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RISS 인기검색어
- 검색키워드
- 저자 : Markus Schwaiger (검색결과 2 건)
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Antonia Richter,Karina Knorr,Martin Schlapschy,Stephanie Robu,Volker Morath,Claudia Mendler,Hsi-Yu Yen,Katja Steiger,Marion Kiechle,Wolfgang Weber,Arne Skerra,Markus Schwaiger 대한핵의학회 2020 핵의학 분자영상 Vol.54 No.2
Purpose PASylation® offers the ability to systematically tune and optimize the pharmacokinetics of protein tracers for molecular imaging. Here we report the first clinical translation of a PASylated Fab fragment (89Zr∙Df-HER2-Fab-PAS200) for the molecular imaging of tumor-related HER2 expression. Methods A patient with HER2-positive metastatic breast cancer received 37 MBq of 89Zr∙Df-HER2-Fab-PAS200 at a total mass dose of 70 μg. PET/CT was carried out 6, 24, and 45 h after injection, followed by image analysis of biodistribution, normal organ uptake, and lesion targeting. Results Images show a biodistribution typical for protein tracers, characterized by a prominent blood pool 6 h p.i., which decreased over time. Lesions were detectable as early as 24 h p.i. 89Zr∙Df-HER2-Fab-PAS200 was tolerated well. Conclusion This study demonstrates that a PASylated Fab tracer shows appropriate blood clearance to allow sensitive visualization of small tumor lesions in a clinical setting.
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Kim, Dong-Yeon,Kim, Hyeon Sik,Reder, Sybille,Zheng, Jin Hai,Herz, Michael,Higuchi, Takahiro,Pyo, AYoung,Bom, Hee-Seung,Schwaiger, Markus,Min, Jung-Joon Society of Nuclear Medicine 2015 The Journal of nuclear medicine Vol.56 No.10
<P>Despite substantial advances in the diagnosis of cardiovascular disease, there is a need for <SUP>18</SUP>F-labeled myocardial perfusion agents for the diagnosis of ischemic heart disease because current PET tracers for myocardial perfusion imaging have a short half-life that limits their widespread clinical use in PET. Thus, <SUP>18</SUP>F-labeled fluoroalkylphosphonium derivatives (<SUP>18</SUP>F-FATPs), including (5-<SUP>18</SUP>F-fluoropentyl)triphenylphosphonium cation (<SUP>18</SUP>F-FPTP), (6-<SUP>18</SUP>F-fluorohexyl)triphenylphosphonium cation (<SUP>18</SUP>F-FHTP), and (2-(2-<SUP>18</SUP>F-fluoroethoxy)ethyl)triphenylphosphonium cation (<SUP>18</SUP>F-FETP), were synthesized. The myocardial extraction and image quality of the <SUP>18</SUP>F-FATPs were compared with those of <SUP>13</SUP>N-NH<SUB>3</SUB> in rat models. <B>Methods:</B> The first-pass extraction fraction (EF) values of the <SUP>18</SUP>F-FATPs (<SUP>18</SUP>F-FPTP, <SUP>18</SUP>F-FHTP, <SUP>18</SUP>F-FETP) and <SUP>13</SUP>N-NH<SUB>3</SUB> were measured in isolated rat hearts perfused with the Langendorff method (flow velocities, 0.5, 4.0, 8.0, and 16.0 mL/min). Normal and myocardial infarction rats were imaged with small-animal PET after intravenous injection of 37 MBq of <SUP>18</SUP>F-FATPs and <SUP>13</SUP>N-NH<SUB>3.</SUB> To determine pharmacokinetics, a region of interest was drawn around the heart, and time–activity curves of the <SUP>18</SUP>F-FATPs and <SUP>13</SUP>N-NH<SUB>3</SUB> were generated to obtain the counts per pixel per second. Defect size was analyzed on the basis of polar map images of <SUP>18</SUP>F-FATPs and <SUP>13</SUP>N-NH<SUB>3.</SUB> <B>Results:</B> The EF values of <SUP>18</SUP>F-FATPs and <SUP>13</SUP>N-NH<SUB>3</SUB> were comparable at low flow velocity (0.5 mL/min), whereas at higher flows EF values of <SUP>18</SUP>F-FATPs were significantly higher than those of <SUP>13</SUP>N-NH<SUB>3</SUB> (4.0, 8.0, and 16.0 mL/min, <I>P</I> < 0.05). Myocardium-to-liver ratios of <SUP>18</SUP>F-FPTP, <SUP>18</SUP>F-FHTP, <SUP>18</SUP>F-FETP, and <SUP>13</SUP>N-NH<SUB>3</SUB> were 2.10 ± 0.30, 4.36 ± 0.20, 3.88 ± 1.03, and 0.70 ± 0.09, respectively, 10 min after injection, whereas myocardium-to-lung ratios were 5.00 ± 0.25, 4.33 ± 0.20, 7.98 ± 1.23, and 2.26 ± 0.14, respectively. Although <SUP>18</SUP>F-FATPs and <SUP>13</SUP>N-NH<SUB>3</SUB> sharply delineated myocardial perfusion defects, defect size on the <SUP>13</SUP>N-NH<SUB>3</SUB> images was significantly smaller than on the <SUP>18</SUP>F-FATP images soon after tracer injection (0–10 min, <I>P</I> = 0.027). <B>Conclusion:</B> <SUP>18</SUP>F-FATPs exhibit higher EF values and more rapid clearance from the liver and lung than <SUP>13</SUP>N-NH<SUB>3</SUB> in normal rats, which led to excellent image quality in a rat model of coronary occlusion. Therefore, <SUP>18</SUP>F-FATPs are promising new PET radiopharmaceuticals for myocardial perfusion imaging.</P>
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