Steroid sulfatase catalyses the hydrolysis of sulfated steroids to their co
rresponding hydroxylated forms. Since oestrogens and androgens can be synth
esised intracellularly from the abundant circulating sulfated steroids, ste
roid sulfatase inhibitors should prove to be valuable therapeutic agents fo
r the treatment of hormone-dependent diseases. Furthermore, steroid sulfata
se inhibitors have been reported to control brain concentrations of sulfate
d neurosteroids and also to improve memory. Such therapeutic potential stim
ulated research and development of steroid sulfatase inhibitors and importa
nt progress has been achieved during the last ten years. This review focuse
s on patented steroid sulfatase inhibitors, but discussion of unpatented in
hibitors published in the literature has been included to complement the in
formation presented.