TABLE 1

Representative mutations in cancer cells and inhibition by small molecule tyrosine kinase inhibitors


Target

Mutation

Tumor Type(s)

Tyrosine Kinase Inhibitor
BCR-ABL tyrosine kinase BCR-ABL a CML; ALL Imatinib (STI 751; Gleevec)
c-KIT tyrosine kinase; PDGFR kinase c-KITb GISTs Imatinib (STI 751; Gleevec)
EGFR tyrosine kinase EGFR tyrosine kinase domainc Nonsmall cell lung cancer Gefitinib (Iressa); Erlotinib (OSI-774; Tarceva)
FLT-3 kinase FLT-3-ITD or FLT-3D835d AML Sutent (SU11248)
B-Raf kinase
B-Raf V599E e
Solid tumors (melanoma, renal carcinoma)
Sorafenib (BAY 43-9006)
  • a Druker (2004); b Savage and Antman (2002); c Pao and Miller (2005); d Gilliland and Griffin (2002); e Sharma et al. (2005).