Sarah L Anderson1, Trevor R Beutel2, Jennifer M Trujillo3. 1. University of Colorado Skaggs School of Pharmacy & Pharmaceutical Sciences, Department of Clinical Pharmacy, 12850 E. Montview Blvd., Aurora, CO 80045, United States of America. Electronic address: sarah.anderson@cuanschutz.edu. 2. University of Colorado Skaggs School of Pharmacy & Pharmaceutical Sciences, Department of Clinical Pharmacy, 12850 E. Montview Blvd., Aurora, CO 80045, United States of America. Electronic address: Trevor.2.Beutel@cuanschutz.edu. 3. University of Colorado Skaggs School of Pharmacy & Pharmaceutical Sciences, Department of Clinical Pharmacy, 12850 E. Montview Blvd., Aurora, CO 80045, United States of America. Electronic address: Jennifer.Trujillo@cuanschutz.edu.
Abstract
BACKGROUND: Previously, the only available glucagon-like peptide-1 receptor agonists (GLP-1 RA) were injectable. Approval of oral semaglutide (Rybelsus®) represents the first orally available GLP-1 RA. OBJECTIVE: To review the literature and describe pharmacologic, pharmacokinetic, and pharmacodynamics properties; clinical safety; and efficacy of oral semaglutide, a newly approved oral GLP-1 RA. METHODS: A MEDLINE (1995-October 2019) and ClinicalTrials.gov search was conducted using the terms oral semaglutide, semaglutide, PIONEER, and a combination of those terms. Reference citations from publications identified were also reviewed. All English-language studies, including abstracts, evaluating oral semaglutide use in humans were included in this review. CONCLUSIONS: The approval of oral semaglutide (Rybelsus®) represents a paradigm shift in the management of T2D as this is the first FDA-approved oral GLP-1 RA. Oral semaglutide may be an attractive option for patients with T2D who require improved glycemic control, would like to lose weight, and who are not interested in injectable therapy. However, the lack of positive cardiovascular (CV) and renal data are significant limitations to its use.
BACKGROUND: Previously, the only available glucagon-like peptide-1 receptor agonists (GLP-1 RA) were injectable. Approval of oral semaglutide (Rybelsus®) represents the first orally available GLP-1 RA. OBJECTIVE: To review the literature and describe pharmacologic, pharmacokinetic, and pharmacodynamics properties; clinical safety; and efficacy of oral semaglutide, a newly approved oral GLP-1 RA. METHODS: A MEDLINE (1995-October 2019) and ClinicalTrials.gov search was conducted using the terms oral semaglutide, semaglutide, PIONEER, and a combination of those terms. Reference citations from publications identified were also reviewed. All English-language studies, including abstracts, evaluating oral semaglutide use in humans were included in this review. CONCLUSIONS: The approval of oral semaglutide (Rybelsus®) represents a paradigm shift in the management of T2D as this is the first FDA-approved oral GLP-1 RA. Oral semaglutide may be an attractive option for patients with T2D who require improved glycemic control, would like to lose weight, and who are not interested in injectable therapy. However, the lack of positive cardiovascular (CV) and renal data are significant limitations to its use.
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