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targeted therapy

Monday 2 January 2006

Targets

- receptor tyrosine kinases (RTKs )

  • C-kit (KIT)
    • Axitinib , Sunitinib , Sorafenib

- EpCAM : catumaxomab , edrecolomab
- VEGF-A (VEGFA )

- CD20: rituximab , tositumomab , ibritumomab
- CD52: alemtuzumab
- CD33: gemtuzumab

- BCR-ABL fusion protein : imatinib , nilotinib , dasatinib
- ABL1
- SRC (Src): bosutinib
- EGFR
- Janus kinase 2 (JAK2 ): lestaurtinib
- IL-2

  • exotoxin against IL-2 (denileukin diftitox )

- MET

- VEGFR2

  • cabozantinib (XL184 )

Small molecules

- cabozantinib (XL184) (Exelis)

  • tyrosine kinase MET
  • tyrosine kinase VEGFR2

- XL147 (Exelis)

  • phosphoinositide-3 kinase (PI3KCA , PI3 kinase) in the PI3K signaling pathway.

- XL765 (Exelis)

  • PI3K and mTOR , kinasesXL765, which targets PI3K kinase and mTOR kinase in the PI3K signaling pathway

- XL880 (foretinib) (Exelis)

Localization

- targeted therapy in NSCLC

References

- Imai K, Takaoka A. Comparing antibody and small-molecule therapies for cancer. Nat Rev Cancer. 2006 Sep;6(9):714-27. PMID: 16929325

- Hannah AL. Kinases as drug discovery targets in hematologic malignancies. Curr Mol Med. 2005 Nov;5(7):625-42. PMID: 16305489

- Savage DG, Antman KH. Imatinib mesylate—a new oral targeted therapy. N Engl J Med. 2002 Feb 28;346(9):683-93. PMID: 11870247

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