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Re: vinmantoo post# 145564

Tuesday, 07/17/2012 12:50:15 PM

Tuesday, July 17, 2012 12:50:15 PM

Post# of 257382

How does the Ponatinib data stack up to the recent data for Regorafenib in GIST patients whose disease has progressed after both Gleevec and Sutent?



Well obviously someone would have to run a trial to find out for sure, but it is clear that the side effect profile of pona would be dramatically better. It's hard to compare across arrays, but FWIW, the IC50 of pona against wild-type c-Kit is in the 7 nm range (at current 45mg dose the Cmax is 132 nm and trough is 60 nm), while the IC50 for regorafenib is 17 nm. Likely it's more important what the comparative activity is against mutated versions though.

This poster shows some curves comparing pona to other TKIs( not regorafenib) for c-Kit and some other TK's of interest:

http://www.ariad.com/pdf/Gozgit_2012_AACR_POSTER_Ponatinib_noQRcode.pdf

Peter

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