@article{oai:repo.qst.go.jp:00046032,
 author = {Yoshida, Chisato and Tsuji, Atsushi and Sudou, Hitomi and Sugyou, Aya and Sogawa, Chizuru and Inubushi, Masayuki and Uehara, Tomoya and Fukumura, Toshimitsu and Koizumi, Mitsuru and Arano, Yasushi and Saga, Tsuneo and 吉田 千里 and 辻 厚至 and 須藤 仁美 and 須尭 綾 and 曽川 千鶴 and 犬伏 正幸 and 上原 知也 and 福村 利光 and 小泉 満 and 荒野 泰 and 佐賀 恒夫},
 issue = {3},
 journal = {Nuclear Medicine and Biology},
 month = {Dec},
 note = {Introduction: C-kit is an important diagnostic and therapeutic target molecule for several malignancies, and c-kit-targeted drugs have been used clinically. Because abundant c-kit expression in tumors is a prerequisite for successful c-kit-targeted therapy, imaging of c-kit expression is expected to play a pivotal role in the therapeutic decision for each patient. We evaluated 64Cu-labeled Fab of anti-c-kit antibody 12A8 as a positron emission tomography (PET) imaging probe. Methods: 111In- or 125I-labeled 12A8 Fab were evaluated in vitro by cell binding, competitive inhibition, and cellular internalization assays and in vivo by biodistribution in mice bearing c-kit-expressing and -non-expressing tumors. Next, Fab fragment was labeled with the positron emitter 64Cu and evaluated by PET. Results: Radiolabeled 12A8 Fab showed specific binding to c-kit-expressing cells with high affinity, and internalized into cells after binding to c-kit on cell surface. Although tumor accumulation of [111In]Fab was lower than that of [111In]IgG, the faster blood clearance of [111In]Fab provided higher tumor-to-blood ratio at 6 h postinjection onwards. Blood clearance of 64Cu-labeled 12A8 Fab was slower than that of [111In]Fab, but PET using [64Cu]Fab clearly visualized the tumor at 6 h postinjection onwards. Conclusion: The 64Cu-labeled 12A8 Fab could be used for c-kit-specific PET imaging and might help in selecting appropriate patients for c-kit-targeted treatments.},
 pages = {331--337},
 title = {Development of Positron Emission Tomography Probe of 64Cu-labeled Anti-c-kit 12A8 Fab to Measure Protooncogene C-kit Expression},
 volume = {38},
 year = {2010}
}