glucagon 🐶 Veterinary Use | 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:

  • ogluo
  • 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:
  • LIPINSKI: 3
  • HAC: 92
  • HDO: 55
  • TPSA: 1538.74
  • ALOGS: -4.71
  • ROTB: 113

Drug dosage:

DoseUnitRoute
3 mg N
1 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 25, 2020 PMDA Eli Lilly Japan K.K.
Feb. 2, 2021 EMA XERIS PHARMACEUTICALS IRELAND LIMITED
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
Intentional overdose 92.07 21.53 58 3801 62446 50538819
Vasoplegia syndrome 62.72 21.53 15 3844 1099 50600166
Hypoglycaemia 60.14 21.53 42 3817 53539 50547726
Shock 51.39 21.53 27 3832 20623 50580642
Nasal discomfort 48.08 21.53 16 3843 3888 50597377
Necrolytic migratory erythema 46.74 21.53 6 3853 6 50601259
Cardiogenic shock 46.38 21.53 23 3836 15576 50585689
Pulseless electrical activity 46.30 21.53 18 3841 6823 50594442
Hypotension 40.83 21.53 68 3791 235401 50365864
Toxicity to various agents 40.41 21.53 64 3795 212435 50388830
Hypothermia 39.56 21.53 19 3840 11997 50589268
Rhinalgia 38.60 21.53 10 3849 1016 50600249
Cardiac arrest 38.13 21.53 39 3820 83612 50517653
Hypoglycaemic seizure 35.39 21.53 8 3851 457 50600808
Non-cardiogenic pulmonary oedema 33.62 21.53 8 3851 573 50600692
Circulatory collapse 33.04 21.53 20 3839 19980 50581285
Bradycardia 32.97 21.53 32 3827 64394 50536871
Suicide attempt 32.88 21.53 29 3830 51703 50549562
Distributive shock 30.69 21.53 8 3851 832 50600433
Atrioventricular block first degree 30.57 21.53 13 3846 6188 50595077
Haemodynamic instability 30.46 21.53 14 3845 8010 50593255
Respiratory failure 30.26 21.53 36 3823 91145 50510120
Overdose 29.26 21.53 37 3822 99690 50501575
Hyperglycaemia 28.46 21.53 23 3836 36382 50564883
Electrocardiogram U wave present 27.80 21.53 5 3854 88 50601177
Infective pulmonary exacerbation of cystic fibrosis 27.54 21.53 13 3846 7896 50593369
Diabetic ketoacidosis 27.30 21.53 17 3842 17855 50583410
Diabetic retinal oedema 26.95 21.53 6 3853 320 50600945
Pulmonary oedema 26.34 21.53 25 3834 48913 50552352
Cytotoxic oedema 26.05 21.53 5 3854 127 50601138
CSF pressure increased 26.02 21.53 5 3854 128 50601137
Lactic acidosis 25.92 21.53 21 3838 33334 50567931
Multiple organ dysfunction syndrome 25.74 21.53 25 3834 50312 50550953
Hypoxia 25.41 21.53 25 3834 51098 50550167
Hyperdynamic left ventricle 25.38 21.53 5 3854 146 50601119
Multiple lentigines syndrome 25.16 21.53 5 3854 153 50601112
Blood glucose decreased 24.52 21.53 16 3843 18195 50583070
Electrocardiogram P wave abnormal 23.74 21.53 5 3854 205 50601060
Cataract subcapsular 23.67 21.53 6 3853 559 50600706
Blood glucose increased 23.39 21.53 28 3831 71296 50529969
Hyperlipidaemia 22.66 21.53 15 3844 17475 50583790
Mental status changes 22.37 21.53 20 3839 36252 50565013
Colour blindness 22.18 21.53 5 3854 282 50600983
Episcleritis 21.59 21.53 6 3853 795 50600470
Retinal ischaemia 21.56 21.53 5 3854 320 50600945

