Drug intelligence / Profile preview

aromatase inhibitors + tamoxifen

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

Overview

Aromatase inhibitors + tamoxifen refers to the sequential or combined use of two classes of hormonal therapies for the treatment of hormone receptor-positive breast cancer, primarily in postmenopausal women. Aromatase inhibitors (such as anastrozole, letrozole, and exemestane) work by inhibiting the enzyme aromatase, thereby reducing estrogen production and depriving estrogen receptor-positive tumor cells of their growth stimulus. Tamoxifen is a selective estrogen receptor modulator (SERM) that blocks estrogen receptors on breast cancer cells, preventing estrogen from binding and stimulating tumor growth. This combination or sequence is used as adjuvant therapy to lower recurrence risk and improve disease-free survival in early-stage breast cancer. The approach may involve several years of tamoxifen followed by an aromatase inhibitor or vice versa; however, concurrent administration is not standard due to lack of added benefit over monotherapy[1][3][4]. Each drug has a distinct side effect profile—aromatase inhibitors are more associated with joint pain and bone loss/fractures, while tamoxifen carries higher risks for endometrial cancer and thromboembolic events[1][8][10].

02

Targets

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

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