Introduction and Objective: GZR102 is a once-weekly fixed ratio combination of insulin GZR4 and the GLP-1 analog bofanglutide (GZR18). This study evaluated the safety, tolerability, and pharmacokinetics (PK) of GZR102 compared with monotherapy of each component in healthy Chinese participants. Methods: In this double-blind, three-period crossover Phase 1 study, 30 participants (BMI 24-28 kg/m2) were randomized equally to six treatment sequences and received a single subcutaneous administration of GZR102, GZR4, or GZR18 with a 5-week observation period, with at least one week’s washout between each period. PK blood samples were collected up to 840 h post-dose. Results: The ratios (90% CI) of GZR102/GZR4 for the AUCGZR4, 0-840h, AUCGZR4, 0-∞, and Cmax, GZR4 were all within the predefined equivalence range (0.80-1.25). The ratios of GZR102/GZR18 for the AUCGZR18, 0-840h and AUCGZR18, 0-∞ were also within 0.80-1.25, but Cmax, GZR18 was slightly higher for GZR102 vs GZR18 alone (1.36 1.27, 1.46). Nevertheless, the model-predicted data demonstrated that this Cmax difference is expected to be apparently reduced at steady state (1.18 1.10, 1.26). GZR102 was well-tolerated; no death, study product related serious AEs, or injection site reactions were observed. Conclusion: The combination of GZR4 and GZR18 in GZR102 had no significant effect on GZR4 PK or GZR18 total exposure, but did slightly increase the Cmax of GZR18. GZR102 showed favorable safety and tolerability. Disclosure D. Liu: None. F. Wang: None. J. Zhao: None. X. Min: None. Y. Zhang: None. T. Xie: None. A. He: None. W. Chen: None.
LIU et al. (Fri,) studied this question.
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