targeted therapy

Targets

 receptor tyrosine kinases (RTKs )

• ERBB1 (ErbB: HER1/EGF):
  • cetuximab , panitumumab
  • erlotinib , gefitinib , lapatinib , vandetanib , neratinib

• ERBB2 (HER2 /neu)
  • trastuzumab
  • apatinib , neratinib

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

• FLT3 : lestaurtinib
• PDGFR : axitinib , sunitinib , sorafenib
• VEGFR : vandetanib, semaxanib, cediranib, axitinib, sunitinib, sorafenib

 EpCAM : catumaxomab , edrecolomab
 VEGF-A (VEGFA )

• bevacizumab (Avastil)
• fusion protein against VEGF: aflibercept

 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

• cabozantinib (XL184 )

 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