Table 1

Targeted therapies in clinical development

Target
Agent
Agent class

EGFR
IMC-C225 Cetuximab, Erbitux (Imclone)
Monoclonal antibody

ABX-EGF (Abgenix)
Monoclonal antibody

EMD 72000 (Merck KgaA Darmstadt)
Monoclonal antibody

ZD 1839 gefitinib, Iressa (AstraZeneca)
Small molecule kinase inhibitor

OSI-774, erlotinib, Tarceva(OSI-Pharmaceuticals)
Small molecule kinase inhibitor

CI-1033/PD183805 (Pfizer)
Small molecule kinase inhibitor

EKB-569 (Wyeth Ayerst)
Small molecule kinase inhibitor

GW2016/572016(GlaxoSmithKline)
Small molecule kinase inhibitor
HER2/neu
Trastuzumab, Herceptin(Genentech)
Monoclonal antibody

2C4 (Genentech)
Monoclonal antibody

17-AAG
Geldanamycin derivative inhibits HSP90

TAK-165(Takeda Pharmaceuticals)
Small molecule inhibitor

GW2016/572016(GlaxoSmithKline)
Small molecule kinase inhibitor

CP 724, 714 (Pfizer)
Small molecule inhibitor
Ras
R115777(Johnson and Johnson)
Farnesyl transferase inhibitor

SCH66336 (Schering-Plough)
Farnesyl transferase inhibitor

BMS214662(Bristol Myers Squibb)
Farnesyl transferase inhibitor

CT-2584HMS (Cell Therapeutics)
Farnesyl transferase inhibitor
Raf
BAY 43-9006 (Onyx/Bayer)
Small molecule kinase inhibitor
MEK
PD 184352/CI-1040 (Pfizer)
Small molecule kinase inhibitor
PKC-α
ISIS 3521/LY900003 Affinitak(ISIS Pharmaceuticals)
Antisense oligonucleotide

CGP41251/PKC412 (Novartis)
Staurosporine analogue

Bryostatin-1
Small molecule kinase inhibitor

UCN-01 (Kyowa Hakko Kogyo)
Staurosporine analogue
PKC-β
LY333531 (Eli Lilly)
Small molecule kinase inhibitor
Akt
17-AAG
Inhibitor of HSP90

Perifosine (Zenataris)
Alkylphospholipid
mTOR
CCI-779 (Wyeth)
Inhibits mTOR kinase by binding to FKBP

RAD001 (Novartis)
Inhibits mTOR kinase by binding to FKBP

EGFR, epidermal growth factor receptor; MEK, MAP kinase/ERK kinase; mTOR, mammalian target of rapamycin; PKC, protein kinase C.

de Bono et al. Breast Cancer Res 2003 5:154   doi:10.1186/bcr597