The Phase I study demonstrated that intravenously administered radiolabeled TM601 is able to cross the blood-brain barrier, specifically bind to tumor tissue, and is actively internalized by tumor cells, including metastases to the central nervous system.
The purpose of the Phase I study was to determine whether intravenous administration of radiolabeled TM601 would result in intratumoral uptake in patients with a variety of metastatic cancers refractory to treatment. Patients received a test dose of 0.2mg of TM601 labeled with 10mCi of Iodine radioisotope.
Sequential whole body gamma camera images were then collected at five time points – immediately following administration, 3 hours, 24 hours, 48-72 hours, and 168 hours post-administration – to determine tumor uptake and perform dosimetry analysis. Patients whose images indicated tumor-specific uptake received a second therapeutic dose of 0.6mg TM601 labeled with 30mCi of Iodine radioisotope one week later.
Trial results revealed that all six of the evaluable patients with metastatic melanoma demonstrated tumor-specific uptake of radiolabeled TM601 based on the whole body planar gamma camera imaging. Moreover, tumor uptake was observed in metastases in the central nervous system, as well as extracranial sites. No dose-limiting toxicities were observed. The seventh patient did not complete imaging assessments and was therefore not considered to be evaluable.