Corticotropin

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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	Approval Level	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	••••••••••••		•••• •••••••••• ••••••••

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.

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

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
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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.

Products

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International/Other Brands

Acthar / Acthar Gel

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Acthar	Injection	80 [USP'U]/1mL	Intramuscular; Subcutaneous	Mallinckrodt ARD LLC	2013-01-07	Not applicable
Acthar	Injection	80 [USP'U]/1mL	Subcutaneous	Mallinckrodt ARD LLC	2024-02-29	Not applicable
Acthar	Injection	40 [USP'U]/0.5mL	Subcutaneous	Mallinckrodt ARD LLC	2024-02-29	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

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

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

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Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
Unlock 175K+ rows when you subscribe.View sample data
4	Active Not Recruiting	Treatment	Fibrillary Glomerulonephritis	1	somestatus	stop reason	just information to hide
4	Completed	Treatment	Anterior Uveitis (AU) / Clinically Significant Macular Edema / Posterior Uveitis / Scleritis / Uveitis / Uveitis, Intermediate	1	somestatus	stop reason	just information to hide
4	Completed	Treatment	CNS Sarcoidosis	1	somestatus	stop reason	just information to hide
4	Completed	Treatment	Coronavirus Disease 2019 (COVID‑19) / Sarcoidosis, Pulmonary	1	somestatus	stop reason	just information to hide
4	Completed	Treatment	Dermatomyositis (DM) / Juvenile Dermatomyositis (JDM)	1	somestatus	stop reason	just information to hide

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Biovectra Inc.
Questcor

Dosage Forms

Form	Route	Strength
Injection	Subcutaneous	40 [USP'U]/0.5mL
Injection	Subcutaneous	80 [USP'U]/1mL
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
US11975047	No	2023-10-27	2043-10-27

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: Receptor for corticotropin (ACTH). This receptor is mediated by G proteins (G(s)) which activate adenylate cyclase (cAMP)
Specific Function: Corticotropin receptor activity
Gene Name: MC2R
Uniprot ID: Q01718
Uniprot Name: Adrenocorticotropic hormone receptor
Molecular Weight: 33926.28 Da

References

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]
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]
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]
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]
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: 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)
Specific Function: Corticotropin-releasing hormone activity
Gene Name: CRH
Uniprot ID: P06850
Uniprot Name: Corticoliberin
Molecular Weight: 21421.505 Da

References

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]
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]
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]
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]
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

Details1. 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General 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 plays a crucial role in the biosynthesis of all classes of hormonal steroids
Specific Function: 3-beta-hydroxy-delta5-steroid dehydrogenase activity
Gene Name: HSD3B2
Uniprot ID: P26439
Uniprot Name: 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2
Molecular Weight: 42051.845 Da

References

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]

Details2. 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in vitamin D metabolism and in calcium and phosphorus homeostasis. Catalyzes the rate-limiting step in the activation of vitamin D in the kidney, namely the hydroxylation of 25-hydroxyvitamin D3/calcidiol at the C1alpha-position to form the hormonally active form of vitamin D3, 1alpha,25-dihydroxyvitamin D3/calcitriol that acts via the vitamin D receptor (VDR) (PubMed:10518789, PubMed:10566658, PubMed:12050193, PubMed:22862690, PubMed:9486994). Has 1alpha-hydroxylase activity on vitamin D intermediates of the CYP24A1-mediated inactivation pathway (PubMed:10518789, PubMed:22862690). Converts 24R,25-dihydroxyvitamin D3/secalciferol to 1-alpha,24,25-trihydroxyvitamin D3, an active ligand of VDR. Also active on 25-hydroxyvitamin D2 (PubMed:10518789). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via FDXR/adrenodoxin reductase and FDX1/adrenodoxin (PubMed:22862690)
Specific Function: Calcidiol 1-monooxygenase activity
Gene Name: CYP27B1
Uniprot ID: O15528
Uniprot Name: 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
Molecular Weight: 56503.475 Da

References

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]

Details3. 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase with a key role in vitamin D catabolism and calcium homeostasis. Via C24- and C23-oxidation pathways, catalyzes the inactivation of both the vitamin D precursor calcidiol (25-hydroxyvitamin D(3)) and the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:11012668, PubMed:15574355, PubMed:16617161, PubMed:24893882, PubMed:29461981, PubMed:8679605). With initial hydroxylation at C-24 (via C24-oxidation pathway), performs a sequential 6-step oxidation of calcitriol leading to the formation of the biliary metabolite calcitroic acid (PubMed:15574355, PubMed:24893882). With initial hydroxylation at C-23 (via C23-oxidation pathway), catalyzes sequential oxidation of calcidiol leading to the formation of 25(OH)D3-26,23-lactone as end product (PubMed:11012668, PubMed:8679605). Preferentially hydroxylates at C-25 other vitamin D active metabolites, such as CYP11A1-derived secosteroids 20S-hydroxycholecalciferol and 20S,23-dihydroxycholecalciferol (PubMed:25727742). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via FDXR/adrenodoxin reductase and FDX1/adrenodoxin (PubMed:8679605)
Specific Function: 1-alpha,25-dihydroxyvitamin d3 23-hydroxylase activity
Gene Name: CYP24A1
Uniprot ID: Q07973
Uniprot Name: 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
Molecular Weight: 58874.695 Da

References

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]

Details4. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate
Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
Specific Function: 1,8-cineole 2-exo-monooxygenase activity
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

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]
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

Corticotropin

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Clinical Trial & Rare Diseases Add-on Data Package

Pharmacoeconomics

Properties

Targets

References

References

Enzymes

References

References

References

References