Preparation of 125I-Nimotuzumab and Biodistribution Test in Normal Mice



Nimotuzumab labeled with gamma emitting radionuclide is a monoclonal antibody used to detect cancer that overexpress EGFR (epidermal growth factor receptor). Preparation, characterization and biodistribution study on normal mice of 125I nimotuzumab has been carried out. Labeling was carried out using iodogen as oxidator, variation in radioactivity of 125I and reaction time, followed by radiochemical purity test, stability test, biodistribution test on mice and clearance test on Wistar rats. Characterisation and radiochemical purity test were carried out using size exclusion HPLC and paper chromatography with 85% methanol as eluents. Stability on storage at 4°C was observed within 4 weeks. Biodistribution and clearance through urine and faeces was observed within 24 hours and 3 days post injection respectively. Optimal radiolabeling of nimotuzumab was obtained using 1 mCi of 125I in 20 minutes reaction time with radiochemical purity of 98,1% ± 1,2%, and upon storage at 4°C within 2 weeks decreased to 95,3% ± 0,9%. SE HPLC showed similar retention time of nimotuzumab before and after radiolabeling. Biodistribution showed high accumulation of radioactivity in kidneys, liver, spleen, and thyroid, among which the kidneys was the highest. Clearance at 24 and 72 hrs post injection showed faecal excretion of 8,8% ± 0,4% and 14,7% ± 1,1% respectively and renal excretion of 52,7% ± 2,9% and 82% ± 0,6%. respectively. From this experiments it can be concluded that nimotuzumab can be highly labeled with 125I with good stability, and excreted from the body mainly through kidneys.


1. Kartamihardja HS. Peranan kedokteran nuklir dalam deteksi dan lokalisasi infeksi/inflamasi, diktat Workshop Nasional Preparasi dan Aplikasi Radiofarmaka. Jakarta: RS Kanker Dharmais; 2006. 3-8.
2. Narra VR, Howell RW, Harapanhalli RS, Sastry RS. Radiotoxicity of some 1251 and 13‘1 labeled compounds in mouse testes: implications for radiopharrnaceutical design, J.Nucl Med. 1997. 35(12):2196-8.
3. Stephen JM. Radiolabelled antibody and peptides. In: Sampson CB. Textbook of radiopharmaceuticals : theory and practices 3rd ed. 1999. 63-82.
4. European Medicine Agency. Public summary of positive opinion for orphan designation of nimotuzumab for the treatment of pancreatic cancer. Evaluation of Medicines for human use. 2008. 1-4.
5. Crombet T, et al. The use of humanized anti-EGFR MAb (nimotuzumab) and irradiation for the treatment of high grade glioma patients. YM Bioscience. 2008.
6. Asgeirsson KS, Agrawal A, Allen C, Hitch A, Ellis 10, et al. Serum epidermal growth factor receptor and HER2 expression in primary and metastatic breast cancer patients, Research Article, Breast Cancer Research. 2007; [8 tayangan]. diambil dari URL: 6/R75, diakses Maret, 2012.
7. Morales A, Crespo FZ, Gandolf GN, lznaga EN, Peres NP, et al. l88Re-labeled anti-epidermal growth factor receptor humanized monoclonal antibody: labeling condition, in-vitro and in-Vivo stability. Nucl Med Biol. 2003. 25(9):703-1 1.
How to Cite
WIDYASTUTI, WIDYASTUTI; GUNAWAN, ADANG HARDI; RAHMAWATI, FITRI. Preparation of 125I-Nimotuzumab and Biodistribution Test in Normal Mice. JURNAL ILMU KEFARMASIAN INDONESIA, [S.l.], v. 11, n. 1, p. 70-75, apr. 2013. ISSN 2614-6495. Available at: <>. Date accessed: 24 june 2024.