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
Soft tissue mass 77.39 24.25 17 3069 619 29570822
Hypotension 76.06 24.25 97 2989 194257 29377184
Multimorbidity 74.04 24.25 16 3070 539 29570902
Intentional overdose 72.89 24.25 47 3039 38481 29532960
Oesophageal perforation 69.14 24.25 16 3070 739 29570702
Hypoglycaemia 63.23 24.25 47 3039 48299 29523142
Bradycardia 58.57 24.25 51 3035 65578 29505863
Superinfection 58.05 24.25 17 3069 1984 29569457
Oesophageal carcinoma 55.36 24.25 20 3066 4527 29566914
Transplant failure 52.09 24.25 17 3069 2839 29568602
Lung consolidation 49.73 24.25 19 3067 5024 29566417
Inflammatory marker increased 47.92 24.25 17 3069 3650 29567791
Cardiogenic shock 45.34 24.25 27 3059 19163 29552278
Vasoplegia syndrome 44.57 24.25 13 3073 1495 29569946
Immunosuppressant drug level increased 40.08 24.25 16 3070 4749 29566692
Rales 39.25 24.25 18 3068 7492 29563949
Non-cardiogenic pulmonary oedema 35.40 24.25 9 3077 618 29570823
Acute kidney injury 34.12 24.25 81 3005 265186 29306255
Myocardial ischaemia 33.87 24.25 21 3065 16007 29555434
Compartment syndrome 30.65 24.25 11 3075 2441 29569000
Cardiomegaly 28.98 24.25 18 3068 13758 29557683
Haemoptysis 27.71 24.25 24 3062 30526 29540915
Coma scale abnormal 26.94 24.25 11 3075 3458 29567983
Depressed mood 26.06 24.25 18 3068 16430 29555011

FDA Adverse Event Reporting System (Geriatric)

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
Intentional overdose 161.16 18.92 104 6286 89840 64402502
Hypotension 108.56 18.92 159 6231 380815 64111527
Vasoplegia syndrome 106.52 18.92 29 6361 2738 64489604
Hypoglycaemia 100.54 18.92 78 6312 89814 64402528
Bradycardia 85.79 18.92 80 6310 118139 64374203
Cardiogenic shock 85.17 18.92 48 6342 32379 64459963
Soft tissue mass 72.20 18.92 17 6373 892 64491450
Multimorbidity 65.28 18.92 16 6374 996 64491346
Oesophageal perforation 64.83 18.92 16 6374 1025 64491317
Non-cardiogenic pulmonary oedema 61.21 18.92 16 6374 1292 64491050
Suicide attempt 57.22 18.92 51 6339 70956 64421386
Oesophageal carcinoma 55.52 18.92 20 6370 4723 64487619
Cardiac arrest 53.65 18.92 71 6319 153993 64338349
Infective pulmonary exacerbation of cystic fibrosis 52.79 18.92 25 6365 11771 64480571
Transplant failure 48.20 18.92 17 6373 3777 64488565
Superinfection 47.80 18.92 17 6373 3869 64488473
Lung consolidation 45.98 18.92 20 6370 7738 64484604
Shock 44.47 18.92 34 6356 38206 64454136
Pulseless electrical activity 42.18 18.92 22 6368 12717 64479625
Toxicity to various agents 41.60 18.92 103 6287 363410 64128932
Lactic acidosis 39.63 18.92 39 6351 61371 64430971
Hypoglycaemic seizure 38.87 18.92 10 6380 758 64491584
Acute kidney injury 38.11 18.92 114 6276 449126 64043216
Inflammatory marker increased 35.04 18.92 17 6373 8434 64483908
Immunosuppressant drug level increased 34.37 18.92 16 6374 7243 64485099
Respiratory failure 32.92 18.92 58 6332 161125 64331217
Cardiomegaly 31.88 18.92 23 6367 23661 64468681
Overdose 30.77 18.92 56 6334 159510 64332832
Hypothermia 30.72 18.92 21 6369 19835 64472507
Compartment syndrome 28.68 18.92 12 6378 4220 64488122
Hypoxia 28.17 18.92 39 6351 88110 64404232
Rales 28.15 18.92 18 6372 15211 64477131
Myocardial ischaemia 27.74 18.92 21 6369 23230 64469112
Diabetic ketoacidosis 27.17 18.92 23 6367 29822 64462520
Distributive shock 26.12 18.92 9 6381 1866 64490476
Electrocardiogram U wave present 25.14 18.92 5 6385 117 64492225
Diabetic retinal oedema 25.01 18.92 6 6384 341 64492001
Haemoptysis 24.20 18.92 27 6363 49021 64443321
Multiple lentigines syndrome 22.68 18.92 5 6385 195 64492147
Mental status changes 22.51 18.92 29 6361 61133 64431209
CSF pressure increased 22.13 18.92 5 6385 218 64492124
Hypoglycaemic unconsciousness 22.12 18.92 7 6383 1114 64491228
Coma scale abnormal 21.73 18.92 12 6378 7762 64484580
Rhinalgia 21.72 18.92 7 6383 1181 64491161
Circulatory collapse 20.96 18.92 21 6369 33711 64458631
Blood glucose increased 20.92 18.92 36 6354 98037 64394305
Hyperdynamic left ventricle 20.81 18.92 5 6385 286 64492056
Electrocardiogram P wave abnormal 20.73 18.92 5 6385 291 64492051
Atrioventricular block first degree 20.62 18.92 13 6377 10721 64481621
Metabolic acidosis 20.60 18.92 30 6360 70928 64421414
Necrolytic migratory erythema 20.50 18.92 3 6387 9 64492333
Cytotoxic oedema 20.31 18.92 5 6385 317 64492025
Pulse absent 20.16 18.92 12 6378 8934 64483408
Episcleritis 19.74 18.92 6 6384 836 64491506
Cataract subcapsular 19.42 18.92 6 6384 883 64491459
Colour blindness 19.34 18.92 5 6385 386 64491956
Haemodynamic instability 18.97 18.92 14 6376 14898 64477444

