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

Stem definitionDrug idCAS RN
glucagon-like peptide (GLP) analogues and agonists 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 111.91 19.78 67 4243 74085 63410627
Vasoplegia syndrome 63.06 19.78 16 4294 1683 63483029
Hypoglycaemia 62.55 19.78 43 4267 60022 63424690
Hypotension 60.56 19.78 83 4227 272521 63212191
Toxicity to various agents 55.98 19.78 76 4234 247174 63237538
Nasal discomfort 54.72 19.78 18 4292 4742 63479970
Shock 53.94 19.78 28 4282 23435 63461277
Cardiogenic shock 48.83 19.78 24 4286 17908 63466804
Bradycardia 48.52 19.78 40 4270 73187 63411525
Necrolytic migratory erythema 47.43 19.78 6 4304 6 63484706
Pulseless electrical activity 46.67 19.78 18 4292 7503 63477209
Cardiac arrest 44.23 19.78 42 4268 92503 63392209
Hypothermia 42.50 19.78 20 4290 13561 63471151
Suicide attempt 41.87 19.78 34 4276 60884 63423828
Circulatory collapse 41.50 19.78 23 4287 21915 63462797
Rhinalgia 39.93 19.78 11 4299 1588 63483124
Hypoglycaemic seizure 35.87 19.78 8 4302 484 63484228
Overdose 34.91 19.78 41 4269 115037 63369675
Haemodynamic instability 33.35 19.78 15 4295 9175 63475537
Non-cardiogenic pulmonary oedema 32.72 19.78 8 4302 723 63483989
Infective pulmonary exacerbation of cystic fibrosis 30.75 19.78 14 4296 8803 63475909
Respiratory failure 30.41 19.78 36 4274 101822 63382890
Atrioventricular block first degree 30.03 19.78 13 4297 7260 63477452
Pulmonary oedema 28.30 19.78 26 4284 54847 63429865
Hyperglycaemia 27.98 19.78 23 4287 41844 63442868
Electrocardiogram U wave present 27.97 19.78 5 4305 96 63484616
Distributive shock 27.66 19.78 8 4302 1375 63483337
Multiple organ dysfunction syndrome 27.55 19.78 26 4284 56726 63427986
Diabetic retinal oedema 27.53 19.78 6 4304 326 63484386
Blood glucose increased 27.34 19.78 31 4279 83725 63400987
Diabetic ketoacidosis 26.96 19.78 17 4293 20488 63464224
Blood glucose decreased 26.63 19.78 17 4293 20935 63463777
Hypoxia 26.40 19.78 26 4284 59766 63424946
CSF pressure increased 26.10 19.78 5 4305 142 63484570
Multiple lentigines syndrome 25.74 19.78 5 4305 153 63484559
Lactic acidosis 25.52 19.78 21 4289 38266 63446446
Hyperdynamic left ventricle 24.92 19.78 5 4305 181 63484531
Cytotoxic oedema 24.74 19.78 5 4305 188 63484524
Cataract subcapsular 24.02 19.78 6 4304 592 63484120
Electrocardiogram P wave abnormal 23.80 19.78 5 4305 228 63484484
Mental status changes 22.86 19.78 20 4290 39579 63445133
Hyperlipidaemia 22.71 19.78 15 4295 19556 63465156
Metabolic acidosis 22.55 19.78 21 4289 45048 63439664
Colour blindness 22.20 19.78 5 4305 316 63484396
Retinal ischaemia 21.69 19.78 5 4305 351 63484361
Electrocardiogram T wave amplitude decreased 21.38 19.78 5 4305 374 63484338
Episcleritis 20.96 19.78 6 4304 994 63483718

