Table 2 IDH mutant inhibitors.

N/A, not applicable; ND, not determined.

DrugTargetIC50Cancer indicationClinical trial
number
MutantWild-type/mutant
heterodimer
Wild type
AGI-5198IDH1R132H0.07 μMN/A>100 μMN/A
AG-120IDH1R132H12 nM12 nM71 nMLow-grade glioma
Hematologic
malignancies
Advanced
cholangiocarcinoma
NCT02481154
NCT03343197
NCT03071770
NCT02074839
NCT03503409
NCT02989857
NCT03173248
NCT02632708
NCT02677922
NCT03471260
NCT03564821
AGI-6780IDH2R140Q170 nM120 nM2.7 μMN/A
AG-221IDH2R140Q0.32 μM0.31 μM39.8 μMHematologic
malignancies
NCT03515512
NCT03383575
NCT03683433
NCT02577406
NCT01915498
NCT02387866
NCT02632708
NCT02273739
AG-881Pan-specific
mutant IDH
31.9 nM (IDH1R132H)
31.7 nM (IDH2R140Q)
N/AN/AHematological
malignancies
Low-grade glioma
Advanced solid tumors
NCT02492737
NCT02481154
NCT03343197
BAY1436032IDH1R132H15 nMN/A20 μMAdvanced malignanciesNCT02746081
NCT03127735
GSK321IDH1R132H4.6 nMN/A46 nMN/A
GSK864IDH1R132H15.2 nMN/A466.5 nMN/A
IDH305IDH1R132H0.027 nMN/A6.14 μMHematological
malignancies
NCT02381886
MRK-AIDH1R132H5 nMN/AN/DN/A