A Randomized Phase 1 Pharmacokinetic Study Comparing the Potential Biosimilar LRG201902 With Liraglutide (Victoza(®)) in Healthy Male Subjects

Objective: Pharmacokinetic (PK) similarity between biosimilar candidate LRG201902 and European Union-sourced liraglutide reference product (Victoza(®)) was evaluated. Safety and immunogenicity were also assessed. Methods: This single-dose, randomized, open-label, 2-period crossover study (CTR20192342) was conducted in thirty-eight healthy adult male subjects. Volunteers were randomized 1:1 at the beginning to receive a single 0.6 mg dose of Victoza(®) or LRG201902 by subcutaneous injection during the first period. Following 8 days washout period, all subjects received the alternate formulation during the second period. Blood samples were collected up to 72 h after administration. The primary pharmacokinetic endpoints were AUC(0–t), AUC(0–∞), and C(max). Pharmacokinetic similarity was achieved if 90% confidence intervals (CIs) of the geometric mean ratios (GMRs) of AUC0-t, AUC(0–∞), and C(max) were within the range of 80–125%. Other pharmacokinetic parameters including T(max), t(½), and λ(z) were also measured. Safety profile and immunogenicity data were collected from each subject. Results: C(max), AUC(0–t), and AUC(0–∞) were similar between the two groups. GMRs of Cmax, AUC(0–t), and AUC(0–∞) were 113.50%, 107.21%, and 106.97% between LRG201902 and Victoza(®) respectively. The 90% CIs for the GMRs of C(max), AUC(0-t), and AUC(0–∞) were all within the PK equivalence criteria. Mean serum concentration-time profiles, secondary pharmacokinetic parameters (T(max), t(½), and λ(z)) were comparable between groups. Treatment-related adverse events were reported by 27.8% and 23.7% subjects in the LRG201902 and Victoza(®) arms, respectively. All post-dose samples were detected negative for anti-drug antibodies. Conclusion: This study demonstrates pharmacokinetic similarity of LRG201902 to Victoza(®) in healthy subjects. The safety and immunogenicity profiles were similar for the two products.