Corticorelin
Also known as: Acthrel, Corticorelin acetate, corticorelin ovine triflutate, Cortrosyn, CRF (corticotropin-releasing factor), CRH, hCRH synthetic analog, oCRH
Source Corticorelin at Peptiology
Save 10% with code PEPTI-BOSSRABBIT-10
Affiliate link: we earn a commission on purchases made through this link, at no extra cost to you.
Tapping Shop Now & Save 10% copies your 10% off code PEPTI-BOSSRABBIT-10 to your clipboard. Paste it at the Peptiology checkout to claim the discount.
Summary
Corticorelin acetate (also known as Corticorelin, Acthrel) is a synthetic analogue of human corticotropin‑releasing hormone (CRH) administered by injection. It is prescribed primarily to reduce peritumoral brain edema in patients with malignant brain tumors, with the aim of lowering the dose of corticosteroids such as dexamethasone and thereby limiting steroid‑related toxicity.
Mechanism of Action
Corticorelin mimics endogenous CRH and binds CRH receptors (CRHR1/CRHR2) on hypothalamic and peripheral cells. Activation of these receptors modulates the hypothalamic‑pituitary‑adrenal (HPA) axis, leading to altered cortisol dynamics and, importantly for edema, reduces capillary permeability and inflammatory mediator release in the tumor microenvironment. The net effect is decreased vasogenic fluid accumulation around brain tumors without the broad immunosuppressive actions of steroids.
What the Research Shows
Pre‑clinical animal work demonstrated that CRH analogues can lessen vasogenic brain edema. A Phase I randomized trial reported that corticorelin acetate was well tolerated and reduced peritumoral edema signs. Subsequent Phase I/II studies showed neurological improvement and safety. In a prospective, double‑blind, randomized study of 200 patients on chronic dexamethasone, subcutaneous corticorelin (1 mg twice daily) enabled a greater mean reduction in dexamethasone dose (62.7 % vs 51.4 %; P < 0.001) and showed a trend toward more responders (57 % vs 46 %, P = 0.12). Patients receiving corticorelin experienced less steroid‑induced myopathy and fewer Cushing‑type signs. Phase III trials have been announced but results are not yet published. A 2025 review highlighted the peptide’s suitability for intranasal delivery to the brain, though clinical data for that route are lacking.
Reported Benefits
Clinical evidence suggests corticorelin can lower the required dose of corticosteroids in brain‑tumor patients, potentially reducing steroid‑related side effects such as myopathy, Cushing‑type features, and metabolic disturbances. It appears to be well tolerated, with no major adverse events reported in early trials, and may improve neurological function by decreasing edema‑related mass effect.
Limitations of the Evidence
Evidence is confined to early‑phase and one moderate‑size randomized trial; the primary efficacy endpoint did not reach conventional statistical significance. Phase III data are pending, so definitive conclusions about efficacy and safety are unavailable. The drug’s benefit has only been evaluated for peritumoral brain edema, and its utility in other conditions remains unstudied. Long‑term outcomes and comparative effectiveness versus other steroid‑sparing agents have not been established.
Safety Considerations
Across Phase I‑II studies and the double‑blind trial, corticorelin was reported as well tolerated, with no serious drug‑related adverse events. The main safety advantage reported is a reduction in steroid‑associated complications (myopathy, Cushing‑like signs). No specific peptide‑related toxicities were identified, but systematic safety monitoring in larger populations is still needed.
How It Is Administered
Corticorelin acetate is supplied for parenteral use and can be administered intravenously or subcutaneously. The approved dosing regimen in the reported trial was 1 mg subcutaneously twice daily. Emerging research also explores intranasal delivery to bypass the blood‑brain barrier, but this route is not yet part of standard clinical practice.
