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

BACKGROUND AND OBJECTIVES

The 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 safety of GR007 in healthy Chinese subjects.

METHODS

Thirty subjects received a single intramuscular injection of 30 mg (n = 10), 90 mg (n = 10), or 150 mg (n = 10) GR007. After administration, the pharmacokinetic characteristics and safety were evaluated.

RESULTS

No 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) of GR007 in the three groups was between 2.75 and 4.00 h and the geometric mean elimination half-life (T) for each group was 2.38, 2.22, and 3.29 h, respectively. The area under the concentration vs time curve (AUC), but not the maximum concentration (C), increased in a dose-proportional manner.

CONCLUSIONS

The results showed that a single intramuscular injection of 30-150 mg 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.