Ann: Expanded Heart Protection Discovery for Zantrene, page-270

Looking a little deeper...

If we compare the cell viability measures from the recent cell paper to RAC's most recent expanded heart safety data, we find some very interesting comparisons.

Below is the cell viability of multiple myeloma (MM) cells after 60,000 nM of MA2. To me, this looks like between 30-40% cell killing.



Below is the cell viability of MM cells after treatment of varing nM concentrations of Zantrene. To me, it looks like there is roughly 50% cell killing at 15 nM and 90% cell killing at a concentration of 250 nM.



To put that into perspective:
At 15 nM, Zantrene has a concentration that is 4000 times lower than MA2 and is able to kill more MM cells.
At 250 nM, Zantrene has a concentration that is 240 times lower than MA2 and is able to kill more than double the MM cells.
At 250 nM, single agent Zantrene is able to kill more MM cells than MA2 and bortezomib combined.

Limitations:
They are not the same cell lines tested, so caution is encouraged when contrasting drug efficacy.

With that in mind, it is very clear to me that Zantrene is a much more potent and effective FTO inhibitor than MA2. In addition, it may be worthwhile considering the combination of Zantrene and Carfilzomib to the combination of MA2 to bortezomib. I'm looking forward to the in vivo studies and eventual partnership with Amgen.