Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer

Authors: Palmieri, Carlo; Januszewski, Adam; Stanway, Susie; Coombes, R. Charles

Source: Expert Review of Anticancer Therapy, 1 February 2011, vol. 11, no. 2, pp. 179-183(5)


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Endocrine therapy is a key modality in the management of breast cancer, with current options for postmenopausal women including tamoxifen, aromatase inhibitors and fulvestrant. Unfortunately, in spite of these advances, many women still relapse or progress on endocrine therapy. Given that resistance (de novo or acquired resistance) is a major limiting factor in the use of endocrine therapy, additional endocrine therapies with novel methods of action are required. Steroid sulfatase, which is responsible for the conversion of estrone sulfate to estrone, as well as dehydroepiandrosterone sulfate to dehydroepiandrosterone, has been implicated in endocrine resistance. In this article, we summarize the preclinical and clinical data to support the potential role of steroid sulfatase in breast cancer, as well as the current data on the first available steroid sulfatase inhibitor named irosustat (STX64; 667 Coumate; BN83495), and discuss its potential clinical development.

Keywords: breast cancer; endocrine therapy; inhibition; irosustat; steroid sulfatase

Document Type: Research Article


Affiliations: 1Cancer Research UK Laboratories, Division of Cancer, Imperial College, Du Cane Road, London, W12 0NN, UK

Publication date: February 1, 2011

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