Kinase Chemistry – Just a year and a half behind the times.

Piper Jaffray

Posted by kinasepro on December 3, 2007

…It’s an investor dog and pony show, and it was last week. Who was there?

Exelixis: George Scangos had this to say on Kinase selectivity:

We get a lot of questions about whether we think that less specific multi-targeted kinase inhibitors are better then more specific kinase inhibitors. I think there is no general answer to that question. Personal view is when your working on the outside of the cell inhibiting a single molecule leads to efficacy, but the efficacy is limited and you can greatly increase the potency by hitting multiple targets at the same time without increasing the toxicity significantly, and I think there is plenty of clinical data now to show that that’s true.

On the other hand when your working downstream inside the cell in the biochemical pathway I think its important to be very specific and so we have a number of other compounds that work downstream within those pathways that are very specific so we tailor the compounds to what we think will optimize balance between efficacy and safety. We have some multi-targeted inhibitors we have some highly selective inhibitors, and we have some that hit a couple of targets.

They keep taunting us with bubble images of XL-880 and XL-184, So here have a guess:


There was also a bit on you should buy XL-647: its ‘More potent’, ‘More safe’ & ‘hits the T790M mutation’

Incyte: /Flexed on the impressive JAK inhibitor results they expect to tell you all about at ASH and beyond.

OSI: Now profitable with Tarceva, whose main competition interestingly enough is Alimta. It sounds like they are keeping OSI-906 for now, but OSI-930 and OSI-632 seem to be for sale.

Infinity: was there dropping some knowledge on the chaperoneness of HSP90 as it relates to kinase inhibitors and resistance.


2 Responses to “Piper Jaffray”

  1. milkshake said

    For cancer, multiple-target for sure. Metabolic diseases – probably not.

    I wonder how these cyclopropandicarboxamides hold in the presence of a nucleophile, like glutathione – because cyclopropane carboxylic cid tends to ring-open; the cyclopropane acts like a less-reactive cousin of a double bond.

  2. Cyclopropanes are sometime referred to as “fat double bonds”

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