RAC Primer, page-459

Preclinical BC results highlighted sensitivity of Bisantrene in BC cells resistant to other therapies at low nM concentrations, indicating FTO mechanism of action. This preclinical study highlights the patient population we should be targeting - metastatic & resistant to therapies.

I am still dubious about anthracene activity. In theory it works, but I'll need to see more evidence before I can be certain. I have my doubts about the safety and tolerability of 250 mg/m2/d compared to 320 mg/m2 single bolus. We have pretty good phase 3 BC data in a non-specific patient population, which indicates that this regimen is safe and tolerable. Building on this trial with a targeted population where an FTO inhibitor would he more effective should provide some interesting results. There's an interesting P2 BC trial that demonstrated the highest clinical response rate compared to other BC trials that used a 5-day 80 mg/m2/d regimen repeated every 3 weeks (IIRC). Clearly, 80 mg/m2 is not a high enough dose for anthracene function, which implicates FTO MoA.