Table 2.
Tyrosine kinase inhibitors used in clinical trials for treating solid tumours
| Tyrosine kinase inhibitor | Kinase target(s) | FDA-approved indications |
|---|---|---|
| Imatinib (Gleevec/Glivec) | BCR-ABL, c-KIT, PDGFR | CML, Ph + ALL, GIST |
| Dasatinib (Sprycel) | SRC, SFKs, BCR-ABL, c-KIT, PDGFR, c-FMS, EPHA2 | CML (2nd-line), Ph + ALL |
| Gefitinib (Iressa) | EGFR | NSCLC |
| Erlotinib (Tarceva) | EGFR | NSCLC |
| Nilotinib (Tasigna) | BCR-ABL, c-KIT, PDGFR | CML (2nd-line) |
| Lapatinib (Tykerb) | EGFR, HER2/neu | Advanced breast cancer |
| Sunitinib (Sutent) | VEGFR2, PDGFR, c-KIT, FLT3 | GIST, renal cell carcinoma |
| Sorafenib (Nexavar) | VEGFR, PDGFR | Renal cell carcinoma, hepatocellular carcinoma |
EGFR epidermal growth factor receptor, CML chronic myeloid leukaemia, EPHA ephrin A, GIST gastrointestinal stromal tumours, FLT3 FMS-like tyrosine kinase 3, NSCLC non-small cell lung carcinoma, Ph + ALL Philadelphia chromosome–positive acute lymphoblastic leukaemia, PDGFR platelet-derived growth factor receptor, VEGFR2 vascular endothelial growth factor receptor-2.