Anthracycline immunoconjugates prepared by a site-specific linkage via an amino-dextran intermediate carrier.

Abstract:

:Anthracycline, either daunomycin or doxorubicin, was site specifically attached to the carbohydrate moiety of a monoclonal anticarcinoembryonic antigen antibody by using amino-dextran as the intermediate carrier. The reaction resulted in an immunoconjugate that contains approximately 20 to 25 molecules of drug per molecule of immunoglobulin G. Flow-cytometric studies revealed the retention of the antibody-binding activity. The immunoconjugate was cytotoxic to the target cells, as examined by the 75selenomethionine incorporation studies, and remained efficient for targeting a human colonic tumor (GW-39) in the nude mouse model. The conjugate possessed a greater antitumor activity against the subcutaneous tumor than either the free drug or an irrelevant antibody conjugate, and it was well tolerated by the animals at a much higher dose level than was the unconjugated drug.

journal_name

Cancer Res

journal_title

Cancer research

authors

Shih LB,Goldenberg DM,Xuan H,Lu H,Sharkey RM,Hall TC

subject

Has Abstract

pub_date

1991-08-15 00:00:00

pages

4192-8

issue

16

eissn

0008-5472

issn

1538-7445

journal_volume

51

pub_type

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