Drug intelligence / Profile preview

exemestane

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Exemestane is an oral, steroidal aromatase inhibitor used primarily to treat hormone-sensitive breast cancer in postmenopausal women. It works by irreversibly binding to and inactivating the aromatase enzyme, which is responsible for converting androgens into estrogens in peripheral tissues. By blocking this conversion, exemestane significantly lowers estrogen levels, thereby slowing or stopping the growth of estrogen-dependent breast tumors. Exemestane is indicated for early and advanced breast cancer in postmenopausal women who have previously been treated with tamoxifen or whose disease has progressed during such therapy. The drug was developed as a "suicide inhibitor," meaning it permanently deactivates its target enzyme through irreversible binding.

Brand names
Aromasin
Other names
exemestane
02

Targets

CYP19A1 (Aromatase)

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