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

Archive for the ‘Approved’ Category


Posted by kinasepro on June 3, 2009

aka Palladia, PHA-291639, & SU11654 got its FDA Approval today! Well… In dogs at least:.  It’s for canine mast cell tumors.

O=C(NCCN1CCCC1)C2=C(NC(/C=C3C(NC4=C\3C=C(C=C4)F)=O)=C2C)C yeh, its the pyrrolidine version of Sutent & its the phosphate salt

Posted in Approved, Pfizer | 8 Comments »

Tasigna Approved

Posted by kinasepro on October 30, 2007

aka nilotinib, AMN-107 is a Novartis‘ follow-on to Gleevec now approved for CML.


wiki; clinic; WO/2002/022597

Posted in Approved, bcr abl, gleevec, Novartis | 4 Comments »


Posted by kinasepro on October 2, 2007

So what are they worth?  TotallyMedicinal’s got the low-low.

TY TM for data: mirrored here.

Posted in Approved | Leave a Comment »

Kinase Inhibitors: On the market

Posted by kinasepro on April 8, 2007

Nothing new to see here, but its about time I got around to it. Here are the currently approved small molecule kinase inhibitors, with a few quick facts and links for each. Xcovery’s got what they’re worth.
Tykerb® , Sprycel®, Sutent®, Nexavar®, Tarceva®, Iressa®, and of course Gleevec®.

Posted in Approved | 2 Comments »

Tykerb ®

Posted by kinasepro on April 8, 2007

Tykerb ®, lapatinib, GW-572016


Discovery: Glaxo UK: WO/1999/35146
US Approval: March 2007

wiki; fda; PDB: 1XKK; Nature Reviews Drug Discovery

Posted in Approved, GSK | Leave a Comment »

Sprycel ®

Posted by kinasepro on April 8, 2007

Sprycel ®, dasatinib, BMS-354825


Discovery: Bristol-Myers Squibb WO/2000/062778
US Approval: June 2006

wiki; PDB: 2GQG; FDA; J Med Chem ’06 6819;

Named after its inventor?

Posted in Approved, BMS | Leave a Comment »

Sutent ®

Posted by kinasepro on April 8, 2007

Sutent ®, sunititnib malate, SU11248


Discovery: Sugen: Provisional filed February 15, 2000 WO/2001/060814. Sugen was bought by Pharmacia-Upjohn which in turn merged with Pfizer.
US Approval: January 2006

wiki; 557795-19-4

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Nexavar ®

Posted by kinasepro on April 8, 2007

Nexavar ®, sorafenib tosylate, BAY-439006


Discovery: Bayer WO/2000/042012
US Approval: December 2005

wiki; Org.Proc.Res.Dev. ’02, 777


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Tarceva ®

Posted by kinasepro on April 8, 2007

Tarceva ®, erlotinib hydrochloride, OSI-774


Discovery: Pfizer WO/1996/30347. Pfizer turned over the rights to OSI to meet U.S. FTC requirements related to Pfizer’s merger with Warner-Lambert in June 2000. The drug is jointly marketted by Genentech, and OSI.
US Approval: November 2004;

PDB: 1M17

Posted in Approved, Genentech, OSI | Leave a Comment »

Iressa ®

Posted by kinasepro on April 8, 2007

Iressa ®, gefitinib, ZD-1839


Discovery: Zeneca (UK) WO/1996/016960
US approval: May 2003
Label change: June 2005

FDA has approved new labeling for Iressa that states the medicine should be used only in cancer patients who have already taken the medicine and whose doctor believes it is helping them. New patients should not be given Iressa because in a large study Iressa did not make people live longer. There are other medicines for non-small cell lung cancer (NSCLC) that have shown an ability to make people live longer.

wiki; PDB: EGFR – 2ITY; Mutant EGFR: 2ITZ, 2ITO

Posted in Approved, Astra | Leave a Comment »