Home > D. Systemic pathology > Toxics and drugs > Therapeutics > Targeted therapy > targeted therapy

targeted therapy

Monday 2 January 2006

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

Portfolio