Pharmacokinetics, immunogenicity, and efficacy of dimeric TNFR binding proteins in healthy and bacteremic baboon

J Appl Physiol (1985). 1998 Apr;84(4):1119-30. doi: 10.1152/jappl.1998.84.4.1119.

Abstract

Immunogenicity, pharmacokinetics, and therapeutic efficacy of three novel dimeric soluble tumor necrosis factor (TNF)-receptor I constructs [TNF-binding protein (bp)] were evaluated in 28 baboons, 12 of which were healthy and 16 were challenged with a lethal Escherichia coli bacteremia. The three constructs differed only in the number of extracellular domains of the TNF receptor I and were dimerized with polyethylene glycol. Although all three constructs had generally similar pharmacokinetics when administered to a naive animal, they differed quantitatively in their immunogenicity. Antibodies were detected more frequently, and titers were significantly higher (P < 0.05) in both healthy and septic baboons that received the 4.0-domain TNF-bp construct, compared with animals receiving the 2.6-domain construct. When the TNF-bp constructs were administered a second time (21 days later), the half-lives of the three constructs were significantly shorter in animals that had an antibody response after the first injection. In contrast, all three TNF-bp constructs were equally effective at improving outcome, blocking a systemic TNF-alpha response, and attenuating the cytokine responses when administered at a dose of 1.0 mg/kg body wt 1 h before a lethal E. coli infusion. The findings suggest that immunogenicity of TNF-bp constructs can be altered by changing the number of functional domains, without affecting their capacity to neutralize TNF-alpha and to abrogate TNF-mediated pathology.

MeSH terms

  • Animals
  • Antibody Formation / physiology
  • Bacteremia / immunology*
  • Bacteremia / pathology
  • Crystallography, X-Ray
  • Escherichia coli Infections / immunology*
  • Escherichia coli Infections / pathology
  • Female
  • Half-Life
  • Immunoglobulin G / biosynthesis
  • Kidney / pathology
  • Kinetics
  • Leukocyte Count
  • Male
  • Molecular Conformation
  • Papio
  • Protein Binding
  • Receptors, Tumor Necrosis Factor / immunology*
  • Receptors, Tumor Necrosis Factor / metabolism*

Substances

  • Immunoglobulin G
  • Receptors, Tumor Necrosis Factor