Drug intelligence / Profile preview

ovarian function suppression + exemestane

Development stage
Unknown
Lead developer
Pfizer
Modality
Peptides, Small Molecules
Administration
Oral, Subcutaneous, Intramuscular
01

Overview

OFS + exemestane is a combination adjuvant endocrine therapy regimen used for the treatment of premenopausal women with hormone receptor-positive (HR+) breast cancer. The regimen consists of ovarian function suppression (OFS)—achieved through gonadotropin-releasing hormone (GnRH) agonists (such as goserelin or leuprorelin), surgical oophorectomy, or ovarian irradiation—paired with exemestane, an oral, steroidal, irreversible aromatase inhibitor. Exemestane works by binding to and inhibiting the aromatase enzyme (CYP19A1), which prevents the conversion of androgens into estrogens in peripheral tissues. In premenopausal women, OFS is necessary when using aromatase inhibitors because these drugs do not effectively inhibit estrogen production from functional ovaries. This combination has been evaluated in major clinical trials such as SOFT (Suppression of Ovarian Function Trial) and TEXT (Tamoxifen and Exemestane Trial), and specifically in the SEAT trial (NCT02440230) to evaluate safety in Chinese populations.

Other names
OFS + exemestaneOFS plus exemestaneovarian function suppression combined with exemestane
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)CYP19A1 (Aromatase)

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