Routes of Administration
Goals & Uses
- Peritumoral brain edema reductionTherapeuticLow
- Differential diagnosis of Cushing's syndromeDiagnosticHigh
- Evaluation of pituitary functionDiagnosticHigh
- Evaluation of hypothalamic-pituitary-adrenal (HPA) axis functionDiagnosticModerate
- Diagnostic assessment of ACTH reserveDiagnosticHigh
Contraindications
- Hypersensitivity to corticorelin or any componentAllergyHigh
- Administration with heparin or heparin-containing solutionsDrug InteractionHigh
- Hypersensitivity to corticorelin or excipientsAllergyHigh
- Acute coronary syndromeCardiovascularModerate
Adverse Effects
- Dyspnea/shortness of breathRespiratoryUncommon
- AnaphylaxisImmunologicRareSevere life-threatening allergic reaction
- Injection site reactionsLocalUncommon
- HeadacheNeurologicCommonPain in the head or upper neck
- HypotensionCardiovascularUncommonLow blood pressure
- FlushingVascularCommonWarmth and redness of the skin
- TachycardiaCardiovascularUncommonAbnormally fast heart rate
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
Drug Interactions
- HeparinHigh
- GlucocorticoidsLow
- Glucocorticoids (exogenous)Moderate
- MetyraponeLow
- Beta‑adrenergic agonistsModerate
Population Constraints
- PregnancyReproductive SafetyRelative
- Pediatric patientsAgeRelative
- Patients with cardiovascular diseaseComorbidityRelative
- Pregnant womenReproductiveRelative
Regulatory Status
- European UnionUnapprovedNot authorized for clinical use in the EU.
- United StatesApprovedApproved: Diagnostic testing of ACTH reserveMarketed as Cortrosyn.
- United KingdomUnapprovedNo marketing authorization.
Approved in the United States for diagnostic use (Cortrosyn). Not indicated for therapeutic treatment of disease.
Evidence & Sources
- Journal ArticleModerateMoliterno JA, Henry E, Pannullo SC2009-01-01T00:00:00.000000Z
- Journal ArticleModerateRecht L, et al.2013-01-01T00:00:00.000000Z
- Journal ArticleModerate2004-01-01T00:00:00.000000Z
- Journal ArticleModerateWong ET, Lok E2025-01-01T00:00:00.000000Z
- Journal ArticleModerateRoth P, et al.2013-01-01T00:00:00.000000Z
- Journal ArticleModerateAlten R, et al.2010-01-01T00:00:00.000000Z
Frequently Asked Questions
What condition is corticorelin acetate used to treat?
It is used to manage peritumoral brain edema in patients with malignant brain tumors, primarily to reduce reliance on systemic corticosteroids.
How does corticorelin differ from steroids in treating brain edema?
Unlike steroids, which act broadly on inflammation and immunosuppression, corticorelin targets CRH receptors to modulate vascular permeability and HPA‑axis activity, aiming to lessen edema while avoiding many steroid‑related systemic side effects.
Is corticorelin approved for clinical use?
Yes, it is an approved prescription medication and has received orphan‑drug status for peritumoral brain edema, although large‑scale Phase III efficacy data are still awaited.
What are the common side effects?
Early studies reported no serious adverse events; the main observed benefit is a reduction in steroid‑related side effects such as myopathy and Cushing‑type features. Specific peptide‑related toxicities have not been identified.
Can corticorelin be given by routes other than injection?
The approved formulations are injectable (intravenous or subcutaneous). Research suggests intranasal delivery may reach the brain, but this method is not yet approved for routine clinical use.
What is Corticorelin?
Corticorelin acetate (also known as Corticorelin, Acthrel) is a synthetic analogue of human corticotropin‑releasing hormone (CRH) administered by injection. It is prescribed primarily to reduce peritumoral brain edema in patients with malignant brain tumors, with the aim of lowering the dose of corticosteroids such as dexamethasone and thereby limiting steroid‑related toxicity.
What is Corticorelin used for?
Corticorelin is educationally associated with: Peritumoral brain edema reduction, Differential diagnosis of Cushing's syndrome, Evaluation of pituitary function, Evaluation of hypothalamic-pituitary-adrenal (HPA) axis function, Diagnostic assessment of ACTH reserve. Educational only — not medical advice.
How is Corticorelin administered?
Recorded routes of administration: Intravenous, Subcutaneous.
What are the potential side effects of Corticorelin?
Reported adverse effects include: Dyspnea/shortness of breath, Anaphylaxis, Injection site reactions, Headache, Hypotension, Flushing, Tachycardia, Nausea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Corticorelin?
Recorded contraindications: Hypersensitivity to corticorelin or any component, Administration with heparin or heparin-containing solutions, Hypersensitivity to corticorelin or excipients, Acute coronary syndrome. Consult a qualified clinician before use.