# Aminoglutethimide

Source: https://onco.cc/drugs/aminoglutethimide/  
OnCo record `aminoglutethimide` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Aminoglutethimide produced a medical adrenalectomy for advanced breast and prostate cancer in the 1970s and 1980s, the ancestor of today's aromatase inhibitors, and was withdrawn once selective drugs arrived.

## Summary

Originally an anticonvulsant, aminoglutethimide was found to block adrenal steroid synthesis and was approved in the United States in 1980 for Cushing's syndrome. Oncologists used it with hydrocortisone as a medical adrenalectomy in postmenopausal women with advanced breast cancer and in men with prostate cancer, with response rates similar to surgical adrenalectomy. Drowsiness, rash and the need for steroid replacement limited it, and the selective aromatase inhibitors anastrozole, letrozole and exemestane replaced it in the 1990s. It has been discontinued in most markets.

## Fields

- Kind: Treatment
- Status: historic
- Last checked: 2026-09-08
- Also known as: Orimeten
- Tags: gap-fill; chembl-universe
- Brand: Cytadren
- Modality: Oral steroidogenesis inhibitor
- Mechanism: Inhibits CYP11A1, the first step of steroid synthesis from cholesterol, and aromatase, so adrenal steroids and oestrogens both fall; cortisol replacement is needed.
- Approvals: US 1980: Cushing's syndrome (used off label as medical adrenalectomy in breast and prostate cancer)

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Aminoglutethimide
- Wikipedia: https://en.wikipedia.org/wiki/Aminoglutethimide
- ChEMBL CHEMBL1200538: https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200538

## Connected records

- cancers: [HR-positive / HER2-negative breast cancer](https://onco.cc/cancers/breast-hr-positive/), [Prostate cancer](https://onco.cc/cancers/prostate/)
- technologies: [Endocrine therapy (SERMs, AIs, SERDs)](https://onco.cc/technologies/endocrine-therapy/)
- targets: [Aromatase (CYP19A1)](https://onco.cc/targets/aromatase/), [CYP11A1 (cholesterol side-chain cleavage enzyme)](https://onco.cc/targets/cyp11a1/)
- drugs: [Exemestane](https://onco.cc/drugs/exemestane/), [Letrozole (and other aromatase inhibitors)](https://onco.cc/drugs/letrozole/)

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JSON: https://onco.cc/api/v1/entities/aminoglutethimide.json