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Nuklearmedizin 1984; 23(04): 193-195
DOI: 10.1055/s-0038-1624217
Originalarbeiten – Original Articles
Schattauer GmbH

A Comparison of the Cyclic Anhydride and Mixed Anhydride Methods for 111In-DTPA Chelation to Monoclonal Antibodies

Ein Vergleich der zyklischen Anhydrid- und gemischten Anhydrid-Methode für die 111In-DTPA Chelatisierung mit monoklonalen Antikörpern
T. S. T. Wang
**   The Departments of Microbiology and Immunology, New York College of Medicine, New York, N. Y, U.S.A
,
S. C. Srivastava
*   The Brookhaven National Laboratory, Upton, N. Y., U.S.A
,
R. A. Fawwaz
1   From the Departments of Radiology, Surgery and Pathology, College of Physicians and Surgeons, Columbia University, New York, N. Y, U.S.A
,
P. Giacomini
1   From the Departments of Radiology, Surgery and Pathology, College of Physicians and Surgeons, Columbia University, New York, N. Y, U.S.A
,
S. Ferrone
**   The Departments of Microbiology and Immunology, New York College of Medicine, New York, N. Y, U.S.A
,
P. Richards
1   From the Departments of Radiology, Surgery and Pathology, College of Physicians and Surgeons, Columbia University, New York, N. Y, U.S.A
,
M. Hardy
1   From the Departments of Radiology, Surgery and Pathology, College of Physicians and Surgeons, Columbia University, New York, N. Y, U.S.A
,
P. O. Alderson
1   From the Departments of Radiology, Surgery and Pathology, College of Physicians and Surgeons, Columbia University, New York, N. Y, U.S.A
› Author AffiliationsThis work was supported in part by NIH grants AM 30468 and HOL 14799.
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Publication History

Received: 28 March 1984

Publication Date:
11 January 2018 (online)

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Summary

The cyclic anhydride (CA) and the mixed anhydride (MA) of DTPA were synthesized and used to chelate 111In to an antimelanoma monoclonal antibody. The CA and MA methods showed mean labeling efficiencies of 25.7 and 20.5%, respectively (p = NS). The binding efficiency of labeled antibody to human melanoma cells in tissue culture also was similar (x̄ = 52 and 50%, respectively, p = NS), as was tumor uptake in nude mice at 96 hrs post-injection (16%-CA vs 12%-MA). The method required less complicated chemical syntheses, much less preparation time, and the product was stable over a much longer period. The results suggest that the CA method is preferable for bifunctional chelate labeling of monoclonal antibodies with 111In-DTPA.

Zusammenfassung

Das zyklische Anhydrid (CA) und das gemischte Anhydrid (MA) des DTPA wurden synthetisiert und angewandt, um 111In mit einem Antimelanom monoklonalen Antikörper zu chelatisieren. Beide Methoden zeigten durchschnittliche Markierungsausbeuten von 25,7 bzw. 20,5% (p = n.s.). Die Markierungsausbeute markierter Antikörper mit menschlichen Melanomzellen in Zellkulturen war ähnlich (x̄ = 52 bzw. 50%, p = n.s.), wie auch die Tumoraufnahme in Nacktmäusen 26 Std. nach Injektion (16% CA vs. 12% MA). Die CA-Methode erforderte weniger komplizierte chemische Synthesen, eine kürzere Vorbereitung, und das Produkt war viel länger stabil. Die Ergebnisse zeigen, daß die CA-Methode für die bifunktionelle Markierung monoklonaler Antikörper mit 111In-DTPA vorzuziehen ist.

 

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