BARC/PUB/2015/1367

 
 

Ga-68 NODAGA RGD: A PET radiopharmaceutical for integrin αvβ3imaging

 
     
 
Author(s)

Vatsa, R.; Bhusari, P.; Kumar, S.; Singh, G.; Chakraborty, S.; Dash, A.; Dhawan, D. K.; Shukla, J.; Mittal, B. R.
(BARC)

Source

European Journal of Nuclear Medicine and Molecular Imaging, 2015. Vol. 42 (S1): pp. S466-S467

ABSTRACT

Angiogenesis plays a key role in the growth and metastases of solid tumors which is strongly regulated by integrin αvβ3. Over expression of integrin αvβ3 is noted in various carcinomas including lung, prostate and breast. Radiolabeled RGD tripeptide can be used to image the over expression of this integrin non-invasively. The aim of the present study was to image αvβ3 over expression in breast and lung carcinoma patients using in-house radiolabeled Ga-68 NODAGA-RGD. Materials and Method: Radiolabeling of NODAGA-RGD was optimized in- house using Ga-68. Radiolabeling was performed at room temperature for 20 min and at 95°C for 5 min. Radiochemical yield was assessed by ITLC. Characterization of radiolabeled product was done by radio-HPLC and MALDI-TOF mass spectrometry. Patients before any definitive treatment (Chemotherapy/Surgery) were enrolled in the study after obtaining clearance from institute ethics committee and written informed consent from patients (breast n=40, lung n=5). Whole body acquisition was done 45 min post intravenous administration of 111MB-185MBq of Ga-68- NODAGA-RGD on a dedicated hybrid PET-CT scanner with 90 sec per bed position. Attenuation correction of the emission images was done using CT. Results: The radiolabeling yield at room temperature was 50-60%. However yield was more than 90% after 5 min heating at 95°C.radio-HPLC showed good radiolabeling. Increase in molecular weight near the weight of Ga-68 on MALDI-TOF reconfirmed attachment of Ga-68 with NODAGA-RGD. The post purification radio-ITLC showed >99% radiochemical purity. All the samples were found to be sterile on sterility test with the endotoxins content <4 EU/ml. The residual ethanol content was <2500ppm in all samples. Physiological uptake of radiotracer was seen in ventricles, salivary glands, thyroid, liver and spleen with excretion through the kidneys. Variable radiotracer uptake was with the SUVmax ranging from 2.89 to 21.12 in breast carcinoma and 1.40 to 7.82 in lung carcinoma. Metastatic lesions were also detected in patients. No adverse reactions were seen post administration of the radiopharmaceutical. Conclusion:Ga-68 labeled NODAGA-RGD synthesis is quick with good radiochemical purity. Good tumor to background ratio was observed in breast and lung carcinoma patients. Metastatic lesions were well visualized. The study indicated that Ga-68 labeled NODAGA-RGD have great potential for imaging angiogenesis.

 
 
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