Selection of Reaction Additives Used in the Preparation of Monomeric Antibody−Calicheamicin Conjugates

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• 作者：Irwin Hollander ; Arthur Kunz ; Philip. R. Hamann
• 刊名：Bioconjugate Chemistry
• 出版年：2008
• 出版时间：January 2008
• 年：2008
• 卷：19
• 期：1
• 页码：358 - 361
• 全文大小：89K
• 年卷期：v.19,no.1(January 2008)
• ISSN：1520-4812

文摘

The formation of protein aggregates can be a major problem during the preparation of antibody−drug conjugates. Herein is described the methods by which reaction additives were selected, which reduce the tendency of antibodies to aggregate during the attachment of the cytotoxic agent calicheamicin to form an immunoconjugate. Reaction conditions were delineated that produced optimized yields of monomeric conjugates. These conditions were used in the preclinical preparations of gemtuzumab ozogamicin (Mylotarg), the first commercially available chemotherapeutic immunoconjugate.