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Purpose: Auger electrons emitted by radioisotopes such as ¹²⁵I have a high linear energy transfer and short mean-free path in tissue (<10 μm), making them suitable for treating micrometastases while sparing normal tissues. The authors developed and subsequently investigated a cancer cell-selective small molecule phospholipid ether analog to deliver ¹²⁵I to triple-negative breast cancer (TNBC) cells in vivo.

Methods: A Current Good Manufacturing Practice (cGMP) method to radiolabel ¹²⁵I-CLR1404 (CLR 125) with >95% radiochemical purity was established. To estimate CLR 125 in vivo dosimetry and identify dose-limiting organs, the biodistribution of the analog compound ¹²⁴I-CLR1404 (CLR 124) was investigated using micro-positron emission tomography (PET)/computed tomography (CT) in conjunction with a Monte Carlo dosimetry platform to estimate CLR 125 dosimetry. In vivo antitumor efficacy was …