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Table 2 Small molecule ErbB inhibitors in breast cancer: clinical data

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]

  1. HER, human epidermal growth factor receptor; MBC, metastatic breast cancer; MR, minor response; NR, not reported; PR, partial response; SD, stable disease (> 6 months unless otherwise stated).