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Re: mcbio post# 133543

Wednesday, 12/21/2011 10:36:35 PM

Wednesday, December 21, 2011 10:36:35 PM

Post# of 257389

Definitely getting crowded but that small Phase 1 trial showed activity in patients that I believe had all failed Herceptin and 81% failed Tykerb so that has to be encouraging I would think.



It is an encouraging sign, but other compounds like afatinib and neratinib have already shown some activity in heavily pre-treated patients and are much further along in development. These two compounds also inhibit EGFR, so ARRY-380 may have a tolerability advantage in this regard.

It's reversible per ARRY's Web site (www.arraybiopharma.com/ProductPipeline/Cancer/HER2.asp ). Which is preferable and why?



Thanks - I actually did skim over the webpage before I posted the question, but somehow missed it. I don't know to what extent it is usually the case in the clinic, but irreversible inhibition is associated with greater potency (at the expense of increased on-target side effects). That could be a factor, but as I said, it might not necessarily play out this way in the clinic.

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