2015 Antineoplastics

TYROSINE KINASES and their INHIBITORS
CETUXIMAB, DASATINIB, ERLOTINIB, GEFITINIB, IMATINIB, LAPATANIB, NALOTINIB, PANITUMUMAB, SORAFENIB, SUNITINIB, TRASTUZUMAB

Signal transduction inhibitors (STIs) like IMATINIB, ERLOTINIB and GEFITINIB bind to the ATP-binding site of tyrosine kinases (NOT the substrate binding site).  STIs generally have fewer side effects than conventional therapies because they are targeted toward the specific defect of a particular cancer:  IMATINIB to bcr‑abl in CML, and ERLOTINIB and GEFITINIB to EGFR which is overexpressed in many epithelial-derived cancers.

Critical facts icon
CANCER TYPE TYROSINE KINASE DRUG
Chronic myeloid leukemia (CML) Bcr-abl

BOSUTINIB
DASATANIB
IMATINIB
NILOTINIB

GIST c-kit

DASATANIB
IMATINIB
NILOTINIB
SUNITINIB

Breast cancer HER2

PERTUZUMAB
TRASTUZUMAB

Epithelial derived
(e.g., lung, pancreas, head and neck, breast, prostate, colon, stomach, ovaries and brain)
EGFR CETUXIMAB
ERLOTINIB
GEFITINIB
PANITUMUMAB
Many
(including glioblastoma, hepatocellular carcinoma)
PDGF-R,
VEGF-R

(discussed under angiogenesis inhibitors)
PAZOPANIB
SORAFENIB SUNITINIB
Email: Dr. Janet Fitzakerley | ©2015 University of Minnesota Medical School Duluth | Last modified: 11-apr-15 9:39 AM