Article
Development of Radiohalogenated Osimertinib Derivatives as Imaging Probes for Companion Diagnostics of Osimertinib.
Journal of medicinal chemistry - 10 Feb 2022
Mishiro Kenji, Nishii Ryuichi, Sawazaki Izumi, Sofuku Tomoki, Fuchigami Takeshi, Sudo Hitomi, Effendi Nurmaya, Makino Akira, Kiyono Yasushi, Shiba Kazuhiro, Taki Junichi, Kinuya Seigo, Ogawa Kazuma
Abstract excerpt
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...
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