The Safety and Dosimetry Study of 177Lu-LNC1003 Injection

This proposal is a phase I, open-label study of a 3-Dose Regimen of Escalating Doses of 177Lu-LNC1003 Injection in patients with PSMA-positive mCRPC. The treatment regimen will consist of a single-dose intravenous administration of 177Lu-LNC1003 Injection per 6-week cycle, for a total of 2 cycles. The dose per cycle will be fixed for each patient and will be escalated in 3 different dose levels, from 30 mCi to 70 mCi (1.11 GBq - 2.59 GBq). This classic "3+3" design recruits 3 patients for the first dose level group. If no dose limiting toxicity (DLT) occurs in the first cycle, then 3 new patients will enter the next higher dose level. If any DLT occurs at a certain dose level, 3 additional patients will be enrolled at this current dose level (in total 6 patients now) to be assessed. The highest dose level(s) at which less than one-third of patients (e.g., 0 of 3 or 1 of 6 patients) experience a DLT will be declared the maximum tolerated dose (MTD). If there is no MTD observed after the dose escalation up to 70 mCi, a comprehensive evaluation should be made by investigator and sponsor to determine whether an escalation to a higher dose can be conducted or not based on the known safety data, radiation doses for similar drugs documented in literature and treatment responses at the doses administered.