@article{oai:repo.qst.go.jp:00085037,
 author = {Mishiro, Kenji and Nishii, Ryuichi and Sawazaki, Izumi and Sofuku, Tomoki and Fuchigami, Takeshi and Sudo, Hitomi and Effendi, Nurmaya and Makino, Akira and Kiyono, Yasushi and Shiba, Kazuhiro and Taki, Junichi and Kinuya, Seigo and Ogawa, Kazuma and Ryuichi, Nishii and Hitomi, Sudo},
 issue = {3},
 journal = {Journal of medicinal chemistry},
 month = {Jan},
 note = {Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor approved for treating non-small-cell lung cancer (NSCLC) with EGFR mutations. Genetic testing is required to detect the mutation for selecting patients who can use osimertinib. Here, we report an attempt to develop nuclear imaging probes that detect the EGFR mutations. We designed and synthesized I-osimertinib and Br-osimertinib with a radioactive or nonradioactive halogen atom at an indole ring in osimertinib and evaluated them.  assays suggested that both I-osimertinib and Br-osimertinib exhibit a specifically high activity toward NSCLC with EGFR L858R/T790M mutations. In biodistribution experiments, the accumulation of both [I]I-osimertinib and [Br]Br-osimertinib in tumors with mutations was significantly higher than that in blood and muscle. However, these osimertinib derivatives showed a significantly higher accumulation in lungs than in tumors. Therefore, for detecting the mutations in lung cancer, further structural modifications of the probes are required.},
 pages = {1835--1847},
 title = {Development of Radiohalogenated Osimertinib Derivatives as Imaging Probes for Companion Diagnostics of Osimertinib},
 volume = {65},
 year = {2022}
}