Aminoglutethimide
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for advanced breast and prostate cancer in the 1970s and 1980s, the ancestor of today's aromatase inhibitors, and was withdrawn once selective drugs arrived.
Overview
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.
Inhibits CYP11A1, the first step of steroid synthesis from cholesterol, and aromatase, so adrenal steroids and oestrogens both fall; cortisol replacement is needed. Connects to Aromatase (CYP19A1) and CYP11A1 (cholesterol side-chain cleavage enzyme).
1.Aminoglutethimide slips into a pocket on Aromatase (CYP19A1).
Approvals
| Region | Year | Indication |
|---|---|---|
| US | 1980 | Cushing's syndrome (used off label as medical adrenalectomy in breast and prostate cancer) |
Trials
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Latest papers
topQuery for this drug: (TITLE:"Aminoglutethimide" OR ABSTRACT:"Aminoglutethimide" OR TITLE:"Cytadren" OR ABSTRACT:"Cytadren" OR TITLE:"Orimeten" OR ABSTRACT:"Orimeten") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Aminoglutethimide, not a curated reading list.
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