Identification

Name
Glucagon
Accession Number
DB00040  (BTD00057, BIOD00057)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Hormones
Description

Glucagon is a 29 residue peptide hormone. Glucagon is synthesized in a special non-pathogenic laboratory strain of Escherichia coli bacteria that has been genetically altered by the addition of the gene for glucagons.

Protein structure
Db00040
Protein chemical formula
C165H249N49O51S1
Protein average weight
3767.1 Da
Sequences
>Glucagon for Injection Sequence 
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Download FASTA Format
Synonyms
  • Glucagon
  • Glucagon (recombinant dna origin)
  • Glucagon recombinant
  • Glucagon, human
  • Glucagon, porcine
  • Glucagone
  • Glucagonum
Product Ingredients
IngredientUNIICASInChI Key
Glucagon hydrochloride1H87NVF4DB19179-82-9Not applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Glucag0nKit1 mg/1mLIntramuscular; Intravenous; SubcutaneousHF Acquisition Co LLC, DBA HealthFirst2018-10-20Not applicableUs
GlucaGenKit; Powder, for solution1 mgIntramuscularNovo Nordisk2010-01-04Not applicableCanada
GlucaGenKit1 mg/1mLBedford Pharmaceuticals2005-06-222016-11-30Us
GlucaGenInjection, powder, for solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousBoehringer Ingelheim Pharmaceuticals, Inc.2005-06-22Not applicableUs
GlucaGenKit1 mg/1mLBoehringer Ingelheim Pharmaceuticals, Inc.2005-06-22Not applicableUs
GlucaGen HypoKitKit1 mg/1mLNovo Nordisk2005-06-22Not applicableUs
GlucaGen HypoKitKit; Powder, for solution1 mgIntramuscularNovo Nordisk2009-12-23Not applicableCanada
GlucagonKit; Powder, for solution1 mgIntramuscular; Intravenous; SubcutaneousEli Lilly & Co. Ltd.2002-05-27Not applicableCanada
GlucagonKit1 mg/1mLFresenius Kabi2015-12-01Not applicableUs
GlucagonKit1 mg/1mLEli Lilly & Co. Ltd.1999-03-01Not applicableUs
Categories
UNII
76LA80IG2G
CAS number
16941-32-5

Pharmacology

Indication

For treatment of severe hypoglycemia, also used in gastrointestinal imaging

Associated Conditions
Pharmacodynamics

Used in the treatment of hypoglycemia and in gastric imaging, glucagon increases blood glucose concentration and is used in the treatment of hypoglycemia. Glucagon acts only on liver glycogen, converting it to glucose through the release of insulin. It also relaxes the smooth muscles of the gastrointestinal tract.

Mechanism of action

Glucagon binds the glucagon receptor, a G protein-coupled receptor located in the plasma membrane, which then initiates a dual signaling pathway using both adenylate cyclase activation and increased intracellular calcium. Adenylate cyclase manufactures cAMP (cyclic AMP), which activates protein kinase A (cAMP-dependent protein kinase). This enzyme, in turn, activates phosphorylase kinase, which, in turn, phosphorylates glycogen phosphorylase, converting into the active form called phosphorylase A. Phosphorylase A is the enzyme responsible for the release of glucose-1-phosphate from glycogen polymers. This yields glucose molecules to be released into the blood. Glucagon receptors are found in the liver, kidney, brain and pancreatic islet cells. The glucagon mediated signals lead to an increase in insulin excretion

