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


Posted by kinasepro on October 31, 2006

Couple things…

  • Looks like Org Syn volume 84 is starting to roll out on the web.
  • Pipeline looks to be down today 😦
  • Some Canadian company, bought some company in Tucson that has some kinase inhibitors (Pi3K, and AKT) ‘in late preclinical development’. For those of us following along at home, that’s code for having compounds with A) crummy PK B) poor selectivity C) CYP issues – or more likely – all of the above. Only reason I can see to list all the programs in the press release is that they are now for sale. Any bets on what they do with the American side of the company?
  • Array announced its p38 program is ready for prime-time. (Of note Array has some of their patents applications downloadable) From that list it looks like plenty of MEK and AKT inhibitors… but P38? Yah there’s a couple from ’04.

3 Responses to “Details…”

  1. milkshake said

    I knew a process chemist from Array and he did not have kind words about their management.

    I will be interested in their data after phase IIb, when the potential for liver tox becomes more clear. So far it has been a show-stopper for every p38 program I heard about. Array has been developing p38 compounds for a while and maybe they need to please investors now. You have to be careful about anouncements and publications from small companies, it is often a half-baked stuff which is presented as a great achievement.

  2. kinasepro said

    Hi Milkshake, Who knows about Array, but my take on P38 is that it does some pretty cool things with the aminal models.

    So much so that companies with a significant investment in p38 programs are reluctant to give them up. That said, some of the big players: BMS, Roche, Vertex etc. are still going full steam P-3-8 and the true believers blame the previous failures on things like off target activity. Shouldn’t be too long before we can put it to bed.

  3. milkshake said

    There is also a recent J&J paper on old class BMS-like p38 compounds and it looks like they may consider going into clinic with it again – but not with the Scios compounds. Keeping an old program alive is one thing but another is to start a new one -unless things change and one of the companies gets some decent late-stage results. AFAIK investors are hesitant to put their money into p38 now.

    It is easy to blame some upstream kinase/isoform/autophosphorylated form inhibition for problems but the fact is that any new antiinflammatory has to have a great safety margin.

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