NOVEL NANOMATERIALS FOR USE IN RADIOIMMUNOTHERAPY

描述(申请人提供)：在美国，每四例死亡中就有一例死于癌症，使其成为仅次于心脏病的第二大死因。据美国国立卫生研究院估计，今年约有555,500名美国人死于癌症。放射免疫治疗(RIT)是治疗癌症的新兴方法之一。在RIT中，通过将合适的放射性核素附着到与癌细胞表达的特定抗原结合的抗体上，将治疗性剂量的电离辐射传递到癌症部位。由于具有合适的核发射特性(Ebeta=1.7 MeV)、物理半衰期(T1/2=17小时)、衰变特性以及发电机的可获得性，使Re-188成为潜在用于RIT的最有吸引力的放射性核素之一。然而，Re-188所需的复杂标记化学，以及无法获得在高比活度下与Re-188形成稳定络合物的良好的螯合剂，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，以便用从现成的188W/188Re发生器获得的Re-188方便地标记癌症靶向抗体。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抗体来进行。

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.