You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameCorticotropin
Accession NumberDB01285
TypeBiotech
GroupsApproved, Vet Approved
DescriptionCorticotropin (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.
Protein structureNo structure small
Related Articles
Protein chemical formulaC207H308N56O58S
Protein average weight4541.0658 Da
Sequences
>ACTH(1-39)
SYSMEHFRWGKPVGKKRRPVKVYPDGAEDQLAEAFPLEF
Download FASTA Format
Synonyms
ACTH
Acthar
Adrenocorticotrophin
Adrenocorticotropic hormone
Corticotrophin
Cortigel
H.P. acthar gel
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Acthar Gel Hp Inj 40unit/mlGel40 unitIntramuscular; SubcutaneousArmour Pharmaceutical Co.1987-12-311999-12-15Canada
Acthar Powder Inj 40unit/vialPowder, for solution40 unitIntramuscular; Intravenous; SubcutaneousArmour Pharmaceutical Co.1988-12-311999-12-15Canada
H.P. ActharInjection80 [USP'U]/mLIntramuscular; SubcutaneousMallinckrodt Ard Inc.2013-01-07Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Acthar GelNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIK0U68Q2TXA
CAS number12427-33-7
Pharmacology
IndicationFor use as a diagnostic agent in the screening of patients presumed to have adrenocortical insufficiency.
Structured Indications
PharmacodynamicsCorticotropin 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 actionAs 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Adrenocorticotropic hormone receptorProteinyes
agonist
HumanQ01718 details
CorticoliberinProteinunknown
agonist
HumanP06850 details
Related Articles
AbsorptionCorticotropin is rapidly absorbed following intramuscular administration; the repository dosage form is slowly absorbed over approximately 8 to 16 hours.
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeAbout 15 minutes following intravenous administration.
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Corticotropin.Approved, Investigational
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Corticotropin.Withdrawn
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Corticotropin.Experimental
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Corticotropin.Approved
ALT-110The risk or severity of adverse effects can be increased when Corticotropin is combined with ALT-110.Investigational
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Corticotropin.Investigational
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Corticotropin.Investigational
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Corticotropin.Withdrawn
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Corticotropin.Approved
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Corticotropin.Experimental
CDX-110The risk or severity of adverse effects can be increased when Corticotropin is combined with CDX-110.Investigational
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Corticotropin.Approved
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Corticotropin.Experimental
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Corticotropin.Approved
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Corticotropin.Investigational
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Corticotropin.Approved
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Corticotropin.Approved
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Corticotropin.Approved, Investigational
FingolimodCorticotropin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Corticotropin is combined with G17DT.Investigational
GI-5005The risk or severity of adverse effects can be increased when Corticotropin is combined with GI-5005.Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Corticotropin.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Corticotropin.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Corticotropin.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Corticotropin.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Corticotropin.Approved
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Corticotropin.Approved
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Corticotropin.Investigational
INGN 201The risk or severity of adverse effects can be increased when Corticotropin is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Corticotropin is combined with INGN 225.Investigational
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Corticotropin.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Corticotropin.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Corticotropin.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Corticotropin.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Corticotropin.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Corticotropin.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Corticotropin is combined with Leflunomide.Approved, Investigational
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Corticotropin.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Corticotropin.Approved
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Corticotropin.Approved
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Corticotropin.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Corticotropin.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Corticotropin.Approved, Investigational
NatalizumabThe risk or severity of adverse effects can be increased when Corticotropin is combined with Natalizumab.Approved, Investigational
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Corticotropin.Approved, Investigational
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Corticotropin.Approved, Withdrawn
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Corticotropin.Approved, Investigational
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Corticotropin.Approved, Investigational
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Corticotropin.Approved, Investigational
Rabies vaccineThe risk or severity of adverse effects can be increased when Corticotropin is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Corticotropin.Approved
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Corticotropin.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Corticotropin.Approved
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Corticotropin.Approved, Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Corticotropin.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Corticotropin.Approved
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Corticotropin.Approved, Investigational
SRP 299The risk or severity of adverse effects can be increased when Corticotropin is combined with SRP 299.Investigational
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Corticotropin.Approved, Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Corticotropin.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Corticotropin is combined with TG4010.Investigational
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Corticotropin.Investigational
TofacitinibCorticotropin may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Corticotropin.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Corticotropin.Approved
TrastuzumabTrastuzumab may increase the neutropenic activities of Corticotropin.Approved, Investigational
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Corticotropin.Withdrawn
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Corticotropin.Approved, Investigational
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Corticotropin.Approved, Investigational
Food InteractionsNot Available
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 ReferencesNot Available
External Links
ATC CodesH01AA01
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (72.7 KB)
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
GelIntramuscular; Subcutaneous40 unit
Powder, for solutionIntramuscular; Intravenous; Subcutaneous40 unit
InjectionIntramuscular; Subcutaneous80 [USP'U]/mL
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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityEasily soluble in cold water, hot water.Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
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
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. [PubMed:17636172 ]
  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. [PubMed:16478774 ]
  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. [PubMed:17584128 ]
  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. [PubMed:17185906 ]
  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. [PubMed:17223989 ]
Kind
Protein
Organism
Human
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
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. [PubMed:16467980 ]
  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. [PubMed:16472586 ]
  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. [PubMed:16503922 ]
  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. [PubMed:16523405 ]
  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. [PubMed:16534240 ]

Enzymes

Kind
Protein
Organism
Human
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 plays a crucial role in the biosynthesis of all classes of hormonal steroids.
Gene Name:
HSD3B2
Uniprot ID:
P26439
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. [PubMed:15208301 ]
Kind
Protein
Organism
Human
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
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. [PubMed:19920212 ]
Kind
Protein
Organism
Human
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 perform up to 6 rounds of hydroxylation of calcitriol leading to calcitroic acid. It also shows 23-hydroxylating activity leading to 1-alpha,25-dihydroxyvitamin D(3)-26,23-lactone as end product.
Gene Name:
CYP24A1
Uniprot ID:
Q07973
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. [PubMed:19920212 ]
Comments
comments powered by Disqus
Drug created on May 23, 2007 23:14 / Updated on November 21, 2016 11:25