Fluorinated Derivatives of AG-881 for Positron Emission Tomography Detection of Mutated Isocitrate Dehydrogenase 1
Thu Hang Lai·Barbara Wenzel·Winnie Deuther‐Conrad·Rodrigo Teodoro·Magali Toussaint·Aurélie Maisonial‐Besset·S Dukic-Stefanovic
Background/Objectives: Since 2016, the mutation of isocitrate dehydrogenase 1 (mIDH1) enzymes has become a major molecular marker for glioma classification and diagnosis. Moreover, the recent success of the INDIGO clinical trial on AG-881 (vorasidenib®), an aminotriazine-based mutated IDH1/2 inhibitor (IC50 = 6 nM/12 nM), validated the need for noninvasive detection of mIDH1 in brain tumors. This work is based on developing a series of novel fluorinated analogues of AG-881 and evaluating their p