In this study, we showed the presence of BAY1436032, a fluorine-containing inhibitor of the R132X-mutant isocitrate dehydrogenase and phase I study drug (NCT02746081) in the target volume of glioma mouse models and its on-target activity through direct detection of decreasing 2-HG production in mIDH1 gliomas. Here, IDH3A is linked to central nervous system cancer.