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Disposition and immunodynamics of basiliximab in liver allograft recipients
Author(s) -
Kovarik John,
Breidenbach Thomas,
Gerbeau Christophe,
Korn Alex,
Schmidt AlbrechtGeorg,
Nashan Björn
Publication year - 1998
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/s0009-9236(98)90024-8
Subject(s) - basiliximab , volume of distribution , pharmacokinetics , medicine , transplantation , clearance , pharmacology , chemistry , urology , endocrinology , tacrolimus
A randomized, open‐label prospective study was conducted with recipients of primary cadaveric liver allografts to characterize the disposition and immunodynamics of basiliximab, an interleukin‐2 receptor, α‐chain chimeric monoclonal antibody for immunoprophylaxis of acute rejection. Patients received a total intravenous dose of 40 mg basiliximab in addition to baseline dual immunosuppression consisting of cyclosporine (INN, ciclosporin) and steroids. The central distribution volume was 5.6 ± 1.7 L with a steady‐state volume of 7.5 ± 2.5 L. It was cleared slowly with a total body clearance of 75 ± 24 ml/hr and an elimination half‐life of 4.1 ± 2.1 days. Basiliximab was measurable in drained ascites fluid, and clearance by this route was an average of 20% of total clearance. Total body clearance correlated positively with volume of postoperative blood loss ( r = 0.5253, p = 0.0101), suggesting that bleeding may represent an additional route of drug removal. A threshold relation was observed between serum concentration of basiliximab and CD25 expression on T lymphocytes whereby complete saturation of interleukin‐2 receptor α‐chain was maintained as long as serum concentrations exceeded 0.1 μg/ml. The duration of receptor saturation was 23 ± 7 days after transplantation (range, 13 to 41 days). Clinical Pharmacology & Therapeutics (1998) 64 , 66–72; doi: