Drug intelligence / Profile preview

aromatase inhibitors + irosustat

Development stage
Unknown
Lead developer
Ipsen
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of an aromatase inhibitor (AI) and irosustat. Aromatase inhibitors are a class of drugs that block the enzyme aromatase, thereby reducing estrogen production, and are commonly used in the treatment of hormone receptor-positive breast cancer. Irosustat is an orally active, irreversible steroid sulfatase (STS) inhibitor that prevents the conversion of inactive steroid sulfates into active estrogens and androgens. The rationale for combining these agents is to achieve more complete suppression of estrogen biosynthesis by inhibiting both major pathways—aromatization and sulfatase-mediated activation—in postmenopausal women with advanced or metastatic ER-positive breast cancer who have progressed on first-line AI therapy. Clinical studies have shown this combination can provide clinical benefit with an acceptable safety profile[1][2][3][4].

02

Targets

STS (Steroid sulfatase)CA2 (Carbonic Anhydrase 2)

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