A randomized phase II presurgical trial of weekly low-dose tamoxifen versus raloxifene versus placebo in premenopausal women with estrogen receptor-positive breast cancer

Davide Serrano, Matteo Lazzeroni, Sara Gandini, Debora Macis, Harriet Johansson, Jennifer Gjerde, Ernst Lien, Irene Feroce, Giancarlo Pruneri, Maria Teresa Sandri, Fabio Bassi, Fabricio Brenelli, Alberto Luini, Massimiliano Cazzaniga, Clara Varricchio, Aliana Guerrieri-Gonzaga, Andrea DeCensi, Bernardo Bonanni

Research output: Contribution to journalArticlepeer-review

Abstract

Introduction: We previously demonstrated that 1 or 5 mg per day of tamoxifen (T) given for four weeks before surgery reduces Ki-67 in breast cancer (BC) patients to the same extent as the standard 20 mg/d. Given the long half-life of T, a weekly dose (10 mg per week (w)) may be worth testing. Also, raloxifene (R) has shown Ki-67 reduction in postmenopausal patients in a preoperative setting, but data in premenopausal women are limited. We conducted a randomized trial testing T 10 mg/w vs. R 60 mg/d vs. placebo in a presurgical model.Methods: Out of 204 screened subjects, 57 were not eligible, 22 refused to participate and 125 were included in the study. The participants were all premenopausal women with estrogen receptor-positive BC. They were randomly assigned to either T 10mg/w or R 60 mg/d or placebo for six weeks before surgery. The primary endpoint was tissue change of Ki-67. Secondary endpoints were modulation of estrogen and progesterone receptors and several other circulating biomarkers.Results: Ki-67 was not significantly modulated by either treatment. In contrast, both selective estrogen receptor modulators (SERMs) significantly modulated circulating IGF-I/IGFBP-3 ratio, cholesterol, fibrinogen and antithrombin III. Estradiol was increased with both SERMs. Within the tamoxifen arm, CYP2D6 polymorphism analysis showed a higher concentration of N-desTamoxifen, one of the tamoxifen metabolites, in subjects with reduced CYP2D6 activity. Moreover, a reduction of Ki-67 and a marked increase of sex hormone-binding globulin (SHBG) were observed in the active phenotype.Conclusions: A weekly dose of tamoxifen and a standard dose of raloxifene did not inhibit tumor cell proliferation, measured as Ki-67 expression, in premenopausal BC patients. However, in the tamoxifen arm women with an extensive phenotype for CYP2D6 reached a significant Ki-67 modulation.

Original languageEnglish
Article numberR47
JournalBreast Cancer Research
Volume15
Issue number3
DOIs
Publication statusPublished - Jun 20 2013

Keywords

  • breast cancer
  • prevention
  • raloxifene
  • tamoxifen

ASJC Scopus subject areas

  • Cancer Research
  • Oncology
  • Medicine(all)

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