irosustat

Irosustat is a first-generation, orally active, irreversible and nonsteroidal inhibitor of steroid sulfatase (STS), belonging to the aryl sulfamate ester class of drugs. It was developed for the treatment of hormone-sensitive cancers such as breast cancer, endometrial cancer, and prostate cancer. By inhibiting STS—a cytoplasmic enzyme responsible for converting inactive steroid sulfates (like estrone sulfate and DHEA sulfate) into their biologically active forms—irosustat reduces local estrogen production in tumors. This mechanism aims to inhibit estrogen-dependent cell growth in hormone-sensitive malignancies. Irosustat was originally designed at the University of Bath and Imperial College London; its development was led by Sterix Ltd (later acquired by Ipsen). The drug reached phase II clinical trials in breast and endometrial cancers but has since been discontinued for all indications[1][2][3][4][5].

Brand names

Oristusane

Other names

irosustat6-Oxo-8,9,10,11-tetrahydro-7H-cyclohepta[c][1]benzopyran-3-O-sulfamate