INTRODUCTION: 131I-CLR1404 is a small molecule that combines a tumor-targeting moiety with a therapeutic radioisotope. The primary aim of this phase 1 study was to determine the administered radioactivity expected to deliver 400 @entity2073 to the bone marrow. The secondary aims were to determine the pharmacokinetic (PK) and safety profiles of 131I-CLR1404. METHODS: Eight subjects with refractory or relapsed advanced solid @entity5 were treated with a single injection of 370 MBq of 131I-CLR1404. Whole body planar nuclear medicine scans were performed at 15-35 minutes, 4-6, 18-24, 48, 72, 144 hours, and 14 days post injection. Optional single photon emission computed tomography imaging was performed on two @entity1 6 days post injection. Clinical laboratory parameters were evaluated in blood and urine. Plasma PK was evaluated on 127I-CLR1404 mass measurements. To evaluate renal clearance of 131I-CLR1404, urine was collected for 14 days post injection. Absorbed dose estimates for target organs were determined using the RADAR method with OLINDA/EXM software. RESULTS: Single administrations of 370 MBq of 131I-CLR1404 were well tolerated by all subjects. No severe adverse events were reported and no adverse event was dose-limiting. Plasma 127I-CLR1404 concentrations declined in a bi-exponential manner with a mean t   value of 822 hours. Mean Cmax and AUC(0-t) values were 72.2 ng/mL and 15753 ng   hr/mL, respectively. An administered activity of approximately 740 MBq is predicted to deliver 400 @entity2073 to marrow. CONCLUSIONS: Preliminary data suggest that 131I-CLR1404 is well tolerated and may have unique potential as an anti- @entity5 agent. TRIAL REGISTRATION: ClinicalTrials.gov NCT00925275.

A Phase 1 Study of 131I-CLR1404 in @entity1 with Relapsed or Refractory Advanced XXXX : Dosimetry, Biodistribution, Pharmacokinetics, and Safety.

@entity5 :: ('MESH:D009369', 'Disease') :: ['cancer', 'tumors'] @entity1 :: ('9606', 'Species') :: ['patients'] @entity2073 :: ('10821', 'Species') :: ['mSv']
@entity5 :: (MESH:D009369,Disease) :: ['Solid Tumors']
