TABLE 2

Anticancer activity of tyrosine kinase inhibitors


Inhibitor

Tyrosine Kinase Target

IC50 for Kinase Inhibition

Neoplasm(s) Targeted

Clinical Status
nM
Imatinib mesylate (STI 751; Gleevec) BCR-ABL 100a,b CML; GISTs Approved
c-KIT 100a
PDGFR 100a
Gefitinib (Iressa) ErbB1 (EGFR) 33b Lung cancer Approved
Erlotinib (OSI-774; Tarceva) ErbB1 (EGFR) 2c Lung cancer Approved
Lapatinib (GW-572016) ErbB1 10d Breast cancer; other solid tumors Phase II
ErbB2 98d
Canertinib (CI-1033) EGFR (nonselective) 17 ErbB1c Breast cancer Phase I/II
9 ErbB2c
Semaxinib (SU5416) VEGFR-2 1040e AML Phase I/II
c-KIT
FLT-3
Vatalanib (PTK787/ZK222584) VEGFR-1 (Flt-1) 77f Colorectal cancer; prostate and renal cancer Phase I/II
VEGF-2 (FLK-1/KDR) 37f
Sutent (SU11248) VEGFR 10g GIST; renal cancer Phase II/III
PDGFR 10g
c-KIT
FLT-3
Sorafenib (BAY 43-9006) B-Raf 38h Renal cancer; malignant melanoma Phase II/III
VEFGR-2 90h
Leflunomide (SU101)
PDGFR
65i
Prostate cancer
Phase II/III
  • a Lyseng-Williamson and Jarvis (2001); b Tibes et al. (2005); c Thomas and Grandis (2004); d Rusnak et al. (2001); e Fong et al. (1999); f Lin et al. (2002); g Mendel et al. (2003); h Wilhelm et al. (2004); i Shawver et al. (1997).