首页> 外文期刊>Journal of Labelled Compounds and Radiopharmaceuticals >17TH WORKSHOP OF THE INTERNATIONAL ISOTOPE SOCIETY - CENTRAL EUROPEAN DIVISION. THE SYNTHESIS AND APPLICATIONS OF ISOTOPES AND ISOTOPICALLY LABELLED COMPOUNDS
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17TH WORKSHOP OF THE INTERNATIONAL ISOTOPE SOCIETY - CENTRAL EUROPEAN DIVISION. THE SYNTHESIS AND APPLICATIONS OF ISOTOPES AND ISOTOPICALLY LABELLED COMPOUNDS

机译:第17届国际同位素协会研讨会 - 中欧司。 同位素和同位素标记化合物的合成和应用

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摘要

Novel targeted MI-PET-tracers are discovered either by conventional drug design processes, i.e. Structure Activity Relationship (SAR) on existing therapeutic compound libraries or literature based scaffolds or using modem tools like combinatorial chemistry and high throughput screening. In a second step, the identified best candidates are investigated for a suitable radiolabelling position. A tailored radiosynthesis process is mandatory, due to the generally short radioactive half-lifes of the radioisotopes of choice, i.e. t_(1/2[F-18]) = 110 min. This short half-life is responsible for a relatively low radiation burden to the patients. However, the short half-life implicitly requires a fully automated radiosynthesis, which is a remote controlled production process, thus, ensuring reliable daily tracer production and distribution to the customer. Therefore, disposable cassette based production processes are developed and established.The low mass dose applied with MI-tracers (<100mug) allows for a fast development process and early 'proof of mechanism' (PoM) studies in patients via a so called 'micro-dose concept' initiated by the regulatory bodies. Data received from these PoM studies can be fed back into the compound generation and early development circle to facilitate further optimization and fine-tuning of the tracer candidates.BSP is actively working on unmet medical needs in various fields, especially in Oncology Imaging (i.e. prostate cancer, and highly tumor specific probes), CNS Imaging (i.e. early detection of dementia), and Cardiovascular Imaging (i.e. myocardial perfusion).Furthermore, Diagnostic Imaging is actively involved in the development of therapeutic drug projects in Oncology, Cardiology, and CNS indications by providing appropriate MI-PET tracers for patient selection and early therapy response monitoring. We actively partner with other pharmaceutical companies and academia to implement Ml as a valuable routine tool for personalized medicine and drug development.
机译:通过常规药物设计方法,即结构活性关系(SAR)在现有治疗性化合物文库或文学基础的支架上或使用调制解调器工具,如组合化学和高通量筛选等靶向MI-PET示踪剂。在第二步中,研究了所识别的最佳候选者以进行合适的放射性标记位置。由于选择的放射性同位素的通常短的放射性半衰期,通常是一种定制的可辐射合成过程,即(1/2 [F-18])= 110分钟。这一短暂的半衰期负责患者的辐射负担相对较低。然而,短半衰期隐含地需要一个完全自动的可放射合成,这是一种远程控制的生产过程,从而确保可靠的日常示踪剂生产和分配给客户。因此,基于一次性盒的生产过程开发和建立。用MI示踪剂(<100mug)施加的低质量剂量允许快速开发过程和早期“机构的验证”(POM)在患者中的研究,通过所谓的“微量” - 由监管机构发起的概念。从这些POM研究中收到的数据可以反馈到复合生成和早期开发圈中,以便于进一步优化和微调示踪剂候选人.BSP正在积极地研究各种领域的未满足的医疗需求,尤其是肿瘤学成像(即前列腺癌症和高度肿瘤特异性探针),CNS成像(即痴呆的早期检测),以及心血管成像(即心肌灌注)。次要的诊断成像积极参与肿瘤,心脏病学和CNS适应症的治疗药物项目的发展通过为患者选择和早期治疗反应监测提供适当的MI-PET示踪剂。我们积极与其他制药公司和学术界合作,将ML作为个性化医学和药物开发的有价值的常规工具。

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