Drug intelligence / Profile preview

anastrozole + exemestane + letrozole

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

Overview

This is a combination of three aromatase inhibitors—anastrozole, exemestane, and letrozole. All three are small molecule drugs used as hormone therapy for the treatment of hormone receptor-positive breast cancer, primarily in postmenopausal women. Aromatase inhibitors work by blocking the enzyme aromatase, which converts androgens to estrogens in peripheral tissues. By lowering estrogen levels, these drugs reduce the growth stimulus for estrogen-dependent breast cancer cells. Anastrozole and letrozole are non-steroidal aromatase inhibitors, while exemestane is a steroidal (irreversible) inhibitor[1][8][9]. These agents are typically used individually rather than in combination; there is no evidence or clinical precedent for using all three simultaneously as a single regimen.

Brand names
ArimidexFemaraAromasin
Other names
Third-generation aromatase inhibitorsAIs
02

Targets

CYP19A1 (Aromatase)

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