Serum half-life and tumor localization of a chimeric antibody deleted of the CH2 domain and directed against the disialoganglioside GD2

Proc Natl Acad Sci U S A. 1990 Aug;87(15):5702-5. doi: 10.1073/pnas.87.15.5702.

Abstract

Recombinant techniques allow one to engineer an antibody molecule and, in this way, manipulate its properties and functions. We engineered a chimeric human/mouse antibody to the tumor-associated antigen ganglioside GD2, with the aim of decreasing its serum half-life, maintaining its full antigen-binding capacity, and deleting its effector functions, thus making it a potentially useful reagent for the radioimaging of tumors. To this end, the constant region of the human gamma 1 chain was mutated by deleting the second domain (CH2). Here we show that the CH2-deleted antibody (ch14.18-delta CH2) was cleared from the blood of athymic (nu/nu) mice bearing human melanoma tumors with the same kinetics as human IgG F(ab')2. At a beta t1/2 of 12 hr, 0.9% of the injected dose of 125I-labeled ch14.18-delta CH2 was found per milliliter of blood 24 hr after i.v. injection. In biodistribution experiments, 125I-labeled ch14.18-delta CH2 targeted specifically to melanoma xenografts, achieving optimal tumor-to-tissue ratios 12-16 hr after i.v. injection. ch14.18-delta CH2 was localized to the melanoma tumors more rapidly and with better localization ratios than the intact chimeric antibody ch14.18. Sixteen hours after i.v. injection, the tumor-to-blood and tumor-to-liver ratios of ch14.18-delta CH2 were 5 and 12, respectively, while optimal localization ratios obtained for ch14.18 were 1 and 5, respectively, but 96 hr after injection. A reagent such as ch14.18-delta CH2 should be useful for radioimmunodetection of human tumors because of reduced immunogenicity, increased targeting specificity, and rapid clearance from circulation.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Cell Line
  • Chimera
  • Chromosome Deletion
  • Fluorescent Antibody Technique
  • Gangliosides / immunology*
  • Humans
  • Immunoglobulin Fab Fragments / genetics*
  • Immunoglobulin Fab Fragments / metabolism
  • Immunoglobulin G / genetics*
  • Immunoglobulin G / metabolism
  • Melanoma / immunology
  • Metabolic Clearance Rate
  • Mice
  • Mice, Nude
  • Neoplasm Transplantation
  • Transplantation, Heterologous

Substances

  • Gangliosides
  • Immunoglobulin Fab Fragments
  • Immunoglobulin G
  • ganglioside, GD2