TargetActionsOrganism
AGlucagon receptor
agonist
Human
UGlucagon-like peptide 2 receptorNot AvailableHuman
UGlucagon-like peptide 1 receptorNot AvailableHuman
Absorption
Not Available
Volume of distribution
  • 0.25 L/kg
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
  • 13.5  mL/min/kg [Adults with IV 1 mg]
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe therapeutic efficacy of (R)-warfarin can be increased when used in combination with Glucagon recombinant.
(S)-WarfarinThe therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Glucagon recombinant.
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Glucagon recombinant is combined with 2,4-thiazolidinedione.
4-hydroxycoumarinThe therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Glucagon recombinant.
AcarboseThe risk or severity of hypoglycemia can be increased when Glucagon recombinant is combined with Acarbose.
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be increased when used in combination with Glucagon recombinant.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Glucagon recombinant is combined with Acetohexamide.
AclidiniumAclidinium may increase the gastrointestinal motility reducing activities of Glucagon recombinant.
AICA ribonucleotideThe risk or severity of hypoglycemia can be increased when Glucagon recombinant is combined with AICA ribonucleotide.
AlaproclateThe risk or severity of hypoglycemia can be increased when Glucagon recombinant is combined with Alaproclate.
Food Interactions
Not Available

References

General References
  1. White CM: A review of potential cardiovascular uses of intravenous glucagon administration. J Clin Pharmacol. 1999 May;39(5):442-7. [PubMed:10234590]
External Links
UniProt
Q8MJ25
Genbank
AF529185
KEGG Drug
D00116
KEGG Compound
C01501
PubChem Substance
46504732
ChEMBL
CHEMBL266481
Therapeutic Targets Database
DAP001037
PharmGKB
PA164779052
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Glucagon_recombinant
ATC Codes
H04AA01 — Glucagon
AHFS Codes
  • 68:22.12 — Glycogenolytic Agents
FDA label
Download (43.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingBasic ScienceBMI >30 kg/m21
1CompletedBasic ScienceBMI >30 kg/m2 / Hyperglucagonaemia1
1CompletedBasic ScienceDiabetes, Diabetes Mellitus Type 11
1CompletedBasic ScienceDiabetes, Diabetes Mellitus Type 1 / Hypoglycemia1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedTreatmentDiabetes Mellitus (DM)1
1CompletedTreatmentDiabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 1 / Type 2 Diabetes Mellitus1
1CompletedTreatmentDiabetes, Diabetes Mellitus Type 12
1CompletedTreatmentHealthy Volunteers / Type 2 Diabetes Mellitus1
1CompletedTreatmentHypoglycemia4
1CompletedTreatmentType 2 Diabetes Mellitus3
1RecruitingBasic ScienceBMI >30 kg/m21
1RecruitingOtherHealthy Volunteers1
1RecruitingTreatmentType1 Diabetes Mellitus1
1WithdrawnBasic ScienceDiabetes, Diabetes Mellitus Type 11
1, 2CompletedPreventionPost-bariatric Hypoglycemia1
2CompletedPreventionCongenital Hyperinsulinism1
2CompletedPreventionDiabetes, Diabetes Mellitus Type 11
2CompletedTreatmentComplications of Bariatric Procedures / Hypoglycemia1
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 17
2CompletedTreatmentHypoglycemia6
2Not Yet RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
2Not Yet RecruitingTreatmentHyperinsulinemic Hypoglycemia1
2RecruitingTreatmentDiabetes, Diabetes Mellitus Type 1 / Hypoglycemia Unawareness1
2WithdrawnTreatmentDiabetes, Diabetes Mellitus Type 12
2, 3CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
2, 3RecruitingBasic ScienceBMI >30 kg/m21
3CompletedNot AvailableDiabetes Mellitus (DM) / Drug-Specific Antibodies / Hypoglycemia1
3CompletedTreatmentDiabetes Mellitus (DM)1
3CompletedTreatmentDiabetes Mellitus (DM) / Drug-Specific Antibodies / Hypoglycemia1
3CompletedTreatmentDiabetes Mellitus (DM) / Hypoglycemia1
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 12
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 1 / Hypoglycemia3
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 1 / Insulin Hypoglycemia / Severe Hypoglycemia1
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 1 / Type 2 Diabetes Mellitus1
3RecruitingTreatmentDiabetes, Diabetes Mellitus Type 1 / Insulin Hypoglycemia / Severe Hypoglycemia1
3RecruitingTreatmentHypoglycemia1
3Unknown StatusBasic ScienceBMI >30 kg/m2 / Diabetes, Diabetes Mellitus Type 1 / Healthy Volunteers1
4Active Not RecruitingBasic ScienceDiabetes, Diabetes Mellitus Type 11
4Active Not RecruitingDiagnosticMalignant Neoplasm of Colon1
4CompletedDiagnosticDiabetes Mellitus (DM)1
4RecruitingBasic ScienceDrug Overdose / Overdose of Beta-adrenergic Blocking Drug1
4Unknown StatusDiagnosticLiver Diseases1
4WithdrawnTreatmentWomen With Fertility Disorder1
Not AvailableActive Not RecruitingBasic ScienceDiabetes Mellitus (DM) / Metabolic Syndromes1
Not AvailableActive Not RecruitingBasic ScienceMetabolic Diseases1
Not AvailableActive Not RecruitingBasic ScienceNormal Cellular Metabolism1
Not AvailableActive Not RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableCompletedBasic ScienceDiabetes Mellitus (DM)1
Not AvailableCompletedBasic ScienceDiabetes, Diabetes Mellitus Type 12
Not AvailableCompletedSupportive CareDiabetes, Diabetes Mellitus Type 11
Not AvailableRecruitingBasic ScienceDiabetes Mellitus (DM) / Non-Alcoholic Fatty Liver Disease (NAFLD) / Total Pancreatectomy1
Not AvailableSuspendedTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableTerminatedTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableUnknown StatusBasic ScienceHealthy Volunteers1
Not AvailableUnknown StatusTreatmentHyperglycemias / Infant, Low Birth Weight1

