7 days; therefore, it would reach steady state in 4–5 weeks. There are few drug interactions and dose adjustments are not necessary. However, similar to other GLP-1 RAs, semaglutide can delay gastric emptying and may impact the absorption of oral medications. Based on clinical trials, semaglutide has been compared with placebo, sitagliptin, exenatide extended release, and insulin glargine as monotherapy or add-on therapy. Semaglutide has resulted in a 1.5–1.9% glycosylated hemoglobin A1c reduction after 30–56 weeks. It also produced 5–10% weight reduction from baseline in clinical efficacy studies. Semaglutide can be another acceptable option for patients with T2DM, and it has a potential role among patients who require weight loss with a low risk of hypoglycemia. This article evaluates the pharmacokinetics of semaglutide and summarizes its application to clinical practice based on efficacy and safety data.

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Correspondence to Jennifer N. Clements.

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No external funding was used in the preparation of this manuscript.

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Sylvie Hall, Diana Isaacs, and Jennifer N. Clements declare they have no conflicts of interest that might be relevant to the contents of this manuscript.

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Hall, S., Isaacs, D. & Clements, J.N. Pharmacokinetics and Clinical Implications of Semaglutide: A New Glucagon-Like Peptide (GLP)-1 Receptor Agonist. Clin Pharmacokinet 57, 1529–1538 (2018). https://doi.org/10.1007/s40262-018-0668-z

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