Corticotropin

Identification

Summary

Corticotropin is a diagnostic agent used in the screening of patients presumed to have adrenocortical insufficiency.

Brand Names
Acthar, Cortrophin
Generic Name
Corticotropin
DrugBank Accession Number
DB01285
Background

Corticotropin (ACTH or adrenocorticotropic hormone) is a polypeptide hormone produced and secreted by the pituitary gland. It is an important player in the hypothalamic-pituitary-adrenal axis.

Type
Biotech
Groups
Approved, Investigational, Vet approved
Biologic Classification
Protein Based Therapies
Hormones
Protein Chemical Formula
C207H308N56O58S
Protein Average Weight
4541.0658 Da
Sequences
>ACTH(1-39)
SYSMEHFRWGKPVGKKRRPVKVYPDGAEDQLAEAFPLEF
Download FASTA Format
Synonyms
  • ACTH
  • Adrenocorticotrophin
  • Adrenocorticotropic hormone
  • Corticotrophin
  • Corticotropin
  • Cortigel
  • H.P. acthar gel

Pharmacology

Indication

For use as a diagnostic agent in the screening of patients presumed to have adrenocortical insufficiency.

Purified corticotropin for injection is indicated for a variety of allergic and autoimmune conditions.1

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Adjunct therapy in treatment ofAcute gouty arthritis••••••••••••••••• •••••••••••••••• •••••••••• ••••••••
Treatment ofAllergic conjunctivitis (ac)•••••••••••••••• •••••••••• ••••••••
Adjunct therapy in treatment ofAnkylosing spondylitis (as)••••••••••••••••• •••••••••••••••• •••••••••• ••••••••
Treatment ofAnterior segment inflammation•••••••••••••••• •••••••••• ••••••••
Treatment ofChorioretinitis•••••••••••••••• •••••••••• ••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Corticotropin acts through the stimulation of cell surface ACTH receptors, which are primarily located on the adrenocortical cells. Corticotropin stimulates the cortex of the adrenal gland and boosts the synthesis of corticosteroids, mainly glucocorticoids but also sex steroids (androgens). Corticotropin is also related to the circadian rhythm in many organisms.

Mechanism of action

As a diagnostic aid (adrenocortical function), corticotropin combines with a specific receptor on the adrenal cell plasma membrane. In patients with normal adrenocortical function, it stimulates the initial reaction involved in the synthesis of adrenal steroids (including cortisol, cortisone, weak androgenic substances, and a limited quantity of aldosterone) from cholesterol by increasing the quantity of cholesterol within the mitochondria. Corticotropin does not significantly increase serum cortisol concentrations in patients with primary adrenocortical insufficiency (Addison's disease). The mechanism of action of corticotropin in the treatment of infantile myoclonic seizures is unknown.

TargetActionsOrganism
AAdrenocorticotropic hormone receptor
agonist
Humans
UCorticoliberin
agonist
Humans
Absorption

Corticotropin is rapidly absorbed following intramuscular administration; the repository dosage form is slowly absorbed over approximately 8 to 16 hours.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

About 15 minutes following intravenous administration.

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

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.
DrugInteraction
AbametapirThe serum concentration of Corticotropin can be increased when it is combined with Abametapir.
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Corticotropin.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Corticotropin.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Corticotropin.
AcarboseThe risk or severity of hyperglycemia can be increased when Corticotropin is combined with Acarbose.
Food Interactions
No interactions found.

Products

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International/Other Brands
Acthar / Acthar Gel
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ActharInjection80 [USP'U]/1mLIntramuscular; SubcutaneousMallinckrodt ARD LLC2013-01-07Not applicableUS flag
Acthar Gel Hp Inj 40unit/mlGel40 unit / mLIntramuscular; SubcutaneousArmour Pharmaceutical Co.1987-12-311999-12-15Canada flag
Acthar Powder Inj 40unit/vialPowder, for solution40 unit / vialIntramuscular; Intravenous; SubcutaneousArmour Pharmaceutical Co.1988-12-311999-12-15Canada flag
H.P. ActharInjection80 [USP'U]/1mLIntramuscular; SubcutaneousQuestcor Pharmaceuticals, Inc.2010-10-152013-08-31US flag
H.P. ActharInjection80 [iU]/1mLIntravenousCangene Biopharma2005-09-092010-02-24US flag

Categories

ATC Codes
H01AA01 — Corticotropin
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
  • Humans and other mammals

Chemical Identifiers

UNII
K0U68Q2TXA
CAS number
12427-33-7

References

Synthesis Reference

Wylie W. Vale, Jr., Mary P. Stenzel-Poore, "Corticotropin-releasing factor overproducing transgenic mice." U.S. Patent US6023011, issued June, 1993.

