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Metopirone (METYRAPONE)
Metopirone works by inhibiting the enzyme responsible for converting a precursor into cortisol, effectively reducing cortisol production.
Metopirone (Metyrapone) is a small molecule adrenal steroid synthesis inhibitor developed by HRA Pharma and currently owned by Esteve. It targets the cytochrome P450 11B1 enzyme in the mitochondria, which is involved in cortisol production. Metopirone is FDA-approved for diagnostic testing of secondary adrenocortical insufficiency since 1961. As an off-patent medication, it is not commercially available as a generic. Metopirone's commercial status and safety considerations require careful evaluation.
At a glance
| Generic name | METYRAPONE |
|---|---|
| Sponsor | Esteve |
| Drug class | Adrenal Steroid Synthesis Inhibitor [EPC] |
| Target | Cytochrome P450 11B1, mitochondrial |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 1961 |
Mechanism of action
The pharmacological effect of Metopirone is to reduce cortisol and corticosterone production by inhibiting the 11-beta-hydroxylation reaction in the adrenal cortex. Removal of the strong inhibitory feedback mechanism exerted by cortisol results in an increase in adrenocorticotropic hormone (ACTH) production by the pituitary. With continued blockade of the enzymatic steps leading to production of cortisol and corticosterone, there is marked increase in adrenocortical secretion of their immediate precursors, 11-desoxycortisol and desoxycorticosterone, which are weak suppressors of ACTH release, and corresponding elevation of these steroids in the plasma and of their metabolites in the urine. These metabolites are readily determined by measuring urinary 17-hydroxycorticosteroids (17-OHCS) or 17-ketogenic steroids (17-KGS). Because of these actions, Metopirone is used as diagnostic test, with urinary 17-OHCS measured as an index of pituitary ACTH responsiveness. Me
Approved indications
- Diagnostic Test for Secondary Adrenocortical Insufficiency
Common side effects
- Hypotension
- Headache
- Dizziness
- Sedation
- Nausea
- Vomiting
- Abdominal discomfort or pain
- Allergic rash
- Decreased white blood cell count or bone marrow depression
Key clinical trials
- Sleep Loss and Circadian Misalignment - Mechanisms of Insulin Resistance (PHASE4)
- Acute Consequences of Glucocorticoid Secretion in Overweight and Obese Individuals During Maximum Calorie Intake (NA)
- Metyrapone Versus Osilodrostat in Patients With Metabolic Autonomous Cortisol Secretion (MACS) (PHASE4)
- Metyrapone for Mild Autonomous Cortisol Secretion (MACS) (PHASE2)
- Effects of Metyrapone in Patients With Hypercortisolism
- Metyrapone Study for Patients Diagnosed With Mild Autonomous Cortisol Secretion - MACS (PHASE2)
- Pembrolizumab in the Treatment of Advanced, Progressive Adrenocortical Carcinoma. (PHASE2)
- Effect of Metyrapone on Cardiovascular Risk Factors in Patients With Adrenal Incidentalomas and Cushing's Syndrome (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Metopirone CI brief — competitive landscape report
- Metopirone updates RSS · CI watch RSS
- Esteve portfolio CI