Use of [123I]-2-iodo-L-phenylalanine as a tumor imaging agent in two dogs with synovial cell sarcoma.

[123I]-iodo-L-phenylalanine was successfully evaluated for gamma camera imaging in vivo in tumor-bearing athymic mice and in humans with brain tumors. Here, we report the use of this tracer in two dogs with synovial cell sarcoma of the tarsus. [123I]-iodo-L-phenylalanine was quantitatively prepared as a kit formulation using the Cu(1+) +-assisted nucleophilic exchange. Rapid [123I]-2-iodo-L-phenylalanine tumor accumulation was observed with good tumor to background contrast and rapid clearance in these two dogs. This radiopharmaceutical is a promising alternative tumor tracer to overcome the known limitations of 18F-fluorodeoxyglucose and, when labelled with radioiodine-131, has the potential to be used for therapeutic purposes.

Comparison between 1 T MRI and non-MRI based volumetry in inoculated tumours in mice.

Tumour volume is an important therapeutic endpoint for mouse tumour models in the evaluation of new chemotherapeutic drugs and in pre-clinical evaluation of new radioimmunotherapy pharmaceuticals. In this study, two 1 T MRI-based methods both using T1-T2 hybrid weighting, a manual method (determination of the area per slice) and a semi-automated method (using thresholding), are compared with two classical methods, the abovementioned calliper method and volumetry by water displacement after dissection of the tumour. Interoperator and intraoperator differences for both MRI-based methods were good (no differences p<0.05 using a repeated measures analysis of variance (ANOVA) test). Correlation between the different methods was excellent. No significant differences were obtained (p<0.05), except for the semi-automated method, because it automatically excludes necrotic regions from the tumour. Therefore, we conclude that both manual and semi-automated tumour volumetry in subcutaneous tumour bearing athymic mice by low-field MRI are accurate and reliable methods. The semi-automated method is especially useful for larger tumour volumes, since it accounts for necrotic areas within the tumour.

Synthesis, radiosynthesis, and in vitro characterization of [125I]-2- iodo-L-phenylalanine in a R1M rhabdomyosarcoma cell model as a new potential tumor tracer for SPECT.

[125I]-2-iodo-L-phenylalanine, a new radioiodinated phenylalanine analog was evaluated as a potential specific tumor tracer for SPECT. The tracer is obtained with an overall radiochemical yield of at least 98%, a purity of > 99%, and a specific activity of 11 MBq/mmol in one pot Kit conditions using the Cu1+ assisted isotopic exchange. The tracer is evaluated in vitro using R1M rat rabdomyosarcoma cells in HEPES buffer with and without Na+ ions and in MEM buffer. The uptake of [125I]-2-iodo-L-phenylalanine follows a reversible pseudo-first-order reaction which is the same in presence and absence of Na+ ions, but the compound is not incorporated into the cell proteins. The reversible uptake is proven to occur with the same affinity as L-henylalanine by a saturable transport system which is competitively inhibited by BCH, an L transport type selective molecule. Trans-stimulation of the efflux by BCH and typical L transported amino acids shows that the transporter is of the antiport type and fulfils all the properties of the LAT1 heterodimer transport system. [125I]-2-iodo-L-phenylalanine is thus a phenylalanine analog that for the uptake uses for the major part the LAT1 transport system which is known to be over-expressed in tumor cells. This, together with the easy Kit preparation, makes [123I]-2-iodo-L-phenylalanine a promising tumor specific tracer for SPECT.