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypoglycemic disorder indication 237630007
Severe hypoglycaemia in patients with diabetes indication 237633009
Gastrointestinal Radiography Adjunct indication
Diabetes mellitus contraindication 73211009 DOID:9351
Insulinoma contraindication 302822000 DOID:3892
Glucagonoma contraindication 302823005
Pheochromocytoma contraindication 302835009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
Glucagon-like peptide 1 receptor GPCR EC50 10.51 CHEMBL
Glucagon-like peptide 1 receptor GPCR EC50 10.36 CHEMBL

External reference:

IDSource
D00116 KEGG_DRUG
19179-82-9 SECONDARY_CAS_RN
4017456 VANDF
C0017687 UMLSCUI
CHEBI:5391 CHEBI
CHEMBL1201618 ChEMBL_ID
CHEMBL266481 ChEMBL_ID
D005934 MESH_DESCRIPTOR_UI
DB00040 DRUGBANK_ID
1136 IUPHAR_LIGAND_ID
933 INN_ID
76LA80IG2G UNII
16132283 PUBCHEM_CID
151823 RXNORM
14121 MMSL
4785 MMSL
585 MMSL
8000 MMSL
d00593 MMSL
002065 NDDF
007100 NDDF
10712001 SNOMEDCT_US
427742003 SNOMEDCT_US
66603002 SNOMEDCT_US
16941-32-5 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Baqsimi HUMAN PRESCRIPTION DRUG LABEL 1 0002-6145 POWDER 3 mg NASAL NDA 27 sections
GlucaGen HUMAN PRESCRIPTION DRUG LABEL 1 0597-0053 INJECTION, POWDER, FOR SOLUTION 1 mg SUBCUTANEOUS NDA 24 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 63323-596 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS NDA 23 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 63323-596 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS NDA 23 sections
Glucagon HUMAN PRESCRIPTION DRUG LABEL 1 63323-596 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS NDA 23 sections
Gvoke HypoPen 0.5 mg Auto-Injector HUMAN PRESCRIPTION DRUG LABEL 1 72065-120 INJECTION, SOLUTION 0.50 mg SUBCUTANEOUS NDA 20 sections
Gvoke HypoPen 1 mg Auto-Injector HUMAN PRESCRIPTION DRUG LABEL 1 72065-121 INJECTION, SOLUTION 1 mg SUBCUTANEOUS NDA 20 sections
Gvoke PFS0.5 mg Pre-filled Syringe HUMAN PRESCRIPTION DRUG LABEL 1 72065-130 INJECTION, SOLUTION 0.50 mg SUBCUTANEOUS NDA 20 sections
Gvoke PFS1 mg Pre-filled Syringe HUMAN PRESCRIPTION DRUG LABEL 1 72065-131 INJECTION, SOLUTION 1 mg SUBCUTANEOUS NDA 20 sections
Gvoke Kit HUMAN PRESCRIPTION DRUG LABEL 1 72065-140 INJECTION, SOLUTION 1 mg SUBCUTANEOUS NDA 20 sections
Gvoke KitVial HUMAN PRESCRIPTION DRUG LABEL 1 72065-141 INJECTION, SOLUTION 1 mg SUBCUTANEOUS NDA 20 sections