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Journal of Clinical Oncology, Vol 22, No 5 (March 1), 2004: pp. 864-871
© 2004 American Society of Clinical Oncology.
DOI: 10.1200/JCO.2004.05.122

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Activity and Safety of the Antiestrogen EM-800, the Orally Active Precursor of Acolbifene, in Tamoxifen-Resistant Breast Cancer

Fernand Labrie, Pierre Champagne, Claude Labrie, Jean Roy, Jacques Laverdière, Louise Provencher, Martin Potvin, Yvan Drolet, Michael Pollak, Lawrence Panasci, Bernard L'Espérance, Jean Dufresne, Jean Latreille, Jean Robert, Benoît Samson, Jacques Jolivet, Louise Yelle, Lionel Cusan, Pierre Diamond, Bernard Candas

From the Laval University Medical Research Center and Centre Hospitalier Universitaire de Québec; Hôpital du Saint-Sacrement; Hôpital Laval, Québec City; McGill University; Hôpital Sacré-Coeur; Centre Hospitalier Universitaire de Montréal (CHUM); Hôpital Charles-Lemoyne, Montreal; Centre Hospitalier Universitaire de Sherbrooke, Sherbrooke, Québec, Canada

Address reprint requests to Fernand Labrie, MD, Oncology and Molecular Endocrinology Research Center, Laval University Medical Center, 2705 Laurier Blvd, T-3-67, Quebec City, Quebec, G1V 4G2, Canada; E-mail: fernand.labrie{at}crchul.ulaval.ca

PURPOSE: To determine the efficacy and safety of EM-800 (SCH-57050), the precursor of acolbifene, a new, highly potent, orally active, pure antiestrogen in the mammary gland and endometrium, for the treatment of tamoxifen-resistant breast cancer.

PATIENTS AND METHODS: Forty-three post menopausal/ovariectomized women with breast cancer who had received tamoxifen, either for metastatic disease or as adjuvant to surgery for >= 1 year, and had relapsed were treated in a prospective, multicenter, phase II study with EM-800 (20 mg/d [n = 21] or 40 mg/d [n = 22] orally).

RESULTS: Thirty-seven patients had estrogen receptor (ER)-positive tumors (>10 fmol/mg; mean, 146 fmol/mg cytosolic protein), three patients had ER-negative/progesterone receptor-positive tumors, and three patients had undetermined ER status. The objective response rate to EM-800 was 12%, with one complete response and four partial responses. Ten patients (23%) had stable disease for >= 3 months, and 7 patients (16%) had stable disease for >= 6 months. With a median follow-up of 29 months, median duration of response was 8 months (range, 7 to 71+ months). Treatment with EM-800 was well tolerated. No significant adverse events related to the study drug were observed clinically or biochemically.

CONCLUSION: EM-800 produced responses in a significant proportion of patients with tamoxifen-resistant breast cancer, thus showing that this highly potent, selective estrogen receptor modulator, which lacks estrogenic activity in the mammary gland and endometrium, has incomplete cross-resistance with tamoxifen, thus suggesting additional benefits in the treatment of breast cancer.

Authors' disclosures of potential conflicts of interest are found at the end of this article.


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