Drug intelligence / Profile preview

exemestane + tamoxifen (Imperial Chemical Industries)

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

Overview

exemestane + tamoxifen is a combination hormonal therapy regimen evaluated in the neoadjuvant (preoperative) setting for postmenopausal women with newly diagnosed estrogen receptor-positive (ER+) stage II-III breast cancer. Exemestane is an irreversible steroidal aromatase inactivator that reduces systemic estrogen levels by blocking the conversion of androgens to estrogens. Tamoxifen is a selective estrogen receptor modulator (SERM) that competitively inhibits the binding of estradiol to estrogen receptors in breast tissue. This specific combination was investigated by the University of Colorado, Denver, in a Phase II clinical trial (NCT00212004) to identify molecular predictors of hormone responsiveness and resistance, aiming to optimize preoperative treatment strategies for large or locally advanced tumors.

Other names
exemestane and tamoxifenexemestane/tamoxifen
02

Targets

ESR1 (ERα)CYP19A1 (Aromatase)

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