Drug intelligence / Profile preview

aminoglutethimide + medroxyprogesterone acetate

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

Overview

Aminoglutethimide + medroxyprogesterone acetate is a combination therapy used primarily in the treatment of advanced or metastatic breast cancer. Aminoglutethimide is an aromatase inhibitor and steroidogenesis inhibitor that blocks the conversion of cholesterol to pregnenolone, thereby reducing adrenal glucocorticoids, mineralocorticoids, estrogens, and androgens. Medroxyprogesterone acetate is a synthetic progestin with agonist activity at progesterone, androgen, and glucocorticoid receptors. The combination exploits dual mechanisms—aminoglutethimide suppresses estrogen synthesis (critical for hormone-dependent breast cancers), while medroxyprogesterone acetate provides progestogenic effects that can further inhibit tumor growth and may substitute for corticosteroid replacement during aminoglutethimide therapy. This regimen has been studied in phase II trials for advanced breast cancer patients who are postmenopausal or have hormone-dependent tumors[1][2][4].

02

Targets

PR (Progesterone receptor)CYP19A1 (Aromatase)GR (Glucocorticoid receptor)AR (Adrenergic receptors)

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