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Vinay Kumar Banka,김영주,이윤상,정재민 대한방사성의약품학회 2020 Journal of radiopharmaceuticals and molecular prob Vol.6 No.2
[99mTc]Tc-Hexamethylpropylene amine oxime (HMPAO) is currently used as a regional cerebral blood flow imaging agent for single photon emission computed tomography (SPECT). The HMPAO ligand exists in two isomeric forms: d,l and meso showing different properties in vivo. Later studies indicated that brain uptake patterns of 99mTc-complexes formed from separated enantiomers differed. Separation of enantiomers is difficult by fractional crystallizations method. Usually, the substance is obtained in low chemical yield in a time-consuming procedure. Furthermore, the final product still contains some impurity. So we have developed new efficient route for synthesis of R,R - and S,S -HMPAO enantiomeric compounds in 6-steps. Nucleophilic substitution (SN2) reactions of 2,2-dimethylpropane-1,3-diamine either with S- (1a) or R-methyl-2-chloropropanoate (1b) were performed to produce compounds R,R- (2a) or S,S -isomer (2b) derivatives protected with benzylchloroformate (Cbz), respectively. And then Weinreb amide and methylation reaction using Grignard reagent, oxime formation with ketone group and deprotectiion of Cbz group by hydrogenolysis gave S,S- (7a) or R,R-HMPAO (7b), respectively. Entaniomeric compounds were synthesied with high yield and purity without any undesired product. The 7a or 7b kits containing 10 µg SnCl2-2H2O were labeled with 99mTc with high radiolabeling yield (90%).
<sup>188</sup>Re Labeled liver therapeutic drugs for hepatic carcinoma (HCC)
Seelam, Sudhakara Reddy,Banka, Vinay Kumar,Lee, Yun-Sang,Jeong, Jae Min Korean Society of Radiopharmaceuticals and Molecul 2019 Journal of radiopharmaceuticals and molecular prob Vol.5 No.1
$^{188}Re$ is one of the most readily available generator derived and useful radionuclides for therapy emitting ${\beta}^-$ particles (2.12 MeV, 71.1% and 1.965 MeV, 25.6%) and imageable gammas (155 keV, 15.1%). The $^{188}W/^{188}Re$ generator is an ideal source for the long term (4-6 months) continuous availability of no carrier added (NCA) $^{188}Re$ suitable for the preparation of radiopharmaceuticals for radionuclide therapy. Rhenium-188 has been used for the preparation of therapeutic radiopharmaceuticals for the management of diseases such as bone metastasis, rheumatoid arthritis and primary cancers. Several early phase clinical studies using radiopharmaceuticals based on $^{188}Re$ -labeled phosphonates, antibodies, peptides, lipiodol and particulates have been reported. In this review, we addressed the current development status of $^{188}Re$ radiopharmaceuticals for liver cancer therapy and their applications.
Ajit S Shinto,Indira VU,Kamaleshwaran KK,Vinay Kumar Banka,Aswathy KK,Thirumalaisamy SG,Rajamani V,Madhav Mallia,Sharmila Banerjee 대한방사성의약품학회 2015 Journal of radiopharmaceuticals and molecular prob Vol.1 No.2
Radiation synovectomy has been proposed as a promising palliative therapy for recurrent joint effusions for the last two or three decades. Ionizing radiations emitted by intrarticularly administered radiolabelled colloids. The aim of this study was to assess the effectiveness of radiation synovectomy (RSV) using 188Re-tin colloid in the treatment of recurrent joint effusions and chronic synovitis of knee joints. Three phase bone scan was acquired for the concerned joint prior to radiosynovectomy. 188Re-tin colloid was prepared as per the reported protocol. 9 patients, diagnosed with rheumatoid arthritis and suffering from chronic resistant synovitis of the knee, ankle or elbow joints were administered the radiopharmaceuticals, checked for radiochemical purity >95% by intraarticular route. A whole body scan was acquired 2 h post-radiosynovectomy. In all the 9 treatments, no leakage to non-target organs was visible in the whole body scan. Static scans of the joint revealed complete retention of 188Re-tin colloid in the joints post administration of the agent. Clinically all patients exhibited a complete or partial response. RSV with 188Re-tin colloid was safe and effective in patients with chronic synovitis of rheumatoid origin. J Radiopharm Mol Probes 1(2):109-117, 2015
Shinto, Ajit S,Indira, VU,Kamaleshwaran, KK,Banka, Vinay Kumar,Aswathy, KK,Thirumalaisamy, SG,Rajamani, V,Mallia, Madhav,Banerjee, Sharmila Korean Society of Radiopharmaceuticals and Molecul 2015 Journal of radiopharmaceuticals and molecular prob Vol.1 No.2
Radiation synovectomy has been proposed as a promising palliative therapy for recurrent joint effusions for the last two or three decades. Ionizing radiations emitted by intrarticularly administered radiolabelled colloids. The aim of this study was to assess the effectiveness of radiation synovectomy (RSV) using $^{188}Re$-tin colloid in the treatment of recurrent joint effusions and chronic synovitis of knee joints. Three phase bone scan was acquired for the concerned joint prior to radiosynovectomy. $^{188}Re$-tin colloid was prepared as per the reported protocol. 9 patients, diagnosed with rheumatoid arthritis and suffering from chronic resistant synovitis of the knee, ankle or elbow joints were administered the radiopharmaceuticals, checked for radiochemical purity >95% by intraarticular route. A whole body scan was acquired 2 h post-radiosynovectomy. In all the 9 treatments, no leakage to non-target organs was visible in the whole body scan. Static scans of the joint revealed complete retention of $^{188}Re$-tin colloid in the joints post administration of the agent. Clinically all patients exhibited a complete or partial response. RSV with $^{188}Re$-tin colloid was safe and effective in patients with chronic synovitis of rheumatoid origin.
188Re Labeled liver therapeutic drugs for hepatic carcinoma (HCC)
Sudhakara Reddy Seelam,Yun Sang Lee,Vinay Kumar Banka,Jae Min Jeong 대한방사성의약품학회 2019 Journal of radiopharmaceuticals and molecular prob Vol.5 No.1
188Re is one of the most readily available generator derived and useful radionuclides for therapy emitting βˉparticles (2.12 MeV, 71.1% and 1.965 MeV, 25.6%) and imageable gammas (155 keV, 15.1%). The 188W/188Regenerator is an ideal source for the long term (4-6 months) continuous availability of no carrier added (NCA) 188Resuitable for the preparation of radiopharmaceuticals for radionuclide therapy. Rhenium-188 has been used forthe preparation of therapeutic radiopharmaceuticals for the management of diseases such as bone metastasis,rheumatoid arthritis and primary cancers. Several early phase clinical studies using radiopharmaceuticalsbased on 188Re -labeled phosphonates, antibodies, peptides, lipiodol and particulates have been reported. In this review, we addressed the current development status of 188Re radiopharmaceuticals for liver cancertherapy and their applications.