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

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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 Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Adjunct therapy in treatment of	Acute gouty arthritis		••••••••••••		••••• ••••••••••••	•••• •••••••••• ••••••••
Treatment of	Allergic conjunctivitis (ac)		••••••••••••			•••• •••••••••• ••••••••
Adjunct therapy in treatment of	Ankylosing spondylitis (as)		••••••••••••		••••• ••••••••••••	•••• •••••••••• ••••••••
Treatment of	Anterior segment inflammation		••••••••••••			•••• •••••••••• ••••••••
Treatment of	Chorioretinitis		••••••••••••			•••• •••••••••• ••••••••

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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.

Target	Actions	Organism
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 Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abametapir	The serum concentration of Corticotropin can be increased when it is combined with Abametapir.
Abatacept	The risk or severity of adverse effects can be increased when Abatacept is combined with Corticotropin.
Abemaciclib	The metabolism of Abemaciclib can be increased when combined with Corticotropin.
Acalabrutinib	The metabolism of Acalabrutinib can be increased when combined with Corticotropin.
Acarbose	The risk or severity of hyperglycemia can be increased when Corticotropin is combined with Acarbose.

Food Interactions

No interactions found.

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International/Other Brands

Acthar / Acthar Gel

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Acthar	Injection	80 [USP'U]/1mL	Intramuscular; Subcutaneous	Mallinckrodt ARD LLC	2013-01-07	Not applicable
Acthar Gel Hp Inj 40unit/ml	Gel	40 unit / mL	Intramuscular; Subcutaneous	Armour Pharmaceutical Co.	1987-12-31	1999-12-15
Acthar Powder Inj 40unit/vial	Powder, for solution	40 unit / vial	Intramuscular; Intravenous; Subcutaneous	Armour Pharmaceutical Co.	1988-12-31	1999-12-15
H.P. Acthar	Injection	80 [iU]/1mL	Intravenous	Cangene Biopharma	2005-09-09	2010-02-24
H.P. Acthar	Injection	80 [USP'U]/1mL	Intramuscular; Subcutaneous	Questcor Pharmaceuticals, Inc.	2010-10-15	2013-08-31

Categories

ATC Codes

H01AA01 — Corticotropin

• H01AA — ACTH
• H01A — ANTERIOR PITUITARY LOBE HORMONES AND ANALOGUES
• H01 — PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
• H — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS

Drug Categories

• Adrenal Cortex Hormones
• Adrenocorticotropic Hormone
• Amino Acids, Peptides, and Proteins
• Anterior Pituitary Lobe Hormones and Analogues
• Corticosteroids
• Corticosteroids for Systemic Use
• Cytochrome P-450 CYP3A Inducers
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Inducers
• Cytochrome P-450 CYP3A4 Inducers (strength unknown)
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 Enzyme Inducers
• Cytochrome P-450 Substrates
• Fused-Ring Compounds
• Hormones
• Hormones, Hormone Substitutes, and Hormone Antagonists
• Hyperglycemia-Associated Agents
• Immunosuppressive Agents
• Melanocortins
• Nerve Tissue Proteins
• Neuropeptides
• Peptide Hormones
• Peptides
• Pituitary and Hypothalamic Hormones and Analogues
• Pituitary Hormones
• Pituitary Hormones, Anterior
• Pro-Opiomelanocortin
• Proteins
• Steroids
• Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins

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]

External Links

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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Fibrillary Glomerulonephritis	1
4	Completed	Treatment	Anterior Uveitis (AU) / Clinically Significant Macular Edema / Posterior Uveitis / Scleritis / Uveitis / Uveitis, Intermediate	1
4	Completed	Treatment	CNS Sarcoidosis	1
4	Completed	Treatment	Coronavirus Disease 2019 (COVID‑19) / Sarcoidosis, Pulmonary	1
4	Completed	Treatment	Dermatomyositis (DM) / Juvenile Dermatomyositis (JDM)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

• Biovectra Inc.
• Questcor

Dosage Forms

Form	Route	Strength
Gel	Intramuscular; Subcutaneous	40 unit / mL
Powder, for solution	Intramuscular; Intravenous; Subcutaneous	40 unit / vial
Injection	Intramuscular; Subcutaneous	80 [USP'U]/1mL
Injection	Intravenous	80 [iU]/1mL

Prices

Unit description	Cost	Unit
Acthar hp gel 80 unit/ml vial	5584.56USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US11752199	No	2021-02-25	2041-02-25

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	Easily soluble in cold water, hot water.	Not Available

Targets

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Details1. Adrenocorticotropic hormone receptor

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]

Details2. Corticoliberin

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]

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