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 (PI3K, 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)

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