US6023011
General References
  1. FDA Approved Drug Products: CORTROPHIN (corticotropin) gel for injection [Link]
KEGG Drug
D00146
KEGG Compound
C02017
PubChem Substance
46506307
RxNav
376
ChEMBL
CHEMBL1201610
PharmGKB
PA449129
Drugs.com
Drugs.com Drug Page
Wikipedia
Adrenocorticotropic_hormone
MSDS
Download (72.7 KB)

Clinical Trials

Clinical Trials

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Biovectra Inc.
  • Questcor
Dosage Forms
FormRouteStrength
GelIntramuscular; Subcutaneous40 unit / mL
Powder, for solutionIntramuscular; Intravenous; Subcutaneous40 unit / vial
InjectionIntramuscular; Subcutaneous80 [USP'U]/1mL
InjectionIntravenous80 [iU]/1mL
Prices
Unit descriptionCostUnit
Acthar hp gel 80 unit/ml vial5584.56USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US11752199No2021-02-252041-02-25US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityEasily soluble in cold water, hot water.Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Melanocortin receptor activity
Specific Function
Receptor for corticotropin (ACTH). This receptor is mediated by G proteins (G(s)) which activate adenylate cyclase (cAMP).
Gene Name
MC2R
Uniprot ID
Q01718
Uniprot Name
Adrenocorticotropic hormone receptor
Molecular Weight
33926.28 Da
References
  1. Johnston H, King PJ, O'Shaughnessy PJ: Effects of ACTH and expression of the melanocortin-2 receptor in the neonatal mouse testis. Reproduction. 2007 Jun;133(6):1181-7. [Article]
  2. Carey LC, Su Y, Valego NK, Rose JC: Infusion of ACTH stimulates expression of adrenal ACTH receptor and steroidogenic acute regulatory protein mRNA in fetal sheep. Am J Physiol Endocrinol Metab. 2006 Aug;291(2):E214-20. Epub 2006 Feb 14. [Article]
  3. Hruby VJ, Cai M, Cain JP, Mayorov AV, Dedek MM, Trivedi D: Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor. Curr Top Med Chem. 2007;7(11):1107-19. [Article]
  4. Suri D, Alonso M, Weiss RE: A case of ACTH-independent bilateral macronodular adrenal hyperplasia and severe congestive heart failure. J Endocrinol Invest. 2006 Nov;29(10):940-6. [Article]
  5. Lin L, Hindmarsh PC, Metherell LA, Alzyoud M, Al-Ali M, Brain CE, Clark AJ, Dattani MT, Achermann JC: Severe loss-of-function mutations in the adrenocorticotropin receptor (ACTHR, MC2R) can be found in patients diagnosed with salt-losing adrenal hypoplasia. Clin Endocrinol (Oxf). 2007 Feb;66(2):205-10. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Receptor binding
Specific Function
Hormone regulating the release of corticotropin from pituitary gland (By similarity). Induces NLRP6 in intestinal epithelial cells, hence may influence gut microbiota profile (By similarity).
Gene Name
CRH
Uniprot ID
P06850
Uniprot Name
Corticoliberin
Molecular Weight
21421.505 Da
References
  1. Hellman P, Linder F, Hennings J, Hessman O, Eriksson B, Orlefors H, Akerstrom G: Bilateral adrenalectomy for ectopic Cushing's syndrome-discussions on technique and indication. World J Surg. 2006 May;30(5):909-16. [Article]
  2. Dinan TG, Quigley EM, Ahmed SM, Scully P, O'Brien S, O'Mahony L, O'Mahony S, Shanahan F, Keeling PW: Hypothalamic-pituitary-gut axis dysregulation in irritable bowel syndrome: plasma cytokines as a potential biomarker? Gastroenterology. 2006 Feb;130(2):304-11. [Article]
  3. Zhao LF, Iwasaki Y, Oki Y, Tsugita M, Taguchi T, Nishiyama M, Takao T, Kambayashi M, Hashimoto K: Purinergic receptor ligands stimulate pro-opiomelanocortin gene expression in AtT-20 pituitary corticotroph cells. J Neuroendocrinol. 2006 Apr;18(4):273-8. [Article]
