Pharmacokinetics and Safety of Recombinant Human Interleukin-1 Receptor Antagonist GR007 in Healthy Chinese Subjects

Background and ObjectivesThe recombinant human interleukin-1 receptor antagonist (rhIL-1Ra) GR007 is a candidate drug with the potential to prevent the toxicity induced by chemotherapy agents by blocking the IL-1 signaling pathway. The aim of this study was to assess the pharmacokinetics and safetyof GR007 in healthy Chinese subjects.MethodsThirty subjects received a single intramuscular injection of 30mg (n=10), 90mg (n=10), or 150mg (n=10) GR007. After administration, the pharmacokinetic characteristics and safety were evaluated.ResultsNo serious adverse events were reported in this study, and the adverse events reported showed no dose dependency. Pharmacokinetic analysis showed that the median time to maximum concentration (T-max) of GR007 in the three groups was between 2.75 and 4.00h and the geometric mean elimination half-life (T-1/2) for each group was 2.38, 2.22, and 3.29h, respectively. The area under the concentration vs time curve (AUC), but not the maximum concentration (C-max), increased in a dose-proportional manner.ConclusionsThe results showed that a single intramuscular injection of 30-150mg GR007 had good safety and tolerability in healthy Chinese subjects. The results of the evaluation of the safety and pharmacokinetics of GR007 performed in this study support its use as a repeated daily injection in ongoing clinical trials focusing on patients with cancer.