25 January 2022 – Race Oncology Limited (“Race”) is pleased is pleased to share details of a recent independent scientific publication in the journal Cells, confirming Zantrene® (bisantrene dihydrochloride) is a highly effective inhibitor of the Fat Mass and Obesity associated protein (FTO) with potential utility in Type 2 diabetes¹. Type 2 diabetes is characterized by chronic high blood sugar associated with impaired insulin secretion by the pancreas.

In this new work, the University of Lille team has identified that FTO plays a critical role in Type 2 Diabetes and that inhibition of FTO by Zantrene at a concentration (100 nM) – below the level observed from prior studies to cause toxicity – is able to increase the production of insulin by diabetic pancreatic tissue more than 20-fold.

This independent work builds on the original identification of Zantrene as a potent FTO inhibitor by Professor Chen and his team at the City of Hope Hospital in 2020 and confirmed by Prof He’s team at the University of Chicago in 2021^2,3.

Chief Scientific Officer, Dr Daniel Tillett said: “The independent confirmation that Zantrene is able to target FTO, this time in the pancreas, and reverse the impaired insulin secretion seen in Type 2 diabetes is of major significance. While further study is needed, it does emphasis the importance of m⁶A methylation deregulation and FTO in a wide range of human metabolic diseases beyond cancer.”

1. Bornaque, F. et al. (2022) Glucose Regulates m⁶A Methylation of RNA in Pancreatic Islets. Cells 11, 291.
2. Cui, YH., Yang, S., Wei, J. et al. (2021) Autophagy of the m⁶A mRNA demethylase FTO is impaired by low-level arsenic exposure to promote tumorigenesis. Nat Communications 12, 2183
3. Su, R., Dong, L., Li, Y., Gao, M., Han, L., Wunderlich, M., et al. (2020) Targeting FTO Suppresses Cancer Stem Cell Maintenance and Immune Evasion. Cancer Cell, 38(1), 79–96.e11