Gefitinib or placebo in combination with tamoxifen in patients with hormone receptor-positive metastatic breast cancer: a randomized phase II study

Clin Cancer Res. 2011 Mar 1;17(5):1147-59. doi: 10.1158/1078-0432.CCR-10-1869. Epub 2011 Jan 10.

Abstract

Purpose: Increased growth factor signaling may contribute to tamoxifen resistance. This randomized phase II trial assessed tamoxifen plus placebo or the epidermal growth factor receptor inhibitor gefitinib in estrogen receptor (ER)-positive metastatic breast cancer.

Experimental design: Patients with newly metastatic disease or recurred after adjuvant tamoxifen (stratum 1), or recurred during/after adjuvant aromatase inhibitor (AI) or after failed first-line AI (stratum 2), were eligible. Primary variables were progression-free survival (PFS; stratum 1) and clinical benefit rate (CBR; stratum 2). A 5% or more improvement in response variables with gefitinib was considered to warrant further investigation. Outcome was correlated with biomarkers measured on the primary tumor.

Results: In stratum 1 (n = 206), the PFS HR (gefitinib:placebo) was 0.84 (95% CI, 0.59-1.18; median PFS 10.9 versus 8.8 months). In the stratum 1 endocrine therapy-naïve subset (n = 158) the HR was 0.78 (95% CI, 0.52-1.15), and the prior endocrine-treated subgroup (n = 48) 1.47 (95% CI, 0.63-3.45). In stratum 1, CBRs were 50.5% with gefitinib and 45.5% with placebo. In stratum 2 (n = 84), CBRs were 29.2% with gefitinib and 31.4% with placebo. Biomarker analysis suggested that in stratum 1 there was greater benefit with gefitinib in patients who were ER-negative or had lower levels of ER protein.

Conclusions: In stratum 1, the improved PFS with gefitinib plus tamoxifen met the protocol criteria to warrant further investigation of this strategy. In stratum 2, there was a numerical disadvantage for gefitinib; additional investigation after AI therapy is not warranted. Studies of predictive biomarkers are needed to subset appropriate patients.

Publication types

  • Clinical Trial, Phase II
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents, Hormonal / administration & dosage
  • Antineoplastic Agents, Hormonal / adverse effects
  • Antineoplastic Agents, Hormonal / therapeutic use
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Biomarkers, Tumor
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Drug-Related Side Effects and Adverse Reactions
  • ErbB Receptors / antagonists & inhibitors
  • Female
  • Gefitinib
  • Humans
  • Middle Aged
  • Neoplasms, Hormone-Dependent / drug therapy*
  • Placebos
  • Quinazolines / administration & dosage*
  • Quinazolines / adverse effects
  • Quinazolines / pharmacokinetics
  • Receptor, ErbB-2 / analysis
  • Receptors, Estrogen / antagonists & inhibitors
  • Signal Transduction / drug effects
  • Tamoxifen / administration & dosage*
  • Tamoxifen / adverse effects
  • Tamoxifen / pharmacokinetics
  • Treatment Outcome

Substances

  • Antineoplastic Agents, Hormonal
  • Biomarkers, Tumor
  • Placebos
  • Quinazolines
  • Receptors, Estrogen
  • Tamoxifen
  • ERBB2 protein, human
  • ErbB Receptors
  • Receptor, ErbB-2
  • Gefitinib