FT-2102 is a potent, orally bioavailable IDH1-mutant inhibitor that has been demonstrated to inhibit 2-HG production in xenograft mouse models and has the potential to penetrate the blood–brain barrier.58 It is currently in phase I clinical trials in combination with ASTX727 (DNA methytransferase inhibitor) (NCT04013880) and in combination with azacitidine or cytarabine in patients with AML or MDS (NCT02719574). Here, IDH1 is linked to acute myeloid leukemia.