  4. Wagner U, Wahle M, Moritz F, Wagner U, Hantzschel H, Baerwald CG: Promoter polymorphisms regulating corticotrophin-releasing hormone transcription in vitro. Horm Metab Res. 2006 Feb;38(2):69-75. [Article]
  5. Matejec R, Uhlich H, Hotz C, Muhling J, Harbach HW, Bodeker RH, Hempelmann G, Teschemacher H: Corticotropin-releasing hormone reduces pressure pain sensitivity in humans without involvement of beta-endorphin(1-31), but does not reduce heat pain sensitivity. Neuroendocrinology. 2005;82(3-4):185-97. Epub 2006 Mar 13. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid delta-isomerase activity
Specific Function
3-beta-HSD is a bifunctional enzyme, that catalyzes the oxidative conversion of Delta(5)-ene-3-beta-hydroxy steroid, and the oxidative conversion of ketosteroids. The 3-beta-HSD enzymatic system pl...
Gene Name
HSD3B2
Uniprot ID
P26439
Uniprot Name
3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2
Molecular Weight
42051.845 Da
References
  1. Bassett MH, Suzuki T, Sasano H, De Vries CJ, Jimenez PT, Carr BR, Rainey WE: The orphan nuclear receptor NGFIB regulates transcription of 3beta-hydroxysteroid dehydrogenase. implications for the control of adrenal functional zonation. J Biol Chem. 2004 Sep 3;279(36):37622-30. Epub 2004 Jun 18. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Iron ion binding
Specific Function
Catalyzes the conversion of 25-hydroxyvitamin D3 (25(OH)D) to 1-alpha,25-dihydroxyvitamin D3 (1,25(OH)2D) plays an important role in normal bone growth, calcium metabolism, and tissue differentiation.
Gene Name
CYP27B1
Uniprot ID
O15528
Uniprot Name
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
Molecular Weight
56503.475 Da
References
  1. Dunbar DR, Khaled H, Evans LC, Al-Dujaili EA, Mullins LJ, Mullins JJ, Kenyon CJ, Bailey MA: Transcriptional and physiological responses to chronic ACTH treatment by the mouse kidney. Physiol Genomics. 2010 Feb 4;40(3):158-66. doi: 10.1152/physiolgenomics.00088.2009. Epub 2009 Nov 17. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxidoreductase activity
Specific Function
Has a role in maintaining calcium homeostasis. Catalyzes the NADPH-dependent 24-hydroxylation of calcidiol (25-hydroxyvitamin D(3)) and calcitriol (1-alpha,25-dihydroxyvitamin D(3)). The enzyme can...
Gene Name
CYP24A1
Uniprot ID
Q07973
Uniprot Name
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
Molecular Weight
58874.695 Da
References
  1. Dunbar DR, Khaled H, Evans LC, Al-Dujaili EA, Mullins LJ, Mullins JJ, Kenyon CJ, Bailey MA: Transcriptional and physiological responses to chronic ACTH treatment by the mouse kidney. Physiol Genomics. 2010 Feb 4;40(3):158-66. doi: 10.1152/physiolgenomics.00088.2009. Epub 2009 Nov 17. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Hanafusa J, Mune T, Tanahashi T, Isomura Y, Suwa T, Isaji M, Daido H, Morita H, Murayama M, Yasuda K: Altered corticosteroid metabolism differentially affects pituitary corticotropin response. Am J Physiol Endocrinol Metab. 2002 Feb;282(2):E466-73. doi: 10.1152/ajpendo.00065.2001. [Article]
  2. Dimaraki EV, Jaffe CA: Troglitazone induces CYP3A4 activity leading to falsely abnormal dexamethasone suppression test. J Clin Endocrinol Metab. 2003 Jul;88(7):3113-6. doi: 10.1210/jc.2002-021778. [Article]

Drug created at May 24, 2007 05:14 / Updated at November 13, 2021 11:07