170908-81-3Relevant articles and documents
Preparation, quality control and biodistribution studies of two [ 111In]-rituximab immunoconjugates
Jalilian, Amir R.,Sardari, Darush,Kia, Leila,Rowshanfarzad, Pejman,Garousi, Javad,Akhlaghi, Mehdi,Shanehsazzadeh, Saeed,Mirzaii, Mohammad
, p. 151 - 170 (2008)
In 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-tetra-acetic 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. Oesterreichische Apotheker-Verlagsgesellschaft m. b. H.
Development of 170Tm-DOTA-cetuximab for radioimmunotherapy
Shirvani-Arani, Simindokht,Bahrami-Samani, Ali,Jalilian, Amir Reza,Shirvani-Arani, Amirsaleh,Ghannadi-Maragheh, Mohammad
, p. 103 - 107 (2012)
Thulium-170 [T1/2=128.4days, Eβ(max)=968keV, Eγ=84keV (3.26%)] has radionuclidic properties suitable for use in therapy. 170Tm can be produced by a relatively feasible route involving thermal neutron bombardment on natural Tm(NO3)3 (100% 169Tm) in medium flux research reactors. The combination of beta-particle emission of Tm-170 with therapeutic properties of C225 monoclonal antibody (cetuximab) as well as optimization studies for future Tm-167 labeling was targeted in this study. Conjugated cetuximab was obtained by the addition of 0.5ml of a cetuximab pharmaceutical solution (1mg, in phosphate buffer, pH7.8) to a glass tube pre-coated with in situ prepared 1,4,7,10-tetraazacyclododecane- N,N,N,N-tetraacetic acid mono-(N-hydroxysuccinimidyl) ester (DOTA-NHS) (~5mg) at 25°C. Cetuximab was labeled with 170Tm-Thulium chloride (100MBq) after conjugation with DOTA-NHS in 2-3h (radiochemical purity >99%, instant thin-layer chromatography, specific activity=77-385TBq/mmol). Biodistribution studies in wild-type rats for free Tm-170 and the radioimmunoconjugate were performed to determine the distribution up to 72h. A comparative time-frame study was performed for critical organs for both radiochemical species. The major organs of accumulation were shown to be the lung, liver, and spleen, respectively.
CONJUGATES OF THE B-SUBUNIT OF SHIGA TOXIN FOR USE AS CONTRASTING AGENTS FOR IMAGING AND THERAPY
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, (2014/06/24)
Multivalent conjugates comprising the following formula: (STxB-linker A-S)x-GNS-(S-linker B-T)y wherein STxB is the B-subunit of Shiga toxin; linker A is a noncleavable linker; linker B is a cleavable linker used to release at least