KinasePro

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

Better Chemistry = Better Drugs

Posted by kinasepro on December 29, 2006

Wull Duh? But in this case it’s a webcast on medchem from some mostly non-chemists: David Snitman, Paul Goddard, Arthur Sands, and Jim Mahoney of Array, ARYx, Lexicon, and Surface Logix respectively.


Array: (From an actual chemist) We’ve got MEK inhibitors. They were in Prague too? Cool.

CN1C2=CC(C(NOCCO)=O)=C(NC3=CC=C(Br)C=C3Cl)C(F)=C2N=C1

>> Aside >> Hadn’t seen the structure before. These look an aweful lot like Pfizer’s ‘non-atp competitive’ compounds: PD184352 was discontinued in ’05, but they have PD-325901 currently in Ph2:

O=C(NOCC1CC1)C2=CC=C(F)C(F)=C2NC3=CC=C(I)C=C3Cl O=C(NOC[C@H](O)CO)C1=CC=C(F)C(F)=C1NC2=CC=C(I)C=C2F<</

ARYx: We just patent bust

Lexicon: We pick new targets. Knockouts … Talks about lx2931, but doesn’t really say anything new.

Surface Logix: mublemumblemumble… Med Chem? Yah we got guys doing that, blabalabla Rho Kinase blabla mumble mumble. Cute animation here.

Drats, The target audience was a bunch of financial advisors I gather, but still… With a title like that I had high hopes. Amusingly David rips on Tykerb and he’s right to point out that it’s taking 1.25g of an insoluble drug to do what it does. Jim talks about protien binding driving their efforts which I guess is interesting, and they all rip on the ‘big biotech'(Biogen / Amgen / Genentech) lack of small molecule productivity.

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5 Responses to “Better Chemistry = Better Drugs”

  1. weirdo said

    “they all rip on the ‘big biotech’(Biogen / Amgen / Genentech) lack of small molecule productivity.”

    That’s pretty funny. How, exactly, do they know? Like Big Pharma, every little rat study that produces a statistically significant (even if usefully insignificant) result no longer results in a press release for “Big Biotech”. Heck, for many, Phase 1 study starts don’t even merit a press release.

    And I’m sure “milkshake” will jump on me for this one, but a “little biotech” milestone simply isn’t the same as a “Big Biotech” or “Big Pharma” milestone. “Little Biotechs” will take molecules forward that “Big XXXXX” will not; and do less work on them. It is no more complext than that. (Yes, there are exceptions to this rule!). And 90% of those will fail; Pfizer will buy the other 10% after a successful Phase 2a.

    Which approach is better? You be the judge.

    KinasePro: your blog is truly awesome, and a great asset to the field. You are, in fact, a pro.

  2. kinasepro said

    I appreciate being held in such high esteem by such a… umm… well… a uh, you wierdo. I also look forward to more of this kind of thing popping up.

  3. milkshake said

    I agree: a startup is likely to overplay the success story to impress the investors. (I spent couple of years at one startup – and half-baked results and proof-of concept projects were routinely presented as “core technology” by our management). I have been discouraging my friends from investing into biotech/pharma startup stocks for this reason.

    I heard that Genentech has been trying to start their own small-molecule programs for several years now but have not been very successful.

  4. kinasepro said

    I’ve been on both sides of the fence. Its probably healthy to argue the pros and cons to the different approaches, but until the hemmoraging stops and the industry as a whole starts growing again… I’d say its pretty clear that noone’s got a lock on how to do this stuff best.

  5. Derek Lowe said

    Amen to that last comment. I’ve been saying something similar for a while about the various big-pharma approaches (run a lot of projects vs. run a few big whoppers, do follow ups out the wazoo versus never do them, etc.) If there were a clear optimal strategy, someone would be eating everyone else’s lunch with it.

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