Aptose Biosciences Inc (APTO)

[Tartiaboy]

Some interesting learnings. In vitro IDH1mut cells are more sensitive to Lux than are IDH1wt cells. In vivo, we see that TUSP is active against IDH2mut cells (at least in some combinations). TUSP showed a PR (not a CR) with an IDH1 patient. IDH1mut has been linked to the upregulation of PDGFRalpha. PDGFRalpha is a target kinase of Lux. There are reasons to think that TUSP and LUX together would be very effective against IDH1mut/IDH2mut. Of course there is not enough data to prove this, but there is enough to pay attention to it.

The kinomes inhibited by TUSP and LUX overlap to some degree, but they also each have unique targets. Together they cover an impressive array of valid kinase targets (i.e. targets shown in the literature to be relevant). Also impressive is the fact that both TUSP and LUX have good safety profiles at plasma levels up to 1 microM minimum.