Drug intelligence / Profile preview

anastrozole + bevacizumab + fulvestrant

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

This is a combination therapy consisting of three agents—anastrozole, bevacizumab, and fulvestrant—used primarily in the treatment of hormone receptor-positive (HR+) advanced or metastatic breast cancer. - **Anastrozole** is a nonsteroidal aromatase inhibitor that reduces estrogen synthesis by inhibiting the aromatase enzyme, thereby lowering circulating estrogen levels. - **Bevacizumab** is a monoclonal antibody targeting vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis and thus reducing tumor blood supply. - **Fulvestrant** is an estrogen receptor antagonist that binds to and accelerates degradation of the estrogen receptor, blocking estrogen signaling in tumor cells. The rationale for combining these agents lies in their complementary mechanisms: - Anastrozole and fulvestrant both target the hormonal axis but at different points—anastrozole decreases systemic estrogen production while fulvestrant degrades the receptor. - Bevacizumab adds antiangiogenic activity to further suppress tumor growth. Clinical studies have evaluated combinations such as anastrozole plus bevacizumab[7], fulvestrant plus bevacizumab[1], and anastrozole plus fulvestrant[2][6]. These combinations have shown feasibility, tolerability, and some improvement in progression-free survival compared to monotherapy arms. However, there are no large-scale phase III trials specifically evaluating all three drugs together; most data come from dual-combination regimens or sequential use.

02

Targets

ESR1 (ERα)VEGFA (Vascular endothelial growth factor A)CYP19A1 (Aromatase)

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