I-Corps: Chemical processes for preparation of diagnostic agents for Positron Emission Tomography imaging

该I-Corps项目的更广泛影响/商业潜力是为疾病的早期检测准备新一代诊断产品，并评估正电子发射断层扫描（PET）成像疗法。PET成像使用放射性示踪剂（用安全的放射性材料标记的药物和生物分子）提供细胞和分子水平上的生物事件信息。 这些测试对于乳腺癌等疾病的早期诊断以及评估对免疫疗法的反应是必要的。目前，很少有化学方法以工业规模生产放射性示踪剂。典型的方法使用不是由商业供应商（放射性药物）生产的放射性材料，这反过来又使得这些放射性示踪剂的生产昂贵。因此，这些材料并不容易获得。该项目采用了一种新的化学工艺，其中使用了放射性药物的放射性材料。这种化学过程适用于商业放射性药物，因此他们可以在现场制造放射性示踪剂，以提供给最终用户。 由于这些商业放射性药物通常已经建立了庞大的分销渠道，更多的患者，包括那些资源不足的地区，将能够受益于这些更便宜和更好的诊断产品。这个I-Corps项目进一步开发了一种新的技术，用于制备新一代的放射性示踪剂用于正电子发射断层扫描（PET）。该创新结合了特定的试剂，反应条件和化学过程，以制备标记的生物分子。该技术使用的盐是在商用回旋加速器中直接产生的。 这里开发的方法允许在标记过程的最后一步将放射性核素添加到感兴趣的生物分子中，保留产物的放射性并显着提高放射化学产率。该技术可用于制备各种放射性示踪剂，应用于神经系统疾病、癌症、药物药代动力学、代谢和靶点结合的检测，以及双重成像剂的制备。该奖项反映了NSF的法定使命，并通过使用基金会的知识价值和更广泛的影响审查标准进行评估，被认为值得支持。

The broader impact/commercial potential of this I-Corps project is to prepare a new generation of diagnostic products for early detection of diseases and to evaluate Positron Emission Tomography (PET) Imaging therapies. PET imaging uses radiotracers (drugs and biomolecules labeled with safe radioactive materials) to provide information about biological events on a cellular and molecular level. Such tests are necessary for the early diagnosis of diseases such as breast cancer as well as the evaluation of responses to immunotherapy. Currently, there are few chemical processes to produce radiotracers on an industrial scale. Typical processes use radioactive materials that are not produced by commercial vendors (radiopharmacies) and this, in turn, makes the production of these radiotracers expensive. Hence, the material is not widely accessible. This project uses a new chemical process in which radioactive materials from radiopharmacies are used. The chemical process is adaptable by commercial radiopharmacies so they can make the radiotracers on-site to provide to end users. Since these commercial radiopharmacies typically have established large distribution channels, more patients, including those in under-resourced areas, will be able to benefit from these cheaper and better diagnostic products.This I-Corps project further develops a novel technology in the preparation of a new generation of radiotracers for use in Positron Emission Tomography (PET). The innovation combines specific reagents, reaction conditions, and chemical processes to allow the preparation of labeled biomolecules. The technology uses salts that are directly produced in commercial cyclotrons. The process developed here allows the radionuclide to be added to the biomolecule of interest in the last step of the labeling process, retaining the radioactivity of the product and significantly improving the radiochemical yield. The technology allows the preparation of a wide variety of radiotracers with applications in the detection of neurological disorders, cancer, drug pharmacokinetics, metabolism, and target engagement, as well as in the preparation of dual imaging agents.This award reflects NSF's statutory mission and has been deemed worthy of support through evaluation using the Foundation's intellectual merit and broader impacts review criteria.