KinasePro

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

BIBW-2992

Posted by kinasepro on September 7, 2007

BI’s irreversible ErbB inhibitor to join the Ph3 club.

O=C(/C=C/CN(C)C)NC3=CC2=C(N=CN=C2C=C3O[C@H]4COCC4)NC1=CC=C(C(Cl)=C1)F

>> update they’ve named it Tovok

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4 Responses to “BIBW-2992”

  1. TotallyMedicinal said

    Thoughts on aetiology?

    Bog standard quinazoline + Iressa style aniline + Zactima-style THF + Wyeth style acrylamide = Phase 3 candidate?

    Who says Big Pharma is struggling with innovation 🙂

  2. kinasepro said

    CI-1033, HKI-272 and EKB-569 are the direct comparators… I think it was actually Zeneca that got the irreversible ball rolling on the quinazoline architecture, but I guess its more important to see if any of these guys can get the ball over the goal line.

    And thank you for the word ‘aetiology’! Its been something I’ve become more interested in of late, but the term had escaped me…

  3. binding said

    Maybe they can get the irreversible ball rolling to the end if they target the most difficult to treat cancer types, because patients would have died anyway before they could complain…

  4. DrBaritone said

    This is rip off time continued. Irreversible inhibitors,….receptor occupancy!

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