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

Journal of Clinical Pharmacology - Tập 50 Số 3 - Trang 276-284 - 2010
Zhenhua Xu1, Qingmin Wang1, Yanli Zhuang1, Bart Frederick1, Hong Yan1, Esther Bouman‐Thio1, Joseph C. Marini1, Monica Keen1, David Snead1, Hugh M. Davis1, Honghui Zhou1
1Centocor Research and Development, Inc., Malvern, Pennsylvania

Tóm tắt

This study characterized the pharmacokinetics (PK) of golimumab, an antitumor necrosis factor alpha human IgG1k 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 (Cmax) and the mean area under the concentration versus time curves from time zero to infinity (AUC0‐∞) were 29.5 ± 5.8 μg/mL and 195.9 ± 48.9 μg·d/mL, respectively. After SC administration, the mean values of Cmax and AUC0‐∞ 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.

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Thông tin
Thông tin xuất bản

Journal of Clinical Pharmacology

Tập 50 Số 3

276-284

Thông tin tác giả