Pharmacoeconomics

Manufacturers
  • Eli lilly and co
  • Novo nordisk pharmaceuticals inc
Packagers
  • Bedford Labs
  • Eli Lilly & Co.
  • Novo Nordisk Inc.
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
KitIntramuscular; Intravenous; Subcutaneous1 mg/1mL
Injection, powder, for solutionIntramuscular; Intravenous; Subcutaneous1 mg/1mL
Kit; powder, for solutionIntramuscular1 mg
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous1 mg/1mL
Kit1 mg/1mL
Kit; powder, for solutionIntramuscular; Intravenous; Subcutaneous1 mg
Powder, for solutionIntramuscular; Intravenous; Subcutaneous1 mg
Prices
Unit descriptionCostUnit
Glucagon 1 mg kit128.34USD kit
Glucagon Emergency 1 mg Kit Box124.05USD box
GlucaGen HypoKit 1 mg Solution Box123.72USD box
Glucagen 1 mg hypokit120.36USD kit
Glucagon 1 mg emergency kit119.28USD kit
Glucagon 1 mg/vial94.98USD vial
Glucagen 1 mg vial84.0USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-1.197Not Available
isoelectric point9.52Not Available

Taxonomy

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

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Peptide hormone binding
Specific Function
G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting gl...
Gene Name
GCGR
Uniprot ID
P47871
Uniprot Name
Glucagon receptor
Molecular Weight
54008.44 Da
References
  1. Katayama T, Shimamoto S, Oda H, Nakahara K, Kangawa K, Murakami N: Glucagon receptor expression and glucagon stimulation of ghrelin secretion in rat stomach. Biochem Biophys Res Commun. 2007 Jun 15;357(4):865-70. Epub 2007 Apr 9. [PubMed:17462598]
  2. Li P, Rogers T, Smiley D, DiMarchi RD, Zhang F: Design, synthesis and crystallization of a novel glucagon analog as a therapeutic agent. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2007 Jul 1;63(Pt 7):599-601. Epub 2007 Jun 15. [PubMed:17620721]
  3. Li XC, Zhuo JL: Targeting glucagon receptor signalling in treating metabolic syndrome and renal injury in Type 2 diabetes: theory versus promise. Clin Sci (Lond). 2007 Aug;113(4):183-93. [PubMed:17623014]
  4. Fischer AJ, Stanke JJ, Ghai K, Scott M, Omar G: Development of bullwhip neurons in the embryonic chicken retina. J Comp Neurol. 2007 Aug 1;503(4):538-49. [PubMed:17534934]
  5. Winzell MS, Brand CL, Wierup N, Sidelmann UG, Sundler F, Nishimura E, Ahren B: Glucagon receptor antagonism improves islet function in mice with insulin resistance induced by a high-fat diet. Diabetologia. 2007 Jul;50(7):1453-62. Epub 2007 May 4. [PubMed:17479245]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  7. Menzel S, Stoffel M, Espinosa R 3rd, Fernald AA, Le Beau MM, Bell GI: Localization of the glucagon receptor gene to human chromosome band 17q25. Genomics. 1994 Mar 15;20(2):327-8. [PubMed:8020989]
