Title

 

       
Approved      
Genentech (S. San Francisco, California) Herceptin (trastuzumab) mAb binds extracellular domain of ErbB2 September, 1998
Novartis (Basel) Gleevec (imatinib) Small molecule binds inactive form of Bcr-Abl May, 2001
Astra-Zeneca (London) Iressa (gefitinib) Small molecule binds to the ATP-binding site of the tyrosine kinase domain of EGFR July, 2003
Imclone Systems (New York) Erbitux (cetuximab) mAb competes with endogenous ligands for binding at EGFR, inducing receptor internalization February, 2004
OSI Pharmaceuticals (Uniondale, New York) Tarceva (erlotinib) Small molecule binds to the ATP-binding site of the tyrosine kinase domain of EGFR November, 2004
Bayer (West Haven, Connecticut) & Onyx Pharmaceuticals (Emeryville, California) Nexavar (sorafenib) Small-molecule Raf-1 inhibitor  
In the pipeline      
Pfizer (Sugen) (New York) Sutent (sunitinib malate) Small-molecule (indolinone) kinase inhibitor of VEGF and PDGF receptors, and FLT3 and Kit Phase 3
GlaxoSmithKline Lapatinib Small molecule with dual affinity for ErbB2 and EGFR Phase 3
Bristol-Myers Squibb (New York) Dasatinib Small-molecule inhibitor that binds active form of Bcr-Abl Phase 2
Novartis (Basel) AMN107 Small molecule with high affinity for Bcr-Abl Phase 2
Pfizer PD325901 Small-molecule, non-ATP-competitive MEK inhibitor Phase 2
Exelixis (S. San Francisco, California) XL880 Small-molecule, spectrum-selective Met/VEGFR inhibitor Phase 1
Array Biopharma (Boulder, Colorado) ARRY-142886 Small-molecule, non-ATP competitive MEK inhibitor Phase 1
National Cancer Institute (Bethesda, Maryland) Adaphostin Small-molecule, substrate-competitive Bcr-Abl inhibitor Preclinical
Onconova Therapeutics (Princeton, New Jersey) ON012380 Small-molecule, substrate-mimetic Bcr-Abl inhibitor Preclinical
Develogen (Goettingen, Germany) Akt inhibitor Small-molecule, substrate-competitive kinase inhibitor Preclinical
Ariad Pharmaceuticals (Cambridge, Massachusetts) AP23846 Small-molecule, ATP-mimetic Src inhibitor Lead optimization

 

 


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