Molecular Targets in Oncology
Signal transduction systems
Angiogenesis
Cell cycle
Apoptosis
Telomerase
Signal Transduction via EGF Receptor Family
R R
RAS RAF
PI3-K pYK K pY SOS
GRB2
pY |
MEK |
PTEN |
STAT |
AKT |
MAPK
P
Gene transcription
Cell cycle progression
Ki67
proliferation/ maturation
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P P |
myc |
cyclin D1 |
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Cyclin D1 |
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DNA |
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Jun Fos |
p27 |
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Myc |
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chemotherapy/ |
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Tunel |
metastasis |
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VEGF |
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radiotherapy resistance |
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angiogenesis |
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survival/anti-apoptosis |
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Approved EGFR-Targeted Therapies
Trastuzumab (Herceptin): ErbB-2 monoclonal antibody for breast cancer
Cetuximab (Erbitux): EGFR monoclonal antibody for colorectal cancer and HNSCC
Gefitinib (Iressa): EGFR tyrosine kinase inhibitor for non small cell lung cancer
Erlotinib (Tarceva): EGFR tyrosine kinase inhibitor for non small cell lung cancer
Approved Molecular-targeted
Therapies
Receptor tyrosine kinase inhibitor: imatinib
àChronic myeloid leukemia (CML)
àGastrointestinal stromal tumor (GIST)
Approved Molecular-targeted
Therapies
Anti VEGF: bevacizumab
àColorectal cancer
àNon small cell lung cancer
Multi-kinase inhibitors
àSunitinib
GIST after failure to imatinib
Renal cell carcinoma
àSorafinib
Renal cell carcinoma, HCC