A novel concept of radiosynthesis of a 99mTc-labeled dimeric RGD peptide as a potential radiotracer for tumor imaging |
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Authors: | Sweety Mittal Mohini Bhadwal Sudipta Chakraborty H.D. Sarma Sharmila Banerjee M.R.A. Pillai |
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Affiliation: | 1. Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai 400085, India;2. Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai 400085, India |
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Abstract: | Radiolabeled Arg-Gly-Asp (RGD) peptides are promising agents for non invasive imaging of αvβ3 expression in malignant tumors. The integrin αvβ3 binding affinity and consequent tumor uptake could be improved when a dimeric RGD peptide is used as the targeting moiety instead of a monomer. Towards this, a novel approach was envisaged to synthesize a 99mTc labeled dimeric RGD derivative using a RGD monomer and [99mTcN]+2 intermediate. The dithiocarbamate derivative of cyclic RGD peptide G3-c(RGDfK) (G3 = Gly-Gly-Gly, f = Phe, K = Lys) was synthesized and radiolabeled with [99mTcN]+2 intermediate to form the 99mTcN-[G3-c(RGDfK)]2 complex in high yield (~98%). Biodistribution studies carried out in C57/BL6 mice bearing melanoma tumors showed good tumor uptake [4.61 ± 0.04% IA/g at 30 min post-injection] with fast clearance of the activity from non-target organs/tissue. Scintigraphic imaging studies showed visible accumulation of activity in the tumor with appreciable target to background ratio. |
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