TY - DATA T1 - A randomized study investigating the effect of omeprazole on the pharmacokinetics of oral semaglutide PY - 2018/08/10 AU - Tine A. Bækdal AU - Astrid Breitschaft AU - Andrea Navarria AU - Cilie W. Hansen UR - https://tandf.figshare.com/articles/dataset/A_randomized_study_investigating_the_effect_of_omeprazole_on_the_pharmacokinetics_of_oral_semaglutide/6727043 DO - 10.6084/m9.figshare.6727043.v4 L4 - https://ndownloader.figshare.com/files/12750887 L4 - https://ndownloader.figshare.com/files/12302573 L4 - https://ndownloader.figshare.com/files/12302576 KW - GLP-1 receptor agonists KW - semaglutide KW - pharmacokinetics KW - omeprazole KW - drug interactions N2 - Background: Since the first oral glucagon-like peptide-1 analog comprises semaglutide co-formulated with an absorption enhancer, sodium N-(8-[2-hydroxybenzoyl] amino) caprylate, which induces a transient, localized increase in gastric pH, we have investigated whether a proton pump inhibitor affects the pharmacokinetics of oral semaglutide. Research design and methods: A single-center, randomized, open-label, parallel-group trial investigated pharmacokinetic interactions of oral semaglutide with omeprazole (40 mg once-daily) in 54 healthy subjects. Primary endpoints were area under the plasma concentration-time curve over 24 h for semaglutide (AUC0−24h,semaglutide,Day10) and maximum concentration of semaglutide (Cmax,semaglutide,Day10) at day 10. Results: Exposure of semaglutide appeared to be slightly increased, although not statistically significantly, with oral semaglutide plus omeprazole versus oral semaglutide alone (AUC0−24h,semaglutide,Day10 [estimated treatment ratio 1.13; 90%CI 0.88, 1.45] and Cmax,semaglutide,Day10 [estimated treatment ratio 1.16; 90%CI 0.90, 1.49]). Gastric pH was higher with oral semaglutide and omeprazole versus oral semaglutide alone. Adverse events were mild or moderate and, most commonly, gastrointestinal disorders. Conclusions: There was a slight non-statistically significant increase in semaglutide exposure when oral semaglutide was administered with omeprazole, but this is not considered clinically relevant and no dose adjustment is likely to be required. ER -