METAL CHELATE CONJUGATED MONOCLONAL ANTIBODIES FOR TUMOR DX & THERAPY

肿瘤相关单抗是潜在的治疗药物 细胞毒剂对恶性细胞的选择性载体。我们正在测试 这一假说出现在几个动物模型系统中：一个是肿瘤病毒 诱导小鼠白血病；另一种是裸鼠裸鼠移植瘤 老鼠。 所使用的杀细胞剂是各种放射性核素。他们的 与单抗结合时的相对疗效正在测试中 并与单独或与之结合的单抗进行比较 毒素。选择用于研究的几种放射性核素的范围包括 核素性质可用，因此铜-67代表弱、短 射程，低能量贝塔发射器，Y-90是远程，高能发射器 β发射体，铋-212是一个短寿命的阿尔法发射体，铅-212 提供短程和长程Beta、排放和后续的Alpha 它的铋-212子体的发射。螯合剂的合成 将这些同位素与抗体连接所需的工作现已完成。 在动物模型系统中，双DOTA络合物已被证明是稳定的。

Tumor-associated monoclonal antibodies are potential therapeutic agents as selective carriers of cytotoxic agents to malignant cells. We are testing this hypothesis in several animal model systems: one is a tumor virus induced leukemia of mice; another is human tumor xenographs in nude athymic mice. The cytocidal agents being employed are various radionuclides. Their relative efficacy when conjugated to monoclonal antibodies is being assayed and compared to that of monoclonal antibodies alone or conjugated to toxins. The several radionuclides chosen for study span the range of nuclidic properties available, thus Copper-67 represents a weak, short range, low energy beta emitter, Yttrium-90 is a long range, high energy beta emitter, Bismuth-212 is a short-lived, alpha emitter and Lead-212 provides both short and long range beta,emissions and the subsequent alpha emission of its Bismuth-212 daughter. The syntheses of the chelating agents required for linkage of these isotopes to antibody is now complete. The Bi-DOTA complex has been shown to be stable in an animal model system.