" Many FTO inhibitors have been developed (Table 2), and a few have advanced into preclinical and clinical trial phases (ref 185), including in cell and animal models for AML."
Ref 185: Canaani, J. et al. A phase II study of bisantrene in patients with relapsed/refractory acute myeloid leukemia. Eur. J. Haematol. 106, 260–266 (2021).
Table 2: Here is Table 2 below. Bisantrene is CS1 (small molecule).
CS1 (Bisantrene) and CS2: "These two compounds bind the catalytic pocket of FTO, within the substrate recognition domain, blocking access by m6A-modified substrates, exhibiting anti-leukaemic effects at very low concentrations190, activation of apoptosis signalling and inhibition of MYC pathways159. Preclinical pharmacological studies in AML mouse models have demonstrated their high therapeutic efficacy, including relapsed AML, at relatively low dosages185,190. CS1 and CS2 have marginal toxicity and high efficacy, positioning the two compounds as promising candidates for therapy. Currently, CS1/bisantrene is under clinical trials in combination with other drugs as a treatment for AML and metastatic breast cancer..".
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