Preparation, Quality Control and Biodistribution Studies of two [111In]-Rituximab Immunoconjugates
AbstractIn order to use Auger-electron therapeutic effects in CD20 antigen targeting in lymphomas, Mabthera™ (rituximab) was successively labeled with [111In]-indium chloride (185 MBq) after conjugation with freshly prepared macrocyclic bifunctional chelating agent, N-succinimidyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA-NHS) and ccDTPA separately. Conjugated-Rituximab was obtained by the addition of 1 ml of a rituximab pharmaceutical solution (5 mg/ml, in phosphate buffer, pH=7.8) to a glass tube pre-coated with freshly prepared DOTA-NHS or ccDTPA (0.01-0.1 mg) at 25°C. Radiolabeling was performed at 37°C in 3h and room temperature for one hour for DOTA-conjugate and DTPA-conjugate respectively. HPLC showed an overall radiochemical purity of 97.5 and 95% for DOTA and DTPA-conjugates respectively (Specific activity =2800-5600 GBq/mM). The final isotonic 111In-rituximab complexes were checked by gel electrophoresis for radiolysis. Preliminary biodistribution studies in normal rat model performed to determine radioimmunoconjugates distribution of up to 48h.
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JALILIAN, A.R.; SARDARI, D.; KIA, L.; ROWSHANFARZAD, P.; GAROUSI, J.; AKHLAGHI, M.; SHANEHSAZZADEH, S.; MIRZAII, M. Preparation, Quality Control and Biodistribution Studies of two [111In]-Rituximab Immunoconjugates. Sci. Pharm. 2008, 76, 151-170.
JALILIAN AR, SARDARI D, KIA L, ROWSHANFARZAD P, GAROUSI J, AKHLAGHI M, SHANEHSAZZADEH S, MIRZAII M. Preparation, Quality Control and Biodistribution Studies of two [111In]-Rituximab Immunoconjugates. Scientia Pharmaceutica. 2008; 76(2):151-170.Chicago/Turabian Style
JALILIAN, Amir R.; SARDARI, Darush; KIA, Leila; ROWSHANFARZAD, Pejman; GAROUSI, Javad; AKHLAGHI, Mehdi; SHANEHSAZZADEH, Saeed; MIRZAII, Mohammad. 2008. "Preparation, Quality Control and Biodistribution Studies of two [111In]-Rituximab Immunoconjugates." Sci. Pharm. 76, no. 2: 151-170.