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. 2023 Nov 29;4(6):e421. doi: 10.1002/mco2.421

TABLE 1.

RNA m6A modification, targets, and drugs in clinical trials.

Target Inhibitor Mechanism Cancer type Clinical trial Phase Status References
METTL3 STC‐15 Inhibiting the catalytic activity of METTL3 Acute myeloid leukemia NCT05584111 I Recruiting N/A
STM2457 Competitive binding to the binding site of the SAM myeloid leukemia N/A N/A N/A 120
FTO Entacapone Regulating the FTO–FOXO1 signaling pathway Gastrointestinal stromal tumor NCT04006769 I Recruiting 121
R‐2HG Activating expression of RARA Leukemia N/A N/A N/A 122
FB23‐2 Activating expression of ASB2 Leukemia N/A N/A N/A 123
Saikosaponin‐D Increasing global m6A RNA methylation Leukemia N/A N/A N/A 124
CS1/CS2 Inhibiting expression of immune checkpoint genes Leukemia N/A N/A N/A 125
Dac51 Blocking immune evasion Lung cancer and melanoma N/A N/A N/A 126
ALKBH5 ALK‐04 Reducing m6A levels, abnormal splicing, Mct4/Slc16a3 expression, and lactate level Melanoma N/A N/A N/A 127
IGF2BP2/3 CWI1‐2 Inhibiting glutamine metabolism regulated by MYC, GPT2, and SLC1A5 Acute myeloid leukemia N/A N/A N/A 128