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 134.92 24.73 30 4219 989 34951693
Multimorbidity 131.71 24.73 29 4220 913 34951769
Oesophageal perforation 124.75 24.73 29 4220 1170 34951512
Superinfection 107.95 24.73 30 4219 2489 34950193
Hypoglycaemia 101.98 24.73 70 4179 54570 34898112
Transplant failure 97.76 24.73 30 4219 3523 34949159
Lung consolidation 90.19 24.73 32 4217 5904 34946778
Hypotension 88.75 24.73 121 4128 221528 34731154
Inflammatory marker increased 87.52 24.73 30 4219 4998 34947684
Bradycardia 81.91 24.73 70 4179 75348 34877334
Oesophageal carcinoma 79.58 24.73 33 4216 9271 34943411
Immunosuppressant drug level increased 78.37 24.73 29 4220 6026 34946656
Haemoptysis 72.79 24.73 48 4201 34958 34917724
Rales 71.08 24.73 31 4218 9852 34942830
Intentional overdose 63.21 24.73 48 4201 43626 34909056
Myocardial ischaemia 62.65 24.73 34 4215 17374 34935308
Acute kidney injury 62.47 24.73 123 4126 304865 34647817
Cardiomegaly 57.92 24.73 31 4218 15407 34937275
Vasoplegia syndrome 56.74 24.73 17 4232 1839 34950843
Pulmonary vasculitis 54.50 24.73 13 4236 586 34952096
Neuritis 48.76 24.73 13 4236 921 34951761
Labelled drug-drug interaction medication error 42.44 24.73 25 4224 14914 34937768
Cardiogenic shock 42.38 24.73 31 4218 26587 34926095
Compartment syndrome 41.06 24.73 15 4234 3003 34949679
Respiratory symptom 40.36 24.73 13 4236 1784 34950898
Lower respiratory tract infection 37.63 24.73 31 4218 31606 34921076
Coma scale abnormal 36.92 24.73 15 4234 3993 34948689
Productive cough 36.74 24.73 33 4216 37780 34914902
Drug level increased 35.77 24.73 26 4223 22070 34930612
Non-cardiogenic pulmonary oedema 33.56 24.73 9 4240 652 34952030
Pulse absent 31.59 24.73 15 4234 5788 34946894
Ascites 30.93 24.73 33 4216 46538 34906144
Neurological symptom 29.66 24.73 13 4236 4172 34948510
Sleep disorder due to a general medical condition 26.91 24.73 13 4236 5208 34947474

