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Cancer Diagnosis
CLR1404 can easily be radiolabeled with any of the radioactive isotopes of iodine. As such, either the 131I version of CLR1404 could be used for SPECT imaging or the 124I version could be used for PET imaging. Cellectar senior scientists have over 30 years of radioiodination experience and have labeled all PLE analogs with excellent radiochemical yield and purity and with a variety radioiodine isotopes including iodine-125, 131, and 124. Positron imaging used in conjunction with CT scanning has now become the imaging method of choice in oncology.
The current gold standard, 18-Fluorodeoxy glucose (FDG) does help detect a variety of tumors that are known to have increased glucose metabolism. However, FDG localizes in certain normal tissue such as heart, kidney and brain tissues that also have high glucose metabolism. FDG is also known to localize in inflammatory sites. Other major limitations to the use of FDG are found in pelvic imaging due to the high renal (kidney) clearance of the compound. These characteristics of FDG, therefore, decrease its diagnostic specificity for certain malignancies.
A side by side comparison of 124I-CLR1404 to FDG was undertaken in the same mouse (24 hours apart), and as expected, FDG demonstrated significant uptake into the carageenan induced inflammatory lesion (indicated as "I") and only some uptake in a PC3 tumor located in both the thigh and contralateral tibia (indicated as "T"). CLR1404 on the other hand, showed no uptake into the inflammatory lesion (shown as I ?) and significantly better uptake in both tumors. The "H" indicates the heart.
Additionally, the physical half-life of only 110 minutes for fluorine-18 labeled agents severely limits their delivery range to a few hundred miles. Iodine-131, on the other hand, has an eight day half-life and iodine-124 has a four day half-life. These longer half-lives permit manufacturing and worldwide distribution of CLR1404 in any isotopic form from one manufacturing location. Additionally, the longer half-life affords a longer imaging window - up to seven days.
The image on the right reflects the tremendous potential of CLR1404 in certain malignacies such as prostate and ovarian cancer. It is the intent of Cellectar to focus on these types of malignancies where current imaging methods are less effective.
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