From: New targets for therapy in breast cancer: Small molecule tyrosine kinase inhibitors
Agent | Phase of development in breast cancer | Adverse affects | Clinical activity in breast cancer |
---|---|---|---|
Gefitinib | Phase II | Rash, diarrhea, nausea, vomiting, elevated transaminases; 0.3–2% risk for interstitial lung disease [18] | 1 PR, 2 SD in 63 patients [19] |
 |  |  | 2 PR, 3 SD in 19 patients [20] |
 |  |  | 1 MR, 3 SD in 31 patients [21] |
Erlotinib | Phase II: MBC | Rash, diarrhea, nausea, fatigue, headache, elevated transaminases | 1 PR, 3 SD (12 weeks, 16 weeks, and > 28 weeks) in 47 patients [22] |
 |  |  | 0 PR in 18 patients [23] |
EKB-569 | Phase I: advanced solid tumors | Diarrhea, rash, nausea, vomiting, stomatitis, anorexia [24] | NR |
TAK-165 | Phase I: HER2-positive MBC | NR | NR |
GW572016 | Phase II: MBC, either HER2-positive or -negative | Diarrhea, nausea, fatigue, rash, headache, elevation of transaminases | 4 PR in trastuzumab-refractory disease [25] |
 |  |  | 3 PR, 5 SD (12–36+ weeks) in 44 patients with trastuzumab-refractory disease [27] |
PKI-166 | Phase I: advanced cancer completed | Nausea, vomiting, diarrhea, fatigue, myalgia, rash, elevation of transaminases [26] | NR |
 | No longer under clinical development |  |  |
AEE-788 | Phase I: advanced solid tumors | NR | NR |
CI-1033 | Phase II: MBC | Nausea, vomiting, asthenia, diarrhea, rash, mucositis, hypersensitivity, thrombocytopenia | No objective responses reported to date in phase I trials, but 1 SD [16] |