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 169.01 19.01 114 7791 105846 79630637
Hypotension 140.48 19.01 194 7711 440123 79296360
Hypoglycaemia 140.14 19.01 100 7805 101494 79634989
Soft tissue mass 128.52 19.01 29 7876 1259 79735224
Bradycardia 126.91 19.01 106 7799 135451 79601032
Vasoplegia syndrome 121.08 19.01 34 7871 3596 79732887
Multimorbidity 120.02 19.01 28 7877 1411 79735072
Oesophageal perforation 117.58 19.01 28 7877 1543 79734940
Transplant failure 91.68 19.01 29 7876 4612 79731871
Superinfection 90.12 19.01 29 7876 4873 79731610
Cardiogenic shock 88.81 19.01 54 7851 41860 79694623
Lung consolidation 83.69 19.01 32 7873 8915 79727568
Acute kidney injury 78.29 19.01 164 7741 519240 79217243
Oesophageal carcinoma 77.05 19.01 32 7873 11052 79725431
Immunosuppressant drug level increased 69.35 19.01 28 7877 8999 79727484
Inflammatory marker increased 67.95 19.01 29 7876 10711 79725772
Haemoptysis 65.58 19.01 50 7855 55949 79680534
Cardiac arrest 64.07 19.01 82 7823 172014 79564469
Suicide attempt 59.81 19.01 56 7849 82876 79653607
Non-cardiogenic pulmonary oedema 59.03 19.01 16 7889 1483 79735000
Toxicity to various agents 58.69 19.01 129 7776 421411 79315072
Cardiomegaly 58.51 19.01 35 7870 26317 79710166
Myocardial ischaemia 56.93 19.01 34 7871 25485 79710998
Infective pulmonary exacerbation of cystic fibrosis 56.77 19.01 27 7878 12824 79723659
Pulmonary vasculitis 54.03 19.01 13 7892 748 79735735
Rales 53.54 19.01 30 7875 19971 79716512
Neuritis 43.24 19.01 13 7892 1745 79734738
Hypoglycaemic seizure 43.02 19.01 11 7894 813 79735670
Shock 42.63 19.01 35 7870 43513 79692970
Lactic acidosis 42.27 19.01 43 7862 70316 79666167
Coma scale abnormal 40.69 19.01 19 7886 8659 79727824
Pulseless electrical activity 39.97 19.01 22 7883 14138 79722345
Compartment syndrome 39.85 19.01 16 7889 5066 79731417
Respiratory depression 37.56 19.01 27 7878 27603 79708880
Respiratory symptom 33.86 19.01 14 7891 4777 79731706
Labelled drug-drug interaction medication error 33.04 19.01 25 7880 27625 79708858
Hypoxia 31.95 19.01 45 7860 103198 79633285
Hypothermia 30.40 19.01 22 7883 22724 79713759
Coma 29.87 19.01 43 7862 100606 79635877
Overdose 29.75 19.01 60 7845 184146 79552337
Productive cough 29.58 19.01 40 7865 88291 79648192
Pulse absent 29.35 19.01 16 7889 10087 79726396
Respiratory failure 28.11 19.01 58 7847 180853 79555630
Ascites 28.06 19.01 36 7869 75526 79660957
Metabolic acidosis 27.07 19.01 37 7868 82492 79653991
Distributive shock 26.53 19.01 10 7895 2677 79733806
Hypoglycaemic unconsciousness 25.90 19.01 8 7897 1175 79735308
Drug level increased 25.21 19.01 25 7880 39626 79696857
Diabetic retinal oedema 24.80 19.01 6 7899 353 79736130
Electrocardiogram U wave present 24.63 19.01 5 7900 130 79736353
Diabetic ketoacidosis 24.50 19.01 23 7882 34099 79702384
Circulatory collapse 24.41 19.01 24 7881 37644 79698839
Sepsis 24.27 19.01 70 7835 269358 79467125
Hyperdynamic left ventricle 24.11 19.01 6 7899 397 79736086
Ileus 23.44 19.01 20 7885 26191 79710292
Pleural effusion 23.07 19.01 47 7858 145215 79591268
Neurological symptom 23.03 19.01 13 7892 8770 79727713
Multiple lentigines syndrome 22.67 19.01 5 7900 195 79736288
Arthralgia 21.85 19.01 15 7890 571788 79164695
CSF pressure increased 21.39 19.01 5 7900 254 79736229
Necrolytic migratory erythema 20.50 19.01 3 7902 9 79736474
Rhinalgia 20.47 19.01 8 7897 2359 79734124
Mental status changes 20.43 19.01 29 7876 66930 79669553
Pruritus 20.14 19.01 7 7898 394641 79341842
Pulmonary alveolar haemorrhage 19.83 19.01 13 7892 11444 79725039
Rhabdomyolysis 19.58 19.01 36 7869 103095 79633388
Electrocardiogram P wave abnormal 19.53 19.01 5 7900 371 79736112
Cytotoxic oedema 19.26 19.01 5 7900 392 79736091
Haemodynamic instability 19.19 19.01 15 7890 17367 79719116

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 | Suggest Off label Use Form| |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 11590205 April 22, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA
0.5MG/0.1ML (0.5MG/0.1ML) GVOKE PFS XERIS N212097 Sept. 10, 2019 DISCN SOLUTION SUBCUTANEOUS 11590205 April 22, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA
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 DISCN 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 11590205 April 22, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA
1MG/0.2ML (1MG/0.2ML) GVOKE KIT XERIS N212097 Aug. 20, 2021 RX SOLUTION SUBCUTANEOUS 11590205 April 22, 2036 TREATMENT OF SEVERE HYPOGLYCEMIA
1MG/0.2ML (1MG/0.2ML) GVOKE PFS XERIS N212097 Sept. 10, 2019 RX SOLUTION SUBCUTANEOUS 11590205 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)

None

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
Glucocorticoid receptor Nuclear hormone receptor EC50 10.70 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
Glucagon receptor GPCR IC50 8.82 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 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 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 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 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 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
Gvoke KitVial HUMAN PRESCRIPTION DRUG LABEL 1 72065-141 INJECTION, SOLUTION 1 mg SUBCUTANEOUS NDA 20 sections