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aminoglutethimide + danazol + hydrocortisone + tamoxifen

Development stage
Preclinical
Lead developer
Winthrop Company
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of four drugs used primarily in the treatment of advanced breast cancer, especially in postmenopausal women. The regimen is not available as a single branded product but is sometimes used together in clinical practice or research settings. - **Aminoglutethimide**: An aromatase inhibitor that blocks the conversion of androgens to estrogens by inhibiting the enzyme aromatase, thereby reducing estrogen levels[5][6]. - **Danazol**: A synthetic steroid with weak androgenic activity; its mechanism in breast cancer is not fully understood but may involve suppression of ovarian function or other hormonal effects[6]. - **Hydrocortisone**: A glucocorticoid used to replace adrenal steroids suppressed by aminoglutethimide, preventing adrenal insufficiency[5][8]. - **Tamoxifen**: A selective estrogen receptor modulator (SERM) that competitively binds to estrogen receptors, blocking estrogen’s proliferative effects on breast tissue[8]. The combination has been studied for its potential synergistic effects on hormone-sensitive tumors. However, some studies suggest that danazol may antagonize the suppressive effect of aminoglutethimide on biologically active estradiol levels, potentially reducing efficacy when combined[6][8].

Other names
AG + danazol + hydrocortisone + tamoxifenaminoglutethimide/danazol/hydrocortisone/tamoxifen
02

Targets

CNR1 (Cannabinoid receptor 1)CYP11B1 (Cytochrome P450 11B1)ESR1 (ERα)GR (Glucocorticoid receptor)CYP19A1 (Aromatase)ESR2 (ERβ)CYP11A1 (Cholesterol side chain cleavage enzyme)PR (Progesterone receptor)AR (Adrenergic receptors)

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