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PET Imaging of Oncogene Overexpression Using ⁶⁴Cu-Vasoactive Intestinal Peptide (VIP) Analog: Comparison with ^99mTc-VIP Analog

¹ Department of Radiology, Thomas Jefferson University, Philadelphia, Pennsylvania
² Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, Pennsylvania
³ Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada
⁴ Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania
⁵ Department of Medicine, Thomas Jefferson University, Philadelphia, Pennsylvania
⁶ Department of Biochemistry and Molecular Pharmacology, Thomas Jefferson University, Philadelphia, Pennsylvania

View larger version (14K): [in a new window]   FIGURE 1. Schematic presentation of TP3982.

View larger version (22K): [in a new window]   FIGURE 2. Effect of increasing concentration of VIP28, unlabeled TP3654, and unlabeled TP3982, on resting opossum IAS smooth muscle tissue. At 1 x 10–6 mol/L TP3654 and TP3982, 95% relaxivity was achieved with 75% for VIP28 at the same concentration. Data suggest that biologic activity of TP3982 was not compromised.

View larger version (19K): [in a new window]   FIGURE 3. SELDI-TOF-mass spectrum of Cu-TP3982 complex, depicting the complex mass of 4,049.7 Da and the mass of unreacted TP3982 at 3,982.7 Da.

View larger version (17K): [in a new window]   FIGURE 4. HPLC elution profile of 64Cu-TP3982. 100% radioactivity was eluted in a single peak at Rt 8 min. Unbound 64Cu elutes at Rt 4.2 min. The diagonal line is percent solvent B (B = 0.1% TFA/ACN; A = 0.1% TFA/H2O).

View larger version (32K): [in a new window]   FIGURE 5. Composite of 3 representative 24-h images of T47D human BC bearing nude mice receiving 99mTc-TP3654 (left), 99mTc-TP3982 (center), and 64Cu-TP3982 (right). The gray scale in the first 2 -camera images was 0 to 50. The 1-mm coronal PET image of a mouse given 64Cu-TP3982 shows enhanced uptake in the tumor. -Camera images are in posterior position. Tumor is in right flank in each mouse.