  8. Brubaker PL, Drucker DJ: Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels. 2002;8(3-4):179-88. [PubMed:12529935]
  9. Lok S, Kuijper JL, Jelinek LJ, Kramer JM, Whitmore TE, Sprecher CA, Mathewes S, Grant FJ, Biggs SH, Rosenberg GB, et al.: The human glucagon receptor encoding gene: structure, cDNA sequence and chromosomal localization. Gene. 1994 Mar 25;140(2):203-9. [PubMed:8144028]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Glucagon receptor activity
Specific Function
This is a receptor for glucagon-like peptide 2. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name
GLP2R
Uniprot ID
O95838
Uniprot Name
Glucagon-like peptide 2 receptor
Molecular Weight
63000.84 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Boushey RP, Yusta B, Drucker DJ: Glucagon-like peptide (GLP)-2 reduces chemotherapy-associated mortality and enhances cell survival in cells expressing a transfected GLP-2 receptor. Cancer Res. 2001 Jan 15;61(2):687-93. [PubMed:11212269]
  4. Munroe DG, Gupta AK, Kooshesh F, Vyas TB, Rizkalla G, Wang H, Demchyshyn L, Yang ZJ, Kamboj RK, Chen H, McCallum K, Sumner-Smith M, Drucker DJ, Crivici A: Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2. Proc Natl Acad Sci U S A. 1999 Feb 16;96(4):1569-73. [PubMed:9990065]
  5. Estall JL, Koehler JA, Yusta B, Drucker DJ: The glucagon-like peptide-2 receptor C terminus modulates beta-arrestin-2 association but is dispensable for ligand-induced desensitization, endocytosis, and G-protein-dependent effector activation. J Biol Chem. 2005 Jun 10;280(23):22124-34. Epub 2005 Apr 6. [PubMed:15817468]
  6. Brubaker PL, Drucker DJ: Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels. 2002;8(3-4):179-88. [PubMed:12529935]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transmembrane signaling receptor activity
Specific Function
This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name
GLP1R
Uniprot ID
P43220
Uniprot Name
Glucagon-like peptide 1 receptor
Molecular Weight
53025.22 Da
References
  1. Korner M, Stockli M, Waser B, Reubi JC: GLP-1 receptor expression in human tumors and human normal tissues: potential for in vivo targeting. J Nucl Med. 2007 May;48(5):736-43. [PubMed:17475961]
  2. Baggio LL, Drucker DJ: Biology of incretins: GLP-1 and GIP. Gastroenterology. 2007 May;132(6):2131-57. [PubMed:17498508]
  3. Fischer AJ, Stanke JJ, Ghai K, Scott M, Omar G: Development of bullwhip neurons in the embryonic chicken retina. J Comp Neurol. 2007 Aug 1;503(4):538-49. [PubMed:17534934]
  4. Brubaker PL, Drucker DJ: Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels. 2002;8(3-4):179-88. [PubMed:12529935]

Drug created on June 13, 2005 07:24 / Updated on December 14, 2018 14:19