Drug intelligence / Profile preview

aminoglutethimide + cortisone acetate

Development stage
Unknown
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Aminoglutethimide + cortisone acetate is a combination therapy used primarily in the management of hormone-dependent cancers such as metastatic prostate cancer and breast cancer, as well as for suppression of adrenal function in conditions like Cushing's syndrome. Aminoglutethimide acts as a steroidogenesis inhibitor by blocking the enzymatic conversion of cholesterol to pregnenolone, thereby reducing the synthesis of adrenal glucocorticoids, mineralocorticoids, estrogens, and andro gens. This inhibition can lead to increased secretion of adrenocorticotropic hormone (ACTH), which is counteracted by co-administration with a glucocorticoid such as cortisone acetate. Cortisone acetate serves both to replace deficient corticosteroids due to aminoglutethimide-induced suppression and to prevent ACTH-driven escape from steroid blockade. The combination has been shown to provide symptomatic relief (e.g., bone pain) in patients with advanced prostate cancer who have failed other endocrine therapies[1][8][10].

02

Targets

MR (Mineralocorticoid receptor)CYP11A1 (Cholesterol side chain cleavage enzyme)GR (Glucocorticoid receptor)CYP19A1 (Aromatase)

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