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- 저자 : Jeffrey Klenc (검색결과 1 건)
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Initial Evaluation of 99mTc(CO)3(ASMA) as a Renal Tracer in Healthy Human Volunteers
Malgorzata Lipowska,Jeffrey Klenc,Russell D. Folks,Andrew T. Taylor 대한핵의학회 2014 핵의학 분자영상 Vol.48 No.3
Purpose Preclinical studies in rats showed that two of99mTc(CO)3(ASMA) isomers (rac- and L-ASMA) had pharmacokineticproperties equivalent to that of 131I-OIH, theradiopharmaceutical standard for the measurement of effectiverenal plasma flow. The aim of this study was to evaluatethe pharmacokinetics of 99mTc(CO)3(ASMA) isomers inhealthy human subjects. Methods Three ASMA ligands (rac-, L- and D-ASMA) werelabeled with 99mTc(CO)3 using an IsoLink kit (Covidien), andeach formed 99mTc(CO)3(ASMA) tracer was co-injected with131I-OIH into healthy human subjects followed by sequentialimaging, plasma clearance measurements and timed urinecollection. Plasma protein binding, red cell uptake and percentinjected dose in the urine were determined. Urine from eachgroup of volunteers was analyzed for metabolites by HPLC. Results Image quality was excellent with all three agents. Each 99mTc(CO)3(ASMA) preparation was excreted unchangedin the urine. The plasma clearance ratio(99mTc(CO)3(ASMA)/131I-OIH) was 81±3 % for D-ASMAcompared to only 20±4 % for L-ASMA and 37±7 % for rac-ASMA; the 81%clearance ratio for D-ASMA isomer is still∼30 % higher than the 99mTc-MAG3/131I-OIH clearance ratio(∼50-60 %). Red cell uptake was similar for all three tracers(6-9 %), and all tracers had a relatively rapid renal excretion;at 3 h, the 99mTc(CO)3(ASMA)/131I-OIH urine ratio was 100±3%for D-ASMA, 80±2%for L-ASMA and 88±1%for rac-ASMA. Conclusions The renal excretion characteristics of99mTc(CO)3(D-ASMA) in humans are superior to those ofthe other two 99mTc(CO)3(ASMA) isomers studied, but arestill inferior to 131I-OIH, even though there was no differencein the clearance of two of 99mTc(CO)3(ASMA) isomers and131I-OIH in rats. The work described here demonstrates thes e n s i t i v i t y i n i n vivo biologi c a l behavior of99mTc(CO)3(ASMA) isomers to their subtle structuraldifferences.
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