Tumor-Specific Novel Taxoid−Monoclonal Antibody Conjugates

✍ Scribed by Ojima, Iwao; Geng, Xudong; Wu, Xinyuan; Qu, Chuanxing; Borella, Christopher P.; Xie, Hongsheng; Wilhelm, Sharon D.; Leece, Barbara A.; Bartle, Laura M.; Goldmacher, Victor S.; Chari, Ravi V. J.

• Book ID: 120622158
• Publisher: American Chemical Society
• Year: 2002
• Tongue: English
• Weight: 95 KB
• Volume: 45
• Category: Article
• ISSN: 0022-2623
• DOI: 10.1021/jm025540g

✦ Synopsis

Taxoids bearing methyldisulfanyl(alkanoyl) groups for taxoid-antibody immunoconjugates were designed, synthesized and their activities evaluated. A highly cytotoxic C-10 methyldisulfanylpropanoyl taxoid was conjugated to monoclonal antibodies recognizing the epidermal growth factor receptor (EGFR) expressed in human squamous cancers. These conjugates were shown to possess remarkable target-specific antitumor activity in vivo against EGFR-expressing A431 tumor xenografts in severe combined immune deficiency mice, resulting in complete inhibition of tumor growth in all the treated mice.