Steroid sulfatase inhibitors

Steroid sulfatase (STS) regulates the local production of oestrogens and androgens from systemic precursors in several tissues. It catalyses the hydrolysis of the sulfate esters of 3-hydroxy steroids, which are inactive transport or precursor forms of the active 3-hydroxy steroids. In recent years, this enzyme has received considerable attention due to its potential involvement in the pathogenesis of a number of diseases. Inhibitors of STS are considered to be potential new therapeutic agents for the treatment of oestrogen- and androgen-dependent disorders. Indications range from cancers of the breast, endometrium and prostate to androgenic alopecia and acne. in addition, STS inhibitors are proposed to have positive effects on cognitive dysfunction. This review summarises the patents on STS inhibitors that have appeared since 1999, putting them in the context of relevant publications. Earlier patents were covered by a previous review by Poirier, Ciobanu and Maltais in this journal.