Abstract

Most of the reported methods for coupling anthracycline drugs to antibody result in either a loss of pharmacological activity or yield antibodies which have lost much of their immunological specificity. The use of glutaraldehyde for coupling saves both the pharmacological and immunological activities but it causes some polymerization of the antibody or of the macromolecular carrier which is undesirable for in vivo use. A new coupling procedure is reported which uses an activated derivative of daunorubicin added to monoclonal antihuman sarcoma antibody. This coupling procedure has not resulted in significant polymerization of the antibody or Joss of pharmacological activity determined by testing normal and tumour cell Lines in vitro.

Highlights

  • M P AGE, D TmBEAULT, H TREMBLAY, C NOEL, MJ PERRON

  • Desirable carrier antibodies are those which react with cancerassociated antigens expressed on the surface oftumour cells and not found in significant quantity exposed on the surface of normal cells in vital organs [1,2]

  • Monoclonal4E8 or G10 used in this experiment were specific for embryonic prealbumin: both are of the IgG1K isotype

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Summary

Introduction

M P AGE, D TmBEAULT, H TREMBLAY, C NOEL, MJ PERRON. Conjugation of daunorubicin to monoclonal antihuman sarcoma antibody by a novel method. Most of the reported methods for coupling anthracycline drugs to antibody result in either a loss of pharmacological activity or yield antibodies which have lost much of their immunological specificity. The use of glutaraldehyde for coupling saves both the pharmacological and immunological activities but it causes some polymerization of the antibody or of the macromolecular carrier which is undesirable for in vivo use. A new coupling procedure is reported which uses an activated derivative of daunorubicin added to monoclonal antihuman sarcoma antibody. This coupling procedure has not resulted in significant polymerization ofthe antibody or Joss of ph armacological activity determined by testing normal and tumour cell Lines in vitro. Most of the reported conjugation procedures cause some loss of immunological activity

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