Drug intelligence / Profile preview

tamoxifen + aminoglutethimide

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

Overview

Tamoxifen + aminoglutethimide is a combination of two oral endocrine therapies used in the management of advanced breast cancer, particularly in postmenopausal women. Tamoxifen is a selective estrogen receptor modulator (SERM) that competitively inhibits estrogen binding to its receptor, thereby blocking the proliferative action of estrogen on breast cancer cells. Aminoglutethimide is an aromatase inhibitor that suppresses adrenal steroid synthesis, leading to reduced production of estrogens and other steroids. The rationale for combining these agents was based on their different mechanisms of action targeting estrogen pathways; however, clinical studies have shown that the combination does not provide significant benefit over either agent alone and may increase toxicity[1][2][3][5]. This regimen has been studied with or without hydrocortisone supplementation.

02

Targets

ESR2 (ERβ)ESR1 (ERα)Adrenal steroidogenic cytochrome P450 enzymesCYP19A1 (Aromatase)

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