2015 Antineoplastics

DRUGS THAT TARGET ALTERED PROTEIN FUNCTION

Critical Fact Icon
A significant spectrum of action exists among protein function inhibitors. At one end are drugs that target a unique aspect of a specific cancer type (such as L-ASPARAGINASE and IMATINIB); less specific are those that block growth factors or their receptors (such as ERLOTINIB and GEFITINIB); and at the other end are drugs that are really targeting rapidly dividing cells and/or angiogenesis (like BORTEZOMIB, VORINOSTAT, SORAFENIB and SUNITINIB).

Targets

I. Tyrosine kinases:

  • Bcr-Abl: BOSUTINIB, DASATINIB, IMATINIB, NILOTINIB
  • EGFR: CETUXIMAB, ERLOTINIB, GEFITINIB, PANITUMUMAB
  • HER2: PERTUZUMAB, TRASTUZUMAB [ADO-TRASTUZUMAB EMTANSINE]
  • PDGF-R, VEGF-R:  PAZOPANIB, SORAFENIB, SUNITINIB (discussed under angiogenesis inhibitors)

II. Altered intracellular processes

  • Deplete asparagine: L-ASPARAGINASE
  • Proteosome: BORTEZOMIB, CARFILZOMIB
  • HDAC: ROMIDEPSIN, VORINOSTAT
  • Promyelocytic protein: ARSENIC TRIOXIDE (ATO), BEXAROTENE, TRETINOIN (discussed under differentiating agents)

N.B. The signal transduction inhibitors that target Bcr-Abl and EGFR will be presented in lecture V not lecture IV, but on this website they are kept in this mechanistic class

  • in other words, the "lecture" series and this website will handle these drugs a little bit differently
Email: Dr. Janet Fitzakerley | ©2015 University of Minnesota Medical School Duluth | Last modified: 10-may-15 9:08 PM