The pharmacokinetics and safety profiles of belimumab after single subcutaneous and intravenous doses in healthy Japanese volunteers.

摘要: Summary What is Known and Objectives Belimumab a recombinant human monoclonal antibody that binds antagonizes the biological activity of soluble B-lymphocyte stimulator (BLyS) protein. BLyS appears to play role in pathogenesis systemic lupus erythematosus, profile belimumab suggests it may have therapeutic benefit treatment for disease. In this healthy Japanese subjects study, we investigated pharmacokinetics safety single subcutaneous intravenous injection administered as 200 mg/mL liquid formulation. Methods This was an open-label, randomized, parallel-group, single-dose study subjects. Each subject received infusion or 200 mg belimumab. The pharmacokinetic parameters including local tolerance (injection site), biomarkers, immunogenicity adverse events were evaluated up 70 days post-dosing. Results After administration belimumab, all 16 completed study. There no serious related site reactions. All seven considered mild moderate intensity deemed unrelated except cellulitis following administration. bioavailability dose estimated be 77·5%. Time maximum serum concentration after 6·5 days (median). geometric mean terminal half-life comparable between two routes (17·7 days 15·9 days subcutaneous). Serum immunoglobulin G level decreased slightly each treatment. No found produce antibelimumab antibodies. What New Conclusions A favourable absolute seen Considering intersubject variability, exposures consistent with those previously observed non-Japanese Safety biomarker data also previous clinical studies.