Identification
- Summary
Corticorelin ovine triflutate is a synthetic corticotropin-releasing hormone used for diagnostic purposes in differentiating pituitary and ectopic production of ACTH in patients with ACTH-dependent Cushing's syndrome.
- Brand Names
- Acthrel
- Generic Name
- Corticorelin ovine triflutate
- DrugBank Accession Number
- DB09067
- Background
Corticorelin, available commercially as corticorelin ovine triflutate (tradename Acthrel), is a synthetic form of the peptide human corticotropin-releasing hormone (hCRH), a potent stimulator of adrenocorticotropic hormone (ACTH) release from the anterior pituitary. Endogenous forms hCRH are involved in the stress response and its main function is stimulation of the pituitary to release ACTH.
It is used as a diagnostic agent to evaluate the status of the pituitary-adrenal axis in the differentiation of a pituitary source from an ectopic source of excessive ACTH secretion. It provides a differential diagnosis for Cushing's disease (a pituitary source of ACTH excess) or of ectopic ACTH syndrome (an ectopic source of ACTH excess). If corticorelin injection results in an increase of plasma ACTH and cortisol, the patient is diagnosed with Cushing's disease. However, if corticorelin injection does not result in an increase of plasma ACTH and cortisol, the patient is diagnosed with ectopic ACTH syndrome.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- Corticorelin ovine
- Corticorelin ovine triflutate
- Corticorelin triflutate
- Corticotropin-releasing factor (sheep hypothalamus)
- Corticotropin-releasing factor (sheep)
- Ovine ACTH releasing factor
- Ovine corticotropin-releasing factor
- Ovine CRF 41
- Ovine CRH
- Sheep corticotropin-releasing factor
- Sheep corticotropin-releasing factor (1-41)
Pharmacology
- Indication
Corticorelin is indicated for use in differentiating pituitary and ectopic production of ACTH in patients with ACTH-dependent Cushing's syndrome.
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- Contraindications & Blackbox Warnings
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In normal subjects, intravenous administration of corticorelin results in a rapid and sustained increase of plasma ACTH levels and a near parallel increase of plasma cortisol. In addition, intravenous administration of corticorelin to normal subjects causes a concomitant and prolonged release of the related proopiomelanocortin peptides β- and γ-lipotropins (β -and γ-LPH) and β-endorphin (β -END).
- Mechanism of action
Corticorelin is a potent stimulator of adrenocorticotropic hormone (ACTH) release from the anterior pituitary. It is used as a diagnostic agent to evaluate the status of the pituitary-adrenal axis in the differentiation of a pituitary source from an ectopic source of excessive ACTH secretion.
Target Actions Organism ACorticotropin-releasing factor receptor 1 ligand- Absorption
Plasma ACTH levels in normal subjects increased 2 minutes after injection of corticorelin doses of ≥0.3 mcg/kg and reached peak levels after 10-15 minutes. Plasma cortisol levels increased within 10 minutes and reached peak levels at 30 to 60 minutes.
- Volume of distribution
The mean volume of distribution for IR-corticorelin is 6.2 ± 0.5 L
- Protein binding
Corticorelin does not appear to be bound specifically by a circulating plasma protein.
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Plasma half-lives for IR-corticorelin are 11.6 ± 1.5 minutes (mean ± SE) for the fast component and 73 ± 8 minutes for the slow component.
- Clearance
95 ± 11 L/m2/day
- Adverse Effects
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The severity of adverse effects to a corticorelin injection appear to be dose-dependent. Dosages above 1 mcg/kg are not recommended. While few adverse effects have been observed at the 1 mcg/kg or 100 mcg dose, higher doses have been associated with transient tachycardia, decreased blood pressure, loss of consciousness, and asystole.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareArdeparin The risk or severity of hypotension and sinus node depression can be increased when Ardeparin is combined with Corticorelin ovine triflutate. Beclomethasone dipropionate The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Beclomethasone dipropionate. Bemiparin The risk or severity of hypotension and sinus node depression can be increased when Bemiparin is combined with Corticorelin ovine triflutate. Betamethasone The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Betamethasone. Betamethasone phosphate The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Betamethasone phosphate. Budesonide The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Budesonide. Ciclesonide The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Ciclesonide. Clobetasol propionate The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Clobetasol propionate. Corticotropin The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Corticotropin. Corticotropin zinc hydroxide The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Corticotropin zinc hydroxide. 
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- No interactions found.
Products
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Name Kind UNII CAS InChI Key Corticorelin unknown 305OE8862Y 86784-80-7 Not applicable - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Acthrel Injection, powder, lyophilized, for solution 100 ug/2mL Intravenous Ferring Pharmaceuticals Inc. 1997-11-10 Not applicable US 
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 56X54T817Q
- CAS number
- 121249-14-7
References
- General References
- Not Available
- External Links
- KEGG Drug
- D03592
- PubChem Compound
- 16132344
- PubChem Substance
- 310265000
- ChemSpider
- 17289003
- 74671
- ChEBI
- 65307
- ChEMBL
- CHEMBL1201591
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Corticorelin
- FDA label
- Download (2.56 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Active Not Recruiting Basic Science Sleep Restriction 1 1 Completed Basic Science Stress (Psychology) 1 0 Active Not Recruiting Basic Science Sleep Restriction 1 0 Completed Diagnostic Pituitary Neoplasms 1 Not Available Completed Not Available Dependence, Cocaine 1 Not Available Not Yet Recruiting Diagnostic Cushing's Disease / Pituitary Adenoma 1 Not Available Withdrawn Basic Science Functional Dyspepsia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 100 ug/2mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Not Available
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- G-protein coupled receptor for CRH (corticotropin-releasing factor) and UCN (urocortin). Has high affinity for CRH and UCN. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and down-stream effectors, such as adenylate cyclase. Promotes the activation of adenylate cyclase, leading to increased intracellular cAMP levels. Inhibits the activity of the calcium channel CACNA1H. Required for normal embryonic development of the adrenal gland and for normal hormonal responses to stress. Plays a role in the response to anxiogenic stimuli.
- Specific Function
- Corticotrophin-releasing factor receptor activity
- Gene Name
- CRHR1
- Uniprot ID
- P34998
- Uniprot Name
- Corticotropin-releasing factor receptor 1
- Molecular Weight
- 50718.755 Da
Drug created at May 11, 2015 22:48 / Updated at September 05, 2022 12:50