Drug intelligence / Profile preview

aminoglutethimide + hydrocortisone + tamoxifen

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

Overview

Aminoglutethimide + hydrocortisone + tamoxifen is a combination regimen of three small molecule drugs used in the treatment of advanced or metastatic breast cancer, particularly in postmenopausal women. Tamoxifen is a selective estrogen receptor modulator (SERM) that competitively inhibits estrogen binding to its receptor on breast cancer cells, thereby blocking tumor growth driven by estrogen signaling. Aminoglutethimide is an aromatase inhibitor that suppresses adrenal steroid synthesis and reduces peripheral conversion of androgens to estrogens. Hydrocortisone is administered alongside aminoglutethimide to replace glucocorticoids suppressed by aminoglutethimide’s inhibition of adrenal steroidogenesis. The combination was investigated as an endocrine therapy for hormone-responsive breast cancer but did not show significant improvement over tamoxifen alone and was associated with increased toxicity[1][2][3].

Other names
T+AG+HTAM+AG+HCtamoxifen + aminoglutethimide + hydrocortisone
02

Targets

ER (Estrogen receptor)GR (Glucocorticoid receptor)CYP19A1 (Aromatase)

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