Table 1.

IDH1 inhibitors under clinical investigation in metastatic iCCA.

IC50 (µM)
Drug	IDH1 Mutation	Mutant	Wild-Type	Ref	Clinical Trial Number	Phase
AG-120	R132H R132C R132G R132L R132S	0.012 0.013 0.008 0.013 0.012	0.072	[124]	NCT02073994 NCT02989857 NCT04088188 2015-005117-72	I III I III
IDH305	R132H R132C	0.027 0.028	6.14	[125]	NCT02381886	I
FT-2102	R132H R132C	0.0212 0.0094	>20.0	[126]	NCT03684811 2018-001796-21	I/II Ib/II
BAY1436032	R132H R132C R132G R132L R132S	0.015 0.015 0.004 * 0.003 * 0.016 *	20.0	[127,128]	NCT02746081

* IC₅₀ evaluated on primary AML patient-derived cells [128].