btw: XL-880 is now going by GSK-1363089
Posted by kinasepro on March 19, 2009
Posted by kinasepro on March 18, 2009
Posted by kinasepro on August 23, 2008
GSK’s AKT Alkynes?
Yah, you heard it here first. So Technically these are at least 3 years behind the times…
Posted by kinasepro on November 28, 2007
GSK’s been looking at Plk1 for quite a while. Sure the structure was in an earlier application (March), but here it is better late then never. See: WO/2004/074244, WO/2004/087652, WO/2005/019193, WO/2007/030361, US20070010668, & US20070270437
And Vertex has an interesting series of series of Rock inhibitors in WO/2007/133622. Ki is reported to be <100 nM and clean across the cyps.
Oh yah, and if your curious about Cyclacel’s Aurora inhibitor CYC-116, they’ve narrowed it down to 1 of 3 for you and they also give an in vitro panel in WO/2007/132220, WO/2007/132221, WO/2007/132228. The claims make it look like the morpholine.
Posted by kinasepro on June 19, 2007
aka GW-786034 is GSK’s ‘pan Vegfr’ inhibitor:
Posted by kinasepro on May 13, 2007
aka GW-786034 is GSK’s ‘pan Vegfr’ / TIE2 inhibitor:
Posted by kinasepro on April 8, 2007
Tykerb ®, lapatinib, GW-572016
Discovery: Glaxo UK: WO/1999/35146
US Approval: March 2007
Posted by kinasepro on April 5, 2007
Earlier Ranbaxy had WO/2006/082492 and now its: WO/2007/036791. Add to that GSK has 2 oral P38 inhibitors in the clinic but despite some crafty wording of a recent Ranbaxy press release, the current clinical batch wasn’t an Indian invention. It looks as though GSK has shipped finding more backups overseas.
One of them is likely from WO/2006/134382 (compound on the left) The other? Not so obvious. There’s a number of GSK p38 applications, but my guess is it hails from the pyrimidopyridone scaffold: Something like: WO/2003/088972 (above) or WO/2006/104915
Posted by kinasepro on March 14, 2007
After announcement of the positive Ph3 it seemed like just a matter of time, and that time has come. Tykerb gets FDA approval in combination with Xeloda for treatement of advanced metatatic breast cancer where the cancer overexpresses Her2 as a second line therapy. And yes that is a mouthful… a 1.25g/d mouthful, worth eventually an estimated 1b/y.