| |
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|
| 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 |
