表一 以靶標開發的藥物進入開發後期或上市者 |
Target |
Agent |
Indication |
Company |
Stage |
Bcr-abl |
Gleevec (small molecule inhibitor) |
Chronic myelogeneous gastrointestinal stromal cell tumor |
Novartis (Basel, Switzerland) |
Approved |
Her-2 (neu) |
Herceptin (monoclonal antibody) |
Breast cancer |
Genentech (San Francisco, CA) |
Approval |
EGFR |
Iressa (small molecule inhibitor) |
Nonsmall cell lung carcinoma (NSCLC) |
AstraZeneca (London) |
Approval |
EGFR |
Erbitux (molecule inhibitor) |
Head and neck cancers |
Imctone (New York) / Bristol Myers Squibb (New York) |
Approval |
EGFR |
Tarceva (small molecule inhibitor) |
NSCLC and pancreatic cancer |
Genentech / OSi (Melville, NY) / Roche (Basel) |
Approval |
VEGF |
Avastin (monoclonal antibody) |
Colorectal cancer |
Genentech |
Approval |
Ras inhibitor |
R11577 (fernesyl transferase inhibitor) |
Lung cancer |
Johnson and Johnson (New Brunswick, NJ) |
Phase III |
mTOR inhibitor |
Rapamune (rapamycin) |
Immunosuppression |
Wyeth (Collegeville, PA) |
Registered |
Protein kinase C (PKC) |
Affinitak (antisense oligonucleotide) |
NSCLC |
Isis Pharmaceuticals (Carlsbad, CA) / Eli Lilly (Indianapolis, IN) |
Phase III |
PKC-B |
Ruboxistaurin (small molecule inhibitor) |
Diabetic retinopathy |
Eli Lilly |
Phase III |
VEGF |
PTK787 / ZK 222584 |
Melastatic cancer |
Novartis / Schering AG (Berlin) |
Phase III |
VEGF |
Neovastat (cartilage extract) |
NSCLC |
Aetema (Quebec City, Quebec) |
Phase III |
EGF |
ABX-EGF (monoclonal antibody) |
Colorectal and NSCLC |
Abgenix (Freemont, CA) |
Phase II |
EGFR |
TheraCIM (monoclonal antibody) |
Head and neck cancer |
YM Biosciences (Mississauga, Ontario) |
Phase II |
Mixed lineages kinases |
CEP 1347 (small molecule inhibitor) |
Parkinson disease |
Cephalon (West Chester, PA) |
Phase II |
Tyrosine kinase |
CEP 701 (small molecule inhibitor) |
Pancreatic cancer |
Cephalon |
Phase II |
Cyclin dependent kinase |
Flavopiridol (small molecule inhibitor) |
Solid tumors |
Aventis |
Phase II |
VEGF |
VEGF Trap (decoy receptor) |
Non-Hodgkin’s lymphoma |
Regeneron (Tarrytown, NY) / Aventis (Bridgewater, NJ) |
Phase I |
VEGF |
Pegaptanib |
Age-related molecular degeneration ( AMD) |
Eyetech phar / Pfizer |
Approved |
VEGF |
Ranbizumab |
AMD |
Genentech / Novartis |
Approved |
資料來源:Nature Review Drug Discovery 2003 及科技政策研究與資訊中心(STPI)本室整理。 |