Targeted imaging of gastrin-releasing peptide receptors with 99mTc-EDDA/HYNIC-[Lys3]-bombesin: biokinetics and dosimetry in women.

BACKGROUND: The gastrin-releasing peptide receptor (GRP-R) is expressed in several normal human tissues and is overexpressed in various human tumors including breast, prostate, small-cell lung cancer and pancreatic cancer. Recently, 99mTc-EDDA/HYNIC-[Lys]-bombesin (99mTc-HYNIC-BN) was reported as a radiopharmaceutical with high stability in human serum, specific cell GRP-R binding and rapid cell internalization. AIM: The aim of this study was to determine the biokinetics and dosimetry of 99mTc-HYNIC-BN and the feasibility of using this radiopharmaceutical to image GRP-R in four early breast cancer patients and seven healthy women. METHODS: Whole-body images were acquired at 20, 90, 180 min, and 24 h after 99mTc-HYNIC-BN administration. The same regions of interest were drawn around source organs on each time frame and regions of interest were converted to activity (conjugate view counting method). The image sequence was used to extrapolate 99mTc-HYNIC-BN time-activity curves in each organ to calculate the total number of disintegrations (N) that occurred in the source regions. N data were the input for the OLINDA/EXM code to calculate internal radiation dose estimates. RESULTS: 99mTc-HYNIC-BN had a rapid blood clearance with mainly renal excretion. No statistically significant differences (P>0.05) in the radiation-absorbed doses among cancer patients and healthy women were observed. The average equivalent doses (n=11) were 24.8+/-8.8 mSv (kidneys), 7.3+/-1.8 mSv (lungs), 6.5+/-4.0 mSv (breast), 2.0+/-0.3 mSv (pancreas), 1.6+/-0.3 mSv (liver), 1.2+/-0.2 mSv (ovaries), and 1.0+/-0.2 mSv (red marrow). The effective dose was 3.3+/-0.6 mSv. The images showed well-differentiated concentration of 99mTc-HYNIC-BN in cancer mammary tissue. CONCLUSION: All the absorbed doses were comparable with those known for most of the 99mTc studies. 99mTc-HYNIC-BN shows high tumor uptake in breasts with malignant tumors so it is a promising imaging radiopharmaceutical to target site-specific early breast cancer. The results obtained warrant a further clinical study to determine specificity/sensibility of 99mTc-HYNIC-BN.

Biokinetics and dosimetry of 188Re-anti-CD20 in patients with non-Hodgkin's lymphoma: preliminary experience.

BACKGROUND: Radioimmunotherapy is a molecular targeting treatment for high-risk leukemia and lymphoma. Rhenium-188-labeled anti-CD66 monoclonal antibody has been used successfully in patients with high-risk acute myeloid leukemia or myelodysplastic syndrome. Our aim was to establish the biokinetics of (188)Re-anti-CD20 in patients and to evaluate its dosimetry as a target-specific radiopharmaceutical for non-Hodgkin's lymphoma (NHL) radioimmunotherapy. METHODS: Whole-body images were acquired at various times after administration of (188)Re-anti-CD20, obtained from instant freeze-dried kit formulations with radiochemical purity >95%. Regions of interest (ROIs) were drawn around source organs in each time frame. The cpm of each ROI was converted to activity using the conjugate view counting method. The image sequence was used to extrapolate time-activity curves in each organ to calculate the total number of disintegrations (N) that occurred in the source regions. N data were the input for the OLINDA/EXM code to calculate internal radiation dose estimates. RESULTS: Dosimetric studies indicated that after administration of 4.87-8.72 GBq of (188)Re-anti-CD20, the absorbed dose to total body would be 0.75 Gy, which corresponds with the recommended dose for NHL therapies. CONCLUSIONS: The calculated absorbed doses of (188)Re-anti-CD20 indicate that it may be used in radioimmunotherapy. Therefore, these preliminary data justify a full assessment of the safety, toxicity, and efficacy of (188)Re-anti-CD20 in a clinical study.