Pharmacokinetics of first semaglutid drug in Russian Federation: results of open-label randomized clinical trial

Introduction. Diabetes mellitus is a chronic disease that can impact all aspects of metabolism. Incretin mimetics, such as semaglutide, are a promising group of drugs to treat type 2 diabetes mellitus both through the improvement of glycemic control and additional effects on the cardiovascular system and body weight. The development of a generic semaglutide-containing drug is a burning issue which settlement will increase the availability of semaglutide in the Russian Federation Aim. To study the comparative pharmacokinetics, bioequivalence, safety and tolerability of a semaglutide containing GP40221 and Ozempic® in healthy volunteers. Materials and methods . This open-label, randomized, single-dose, parallel group study assessed the bioequivalence of a single dose of 0.5 mg of the study drugs in healthy male subjects under fasting conditions. The conclusion about the bioequivalence of the brand name drug versus the generic drug was made using the classical approach based on the assessment of 90% confidence intervals of the ratios of geometric means of the primary pharmacokinetic parameters (AUC 0-t , С max ) for the active substance of the study drugs. Results. The results of the study showed that the 90% CI values of the ratios of geometric means of the primary PK parameters of semaglutide were 85.96–109.01% and 89.14–111.40% for AUC 0-t и C max , respectively, and are well within acceptable limits 80.00–125.00%. The comparable safety of the study drugs containing semaglutide has been proven. Conclusion. Thus, GP40221 (GEROPHARM LLC, Russia) and Ozempic® (Novo Nordisk A/S, Denmark) can be considered bioequivalent and equally safe based on the results of this clinical study. The results of this study allow us to recommend a drug developer to submit specific data on their study drug GP40221 to the Ministry of Health of the Russian Federation to obtain marketing authorization.