Subcutaneous Bioavailability of Golimumab at 3 Different Injection Sites in Healthy Subjects

This study characterized the pharmacokinetics (PK) of golimumab, an antitumor necrosis factor alpha human IgG1κ monoclonal antibody, after a single intravenous (IV) or subcutaneous (SC) administration in healthy subjects and determined the absolute bioavailability of SC golimumab delivered at 3 different anatomical regions. Seventy-eight healthy adult males were randomly assigned to receive a single dose of golimumab 100 mg by IV (30-minute infusion, n = 23) or SC administration at different sites (upper arm, n =18; abdomen, n =18; thigh, n = 19). Serial blood samples were collected for PK characterization. Following IV administration, the mean maximum observed serum golimumab concentration (C max ) and the mean area under the concentration versus time curves from time zero to infinity (AUC 0-∞ ) were 29.5 ± 5.8 μg/mL and 195.9 ± 48.9 μg·d/mL, respectively. After SC administration, the mean values of C max and AUC 0-∞ were 6.3 ± 2.8 μg/mL and 100.1 ± 29.2 μg·d/mL, respectively. The median terminal half-life was similar for SC and IV administration (10.9 and 11.8 days, respectively), The overall mean bioavailability of SC golimumab was 51 %, and absorption was similar for the 3 injection sites. Golimumab 100 mg was generally well tolerated in this study. Results support the flexibility in the choice of an injection site for SC administration of golimumab.