Drug intelligence / Profile preview

everolimus + exemestane

Development stage
Phase 4
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Everolimus plus exemestane is an oral combination therapy used primarily to treat postmenopausal women with advanced, hormone receptor-positive, HER2-negative breast cancer that has progressed following treatment with nonsteroidal aromatase inhibitors. Everolimus is a selective inhibitor of the mammalian target of rapamycin (mTOR), blocking downstream signaling in the mTOR pathway and thereby inhibiting cancer cell growth and proliferation. Exemestane is a steroidal aromatase inhibitor that reduces estrogen production, further suppressing hormone-driven tumor growth. The combination has been shown to significantly prolong progression-free survival compared to exemestane alone in this patient population[1][3][6]. This regimen was notably studied in the BOLERO-2 trial.

Other names
Eve-ExeExe-EveEVEREXEM
02

Targets

CYP19A1 (Aromatase)Mechanistic target of rapamycin complex 1

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