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

LY333531 / Arxxant

Posted by kinasepro on November 13, 2006

Hi Lilly, So are you guys any closer to market with this protein kinase C-beta inhibiting staurosporine analog, Ruboxistaurin, or not?



I see you announced today the ‘results‘ of your diabetic retinopathy phase iii study. The FDA asked for more data back in August, and its still not clear if we’re going to see an approval, a new trial, or a withdrawal.

J Med Chem 1996, 2664
Org lett 2001, 3409


5 Responses to “LY333531 / Arxxant”

  1. Eric said

    What does the little s in the structure represent?

  2. kinasepro said


    If this compound gets approved it will be the first chiral kinase targetting drug.

  3. Eric said

    Thanks, haven’t seen that listed on a structure before.

  4. Bruce007 said

    The “S” is a stereochemical descriptor (standardized term) to indicate the arrangement of atoms in space around the carbon stereocenter, according to the Cahn-Ingold-Prelog rules for chemical nomenclature. The original journal article was published in 1967 in Angewandte Chemie. The choice in this case is “R” (rectus, for righthanded) or “S” (sinister, for lefthanded).

  5. Jim Kerhin said

    I was a test subject (type1 since 1975) for ly333531 from about 2001-2003?? in Milwaukee. I believe they were studying Macular Edema. I had a little but it seemed to have been stopped during the study period and for a few years after. I’d sure like to know more about getting some more. I’m a believer!

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