Subcutaneous bioavailability of golimumab at 3 different injection sites in
healthy subjects.
Author(s): Xu Z, Wang Q, Zhuang Y, Frederick B, Yan H, Bouman-Thio E, Marini JC, Keen M,
Snead D, Davis HM, Zhou H.
Affiliation(s): Centocor Research and Development Inc, Malvern, PA 19355, USA.
Publication date & source: 2010, J Clin Pharmacol. , 50(3):276-84
This study characterized the pharmacokinetics (PK) of golimumab, an antitumor
necrosis factor alpha human IgG1kappa 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-infinity)) were 29.5 +/- 5.8 microg/mL and 195.9 +/- 48.9
microg x d/mL, respectively. After SC administration, the mean values of C(max)
and AUC(0-infinity) were 6.3 +/- 2.8 microg/mL and 100.1 +/- 29.2 microg x 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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