http://pubs.acs.org/doi/pdf/10.1021/cr400460s

Metallodrugs in Medicinal Inorganic Chemistry

Background Metastatic castration-resistant prostate cancer remains fatal despite recent advances. Prostate-specific membrane antigen (PSMA) is highly expressed in metastatic castration-res...

https://www.nejm.org/doi/suppl/10.1056/NEJMoa2107322/suppl_file/nejmoa2107322_appendix.pdf

Lutetium-177-PSMA-617 for Metastatic Castration-Resistant Prostate Cancer.

Diverse radiochemistry is an essential component of nuclear medicine; this includes imaging techniques such as positron emission tomography (PET). As such, PET can track diseases at an early stage of development, help patient care planning through personalized medicine and support drug discovery programs. Fluorine-18 is the most frequently used radioisotope in PET radiopharmaceuticals for both clinical and preclinical research. Its physical and nuclear characteristics (97% β+ decay, 109.8 min half-life, 635 keV positron energy) and high specific activity make it an attractive nuclide for labeling and molecular imaging. Arenes and heteroarenes are privileged candidates for 18F-incorporation as they are metabolically robust and therefore widely used by medicinal chemists and radiochemists alike. For many years, the range of (hetero)arenes amenable to 18F-fluorination was limited by the lack of chemically diverse precursors, and of radiochemical methods allowing 18F-incorporation in high selectivity and effi...

18F-Labeling of Arenes and Heteroarenes for Applications in Positron Emission Tomography

Bifunctional coupling agents for radiolabeling of biomolecules and target-specific delivery of metallic radionuclides.

There is a great current interest in developing target-specific radiopharmaceuticals for early detection of diseases and radiotherapy of cancers. This critical review will focus on the role of coordination chemistry in the development of target-specific radiopharmaceuticals. It will also discuss the recent development in technetium, copper, gallium, indium, yttrium and lanthanide chemistry, as well as analytical tools for quality control and characterization of radiolabeled small biomolecules (159 references).

The role of coordination chemistry in the development of target-specific radiopharmaceuticals.

Evolution of Tc-99m in diagnostic radiopharmaceuticals

Background: This review provides a comprehensive summary of the production of 177Lu to meet expected future research and clinical demands. Availability of options represents the cornerstone for sustainable growth for the routine production of adequate activity levels of 177Lu having the required quality for preparation of a variety of 177Lu-labeled radiopharmaceuticals. The tremendous prospects associated with production of 177Lu for use in targeted radionuclide therapy (TRT) dictate that a holistic consideration should evaluate all governing factors that determine its success. Methods: While both “direct” and “indirect” reactor production routes offer the possibility for sustainable 177Lu availability, there are several issues and challenges that must be considered to realize the full potential of these production strategies. Results: This article presents a mini review on the latest developments, current status, key challenges and possibilities for the near future. Conclusion: A broad understanding and discussion of the issues associated with 177Lu production and processing approaches would not only ensure sustained growth and future expansion for the availability and use of 177Lu-labeled radiopharmaceuticals, but also help future developments.

/pdf/production-of-177-lu-for-targeted-radionuclide-therapy-2s5ap1bea0.pdf

Production of (177)Lu for Targeted Radionuclide Therapy: Available Options.

Lutetium-177 therapeutic radiopharmaceuticals: linking chemistry, radiochemistry, and practical applications.

Production logistics of 177Lu for radionuclide therapy

313 Objectives To design a robust and efficient computational platform to accurately quantify pulmonary infections in rabbits through precise segmentation of high-distributed uptakes from 18F-FDG-PET images. Methods PET-CTs were analyzed from 10 rabbits infected with aerosolized Mycobacterium tuberculosis (H37Rv strain) over various time points (0 to 38 weeks). An overview of the proposed framework is as follows: (i) the histogram of the PET image(s) were estimated and smoothed via diffusion based kernel density estimation; (ii) the similarity of all points on the smoothed histogram was calculated using a novel similarity function, with the assumption that closer points on the histogram are more similar and more likely to belong to the same class; and (iii) the Affinity Propagation (AP) method was used to cluster the data points in order to find optimal thresholding levels to separate the high-uptake regions into several classes, which may further aid in the definition of target boundaries. Results The Dice Similarity Coefficient (DSC), sensitivity, and specificity were calculated between the segmentation region that was found by the proposed method and compared to two expert delineations. The average DSC was 89.06 ±9.82% with a sensitivity of 97.87±7.09% and a specificity of 83.70±15.32%. The correlation coefficient between the delineation performances of the two expert observers was R2=0.85 (p Conclusions Our proposed segmentation method quantified the distributed uptake regions with high accuracy and within seconds; hence, it outperformed the state-of-the-art methods. Research Support This research is supported by CIDI, the intramural research program of the National Institute of Allergy and Infectious Diseases (NIAID) and the National Institute of Biomedical Imaging and Bioengineering (NIBIB). Dr. Jain acknowledges the NIH Director’s New Innovator Award (OD006492). The rabbit infection study is funded by HHMI, NIAD R01AI079590, and R01A1035272.

http://jnm.snmjournals.org/content/early/2012/12/19/jnumed.112.110338.full.pdf

M. R. A. Pillai

Papers

Evolution of Tc-99m in diagnostic radiopharmaceuticals

Production of (177)Lu for Targeted Radionuclide Therapy: Available Options.

Lutetium-177 therapeutic radiopharmaceuticals: linking chemistry, radiochemistry, and practical applications.

Production logistics of 177Lu for radionuclide therapy

Sustained Availability of 99mTc: Possible Paths Forward