Background
The Ras-Raf-MEK-ERK regulation pathway is involved in numerous cases of cancers. In 2018, the FDA approved binimetinib, a specific allosteric MEK1/2 inhibitor developed for the BRAF positive melanoma treatment1. The two fluorine atoms on the structure allow a potential fluorine‑18 isotopic labeling for PET applications.
Aims
The purpose of our work is to develop a method for the fluorine‑18 isotopic labeling of binimetinib for its evaluation as a potential selective tracer to monitor BRAF mutation. However, binimetinib exhibits two aromatic fluorine atoms located both on inactivated positions, making [18F]binimetinib radiosynthesis a strong radiochemistry challenge.