glucagon Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Glucagon-like Peptide (GLP) analogues 2994 9007-92-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • glucagon hydrochloride recombinant
  • glucagen
  • glucagon
  • glucagonoid
  • glukagon
  • hyperglycemic-glycogenolytic factor
  • glucagon hydrochloride
  • glucagon HCl
  • glucagon recombinant
A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511)
  • Molecular weight: 3482.80
  • Formula: C153H225N43O49S
  • CLOGP: 0
  • LIPINSKI: 3
  • HAC: 92
  • HDO: 55
  • TPSA: 1538.74
  • ALOGS: -4.71
  • ROTB: 113

Drug dosage:

DoseUnitRoute
1 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 14, 1960 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Necrolytic migratory erythema 51.10 47.84 5 74 10 2357996

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypotension 63.42 44.59 18 60 29636 1717067

Pharmacologic Action:

SourceCodeDescription
ATC H04AA01 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
PANCREATIC HORMONES
GLYCOGENOLYTIC HORMONES
Glycogenolytic hormones
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D006728 Hormones
FDA EPC N0000190852 Antihypoglycemic Agent
FDA EPC N0000190853 Gastrointestinal Motility Inhibitor
FDA PE N0000009340 Increased Gluconeogenesis
FDA PE N0000009345 Increased Glycogenolysis
FDA PE N0000008636 Decreased GI Smooth Muscle Tone
FDA PE N0000008635 Decreased GI Motility
FDA PE N0000008652 Decreased Glycolysis

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypoglycemic disorder indication 237630007
Gastrointestinal Radiography Adjunct indication
Diabetes mellitus contraindication 73211009 DOID:9351
Insulinoma contraindication 302822000 DOID:3892
Glucagonoma contraindication 302823005
Pheochromocytoma contraindication 302835009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.12 acidic
pKa2 3.31 acidic
pKa3 3.79 acidic
pKa4 4.27 acidic
pKa5 9.35 acidic
pKa6 9.95 acidic
pKa7 11.89 acidic
pKa8 11.98 acidic
pKa9 12.35 acidic
pKa10 12.43 acidic
pKa11 12.5 acidic
pKa12 12.59 acidic
pKa13 12.81 acidic
pKa14 12.81 acidic
pKa15 12.95 acidic
pKa16 13.03 acidic
pKa17 13.17 acidic
pKa18 13.33 acidic
pKa19 13.38 acidic
pKa20 13.39 acidic
pKa21 13.41 acidic
pKa22 13.65 acidic
pKa23 13.7 acidic
pKa24 13.74 acidic
pKa25 13.89 acidic
pKa26 13.97 acidic
pKa27 11.27 Basic
pKa28 10.75 Basic
pKa29 10.29 Basic
pKa30 7.99 Basic
pKa31 5.98 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
3MG BAQSIMI ELI LILLY AND CO N210134 July 24, 2019 RX POWDER NASAL 10213487 Feb. 16, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA IN PATIENTS WITH DIABETES
0.5MG/0.1ML (0.5MG/0.1ML) GVOKE HYPOPEN XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS 9649364 April 22, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA
0.5MG/0.1ML (0.5MG/0.1ML) GVOKE PFS XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS 9649364 April 22, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA
1MG/0.2ML (1MG/0.2ML) GVOKE HYPOPEN XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS 9649364 April 22, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA
1MG/0.2ML (1MG/0.2ML) GVOKE PFS XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS 9649364 April 22, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
3MG BAQSIMI ELI LILLY AND CO N210134 July 24, 2019 RX POWDER NASAL July 24, 2022 NEW PRODUCT
0.5MG/0.1ML (0.5MG/0.1ML) GVOKE HYPOPEN XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS Sept. 10, 2022 NEW PRODUCT
0.5MG/0.1ML (0.5MG/0.1ML) GVOKE PFS XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS Sept. 10, 2022 NEW PRODUCT
1MG/0.2ML (1MG/0.2ML) GVOKE HYPOPEN XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS Sept. 10, 2022 NEW PRODUCT
1MG/0.2ML (1MG/0.2ML) GVOKE PFS XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS Sept. 10, 2022 NEW PRODUCT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glucagon receptor GPCR AGONIST EC50 9 IUPHAR CHEMBL
Glucagon-like peptide 1 receptor GPCR AGONIST Ki 7 IUPHAR
Glucagon receptor GPCR IC50 8.82 CHEMBL
Adenylate cyclase Enzyme EC50 8.23 CHEMBL

External reference:

IDSource
D005934 MESH_DESCRIPTOR_UI
C0591569 UMLSCUI
D00116 KEGG_DRUG
1H87NVF4DB UNII
19179-82-9 SECONDARY_CAS_RN
933 INN_ID
10712001 SNOMEDCT_US
585 MMSL
4832 RXNORM
66603002 SNOMEDCT_US
4785 MMSL
d00593 MMSL
4017456 VANDF
002065 NDDF
CHEMBL266481 ChEMBL_ID
DB00040 DRUGBANK_ID
CHEBI:5391 CHEBI
CHEMBL1201508 ChEMBL_ID
CHEMBL1201618 ChEMBL_ID
16132283 PUBCHEM_CID
1136 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Baqsimi HUMAN PRESCRIPTION DRUG LABEL 1 0002-6145 POWDER 3 mg NASAL NDA 18 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 0002-8031 KIT 1 mg None NDA 14 sections
GlucaGen HypoKit HUMAN PRESCRIPTION DRUG LABEL 1 0169-7065 KIT 1 mg None NDA 17 sections
GlucaGen HUMAN PRESCRIPTION DRUG LABEL 1 0597-0053 INJECTION, POWDER, FOR SOLUTION 1 mg SUBCUTANEOUS NDA 16 sections
GlucaGen HUMAN PRESCRIPTION DRUG LABEL 1 0597-0260 KIT 1 mg None NDA 16 sections
GLUCAG0N HUMAN PRESCRIPTION DRUG LABEL 1 51662-1323 KIT 1 mg INTRAVENOUS NDA 14 sections
GLUCAGON HUMAN PRESCRIPTION DRUG LABEL 1 51662-1498 KIT 1 mg INTRAMUSCULAR NDA 18 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 54868-5070 KIT 1 mg None NDA 14 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 63323-582 KIT 1 mg None NDA 18 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 63323-593 KIT 1 mg None NDA 16 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 63323-594 KIT 1 mg None NDA 16 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 63323-596 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAMUSCULAR NDA 16 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 64725-8031 KIT 1 mg None NDA 13 sections
Gvoke HypoPen HUMAN PRESCRIPTION DRUG LABEL 1 72065-120 INJECTION, SOLUTION 0.50 mg SUBCUTANEOUS NDA 17 sections
Gvoke HypoPen HUMAN PRESCRIPTION DRUG LABEL 1 72065-121 INJECTION, SOLUTION 1 mg SUBCUTANEOUS NDA 17 sections
Gvoke PFS HUMAN PRESCRIPTION DRUG LABEL 1 72065-130 INJECTION, SOLUTION 0.50 mg SUBCUTANEOUS NDA 17 sections
Gvoke PFS HUMAN PRESCRIPTION DRUG LABEL 1 72065-131 INJECTION, SOLUTION 1 mg SUBCUTANEOUS NDA 17 sections