Drug intelligence / Profile preview

anastrozole + everolimus + fulvestrant

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Anastrozole + everolimus + fulvestrant is a combination regimen of three drugs used in the treatment of advanced or metastatic hormone receptor (HR)-positive, HER2-negative breast cancer, particularly in postmenopausal women. - **Anastrozole** is a nonsteroidal aromatase inhibitor that reduces estrogen production by inhibiting the aromatase enzyme, thereby decreasing tumor growth driven by estrogen. - **Everolimus** is an mTOR (mechanistic target of rapamycin) inhibitor that blocks a key signaling pathway involved in cell proliferation and survival, providing targeted antineoplastic activity. - **Fulvestrant** is a selective estrogen receptor degrader (SERD) that binds to and accelerates degradation of the estrogen receptor, leading to downregulation of ER-mediated signaling. This triple combination was evaluated as first-line therapy for advanced HR-positive, HER2-negative breast cancer in postmenopausal women who had not received prior systemic therapy for metastatic disease. The rationale was to combine endocrine therapies with targeted inhibition of mTOR to overcome resistance mechanisms and improve outcomes. However, clinical trial data did not show significant improvement in progression-free or overall survival compared with fulvestrant alone[1][2][9].

02

Targets

ESR1 (ERα)ESR2 (ERβ)Mechanistic target of rapamycin complex 1CYP19A1 (Aromatase)

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