Drug intelligence / Profile preview

Anastrozole + fulvestrant

Development stage
Phase 3
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intramuscular, Oral
01

Overview

Anastrozole + fulvestrant is a combination therapy used primarily in the treatment of hormone receptor-positive (HR+), HER2-negative metastatic breast cancer in postmenopausal women. Anastrozole is a nonsteroidal aromatase inhibitor that works by inhibiting the enzyme aromatase, thereby reducing estrogen synthesis and lowering circulating estrogen levels. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to the estrogen receptor, blocks its activity, and accelerates its degradation, leading to complete inhibition of estrogen signaling through the receptor. The combination targets two distinct mechanisms within the estrogen pathway—anastrozole reduces available estrogen while fulvestrant eliminates functional receptors—providing a synergistic approach for patients whose cancers are driven by hormonal signaling[1][5][6][8]. This regimen has been shown to improve overall survival compared to monotherapy with either agent alone in certain patient populations[3].

Other names
aromatase inhibitor + fulvestrant
02

Targets

CYP19A1 (Aromatase)ESR1 (ERα)ESR2 (ERβ)

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