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Re: mcbio post# 210889

Thursday, 04/27/2017 10:22:22 PM

Thursday, April 27, 2017 10:22:22 PM

Post# of 251272
AKBA FGEN GSK and PHD Inhibitors:

The cite you indirectly gave ( https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4497972/ ) is a perfect example of the fact that we really don't know much about the target differences between Roxadustat and Vadadustat. For instance it says:

Roxadustat:

"FG-4592 inhibits all three HIF-PHDs" (no comparative IC50s)


Vadadustat:

"AKB-6548 stabilizes HIF2a to a greater extent than HIF1a" (no comment on relative PHD inhibition)

In contrast the paper provides much more information about the GSK and Bayer compounds (it gives IC50s for all 3 PHDs for Bayer, and for 2 IC50s for GSK). But for AKBA and FGEN... pretty much squat.

That said, even if we knew the relative IC50s for each PHD I don't think it would tell us much because PHD/HIF system is at the nexus of a very very complex set of control loops - most of which we know little to nothing about. The best characterization I can cite is the one that JQ pointed out - that Roxa seems to have liver effects that Vada doesn't. (Random note: GSK, like Roxa, shows lipid lowering

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