NOVEL NANOMATERIALS FOR USE IN RADIOIMMUNOTHERAPY

描述（由申请人提供）：在美国，每四个死亡中就有一个死于癌症，使其成为仅次于心脏病的第二大死亡原因。据美国国立卫生研究院估计，今年约有555，500名美国人将死于癌症。放射免疫疗法（RIT）是治疗癌症的新兴模式之一。在RIT中，治疗剂量的电离辐射通过将合适的放射性核素连接到与癌细胞表达的特异性抗原结合的抗体上来递送到癌症部位。合适的核发射特性（Ebeta = 1.7 MeV）、物理半衰期（t1/2 = 17 hr）、衰变特性以及其从发生器的可用性，使得188成为可能用于RIT的最有吸引力的放射性核素之一。然而，Re-188所需的复合物标记化学以及在高比活度下与Re-188形成稳定复合物的良好螯合剂的不可用性限制了Re-188在RIT中的使用。为了克服这些问题，Lynntech目前正在开发纳米颗粒技术，用于方便地用从现成的188 W/188 Re发生器获得的Re-188标记癌症靶向抗体。在第一阶段，概念验证将通过使用新的纳米颗粒技术用Re-188标记抗CEA抗体来证明。

DESCRIPTION (provided by applicant): One of every four deaths in the US is from cancer, making it the second leading cause of death, behind heart disease. According to an NIH estimate, this year about 555,500 Americans will die of cancer. Radioimmunotherapy (RIT) is one of the emerging modalities for the treatment of cancers. In RIT, a therapeutic dose of ionizing radiation is delivered to the cancer sites by attaching a suitable radionuclide to an antibody that binds to a specific antigen expressed by the cancer cells. The suitable nuclear emission properties (Ebeta = 1.7 MeV), the physical half-life (t1/2 = 17 hr), the decay-characteristics, and its availability from a generator, makes rhenium-188 one of the most attractive radionuclides for potential use in RIT. However, the complex labeling chemistry required for Re-188 and non-availability of a good chelating agent that forms stable complexes with Re-188 at high specific activities, limits the use of Re-188 in RIT. To overcome these problems, Lynntech is currently developing nanoparticle technology for a convenient labeling of cancer-targeting antibodies with Re-188 obtained from a readily available 188W/188 Re generator. During Phase I, the proof of concept will be demonstrated by labeling anti-CEA antibody with Re-188 using the new nanoparticle technology.