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

Stem definition	Drug id	CAS RN
Glucagon-like Peptide (GLP) analogues	2994	9007-92-5

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
3	mg	N
1	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intentional overdose	103.15	20.86	63	3991	68054	56219959
Hypoglycaemia	101.20	20.86	58	3996	55757	56232256
Vasoplegia syndrome	87.05	20.86	20	4034	1305	56286708
Toxicity to various agents	71.14	20.86	84	3970	224480	56063533
Cardiogenic shock	55.75	20.86	26	4028	16299	56271714
Hypotension	54.69	20.86	78	3976	250430	56037583
Nasal discomfort	52.10	20.86	17	4037	4115	56283898
Shock	51.54	20.86	27	4027	21701	56266312
Circulatory collapse	49.77	20.86	26	4028	20777	56267236
Necrolytic migratory erythema	47.08	20.86	6	4048	6	56288007
Pulseless electrical activity	46.84	20.86	18	4036	7006	56281007
Cardiac arrest	46.55	20.86	43	4011	86271	56201742
Hypothermia	39.93	20.86	19	4035	12451	56275562
Bradycardia	39.06	20.86	35	4019	67469	56220544
Rhinalgia	38.08	20.86	10	4044	1135	56286878
Hypoglycaemic seizure	35.71	20.86	8	4046	465	56287548
Blood glucose decreased	34.97	20.86	20	4034	19067	56268946
Non-cardiogenic pulmonary oedema	33.43	20.86	8	4046	622	56287391
Overdose	32.41	20.86	39	4015	105791	56182222
Respiratory failure	32.39	20.86	37	4017	95025	56192988
Suicide attempt	31.52	20.86	29	4025	57807	56230206
Infective pulmonary exacerbation of cystic fibrosis	31.00	20.86	14	4040	8143	56279870
Hyperglycaemia	30.75	20.86	24	4030	38257	56249756
Haemodynamic instability	30.72	20.86	14	4040	8315	56279698
Atrioventricular block first degree	30.20	20.86	13	4041	6752	56281261
Distributive shock	29.07	20.86	8	4046	1083	56286930
Electrocardiogram U wave present	27.83	20.86	5	4049	93	56287920
Hypoxia	27.39	20.86	26	4028	53871	56234142
Diabetic ketoacidosis	27.34	20.86	17	4037	18854	56269159
Pulmonary oedema	26.62	20.86	25	4029	51118	56236895
CSF pressure increased	26.12	20.86	5	4049	133	56287880
Multiple organ dysfunction syndrome	25.95	20.86	25	4029	52745	56235268
Lactic acidosis	25.90	20.86	21	4033	35325	56252688
Multiple lentigines syndrome	25.44	20.86	5	4049	153	56287860
Diabetic retinal oedema	25.27	20.86	6	4048	451	56287562
Cytotoxic oedema	24.85	20.86	5	4049	173	56287840
Hyperdynamic left ventricle	24.85	20.86	5	4049	173	56287840
Cataract subcapsular	23.88	20.86	6	4048	571	56287442
Electrocardiogram P wave abnormal	23.86	20.86	5	4049	212	56287801
Blood glucose increased	23.50	20.86	28	4026	75123	56212890
Hyperlipidaemia	22.97	20.86	15	4039	18094	56269919
Mental status changes	22.78	20.86	20	4034	37481	56250532
Colour blindness	22.31	20.86	5	4049	291	56287722
Retinal ischaemia	21.59	20.86	5	4049	337	56287676
Electrocardiogram T wave amplitude decreased	21.41	20.86	5	4049	350	56287663
Episcleritis	20.89	20.86	6	4048	949	56287064

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypoglycaemia	111.11	24.51	71	3656	50875	31642742
Soft tissue mass	108.18	24.51	24	3703	810	31692807
Multimorbidity	105.31	24.51	23	3704	721	31692896
Oesophageal perforation	98.77	24.51	23	3704	967	31692650
Superinfection	84.87	24.51	24	3703	2194	31691423
Transplant failure	76.74	24.51	24	3703	3102	31690515
Hypotension	74.66	24.51	105	3622	204513	31489104
Intentional overdose	71.62	24.51	50	3677	41339	31652278
Lung consolidation	70.90	24.51	26	3701	5447	31688170
Inflammatory marker increased	69.90	24.51	24	3703	4154	31689463
Bradycardia	68.28	24.51	60	3667	69267	31624350
Oesophageal carcinoma	64.56	24.51	27	3700	8006	31685611
Cardiogenic shock	63.55	24.51	37	3690	22371	31671246
Immunosuppressant drug level increased	60.75	24.51	23	3704	5262	31688355
Vasoplegia syndrome	58.64	24.51	17	3710	1696	31691921
Rales	56.17	24.51	25	3702	8614	31685003
Haemoptysis	49.02	24.51	36	3691	32153	31661464
Myocardial ischaemia	48.51	24.51	28	3699	16639	31676978
Cardiomegaly	44.03	24.51	25	3702	14400	31679217
Compartment syndrome	43.34	24.51	15	3712	2656	31690961
Acute kidney injury	40.27	24.51	96	3631	279618	31413999
Coma scale abnormal	38.48	24.51	15	3712	3708	31689909
Non-cardiogenic pulmonary oedema	34.10	24.51	9	3718	634	31692983
Pulse absent	33.16	24.51	15	3712	5362	31688255
Drug level increased	31.67	24.51	23	3704	20163	31673454
Labelled drug-drug interaction medication error	30.23	24.51	19	3708	13144	31680473
Productive cough	28.96	24.51	27	3700	33513	31660104
Lower respiratory tract infection	28.86	24.51	25	3702	28212	31665405
Pulmonary vasculitis	28.62	24.51	7	3720	363	31693254
Ileus	25.43	24.51	18	3709	15151	31678466
Infective pulmonary exacerbation of cystic fibrosis	24.65	24.51	13	3714	6471	31687146
Toxicity to various agents	24.62	24.51	61	3666	181426	31512191

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypoglycaemia	174.48	18.75	112	7035	94252	70827045
Intentional overdose	170.15	18.75	112	7035	98323	70822974
Vasoplegia syndrome	144.18	18.75	38	7109	3118	70918179
Hypotension	119.13	18.75	173	6974	404208	70517089
Cardiogenic shock	117.36	18.75	62	7085	36245	70885052
Bradycardia	102.23	18.75	91	7056	124524	70796773
Soft tissue mass	100.11	18.75	23	7124	1065	70920232
Multimorbidity	92.99	18.75	22	7125	1159	70920138
Oesophageal perforation	90.16	18.75	22	7125	1322	70919975
Toxicity to various agents	83.89	18.75	143	7004	382029	70539268
Transplant failure	69.86	18.75	23	7124	4084	70917213
Superinfection	69.32	18.75	23	7124	4183	70917114
Cardiac arrest	64.62	18.75	80	7067	159754	70761543
Lung consolidation	64.22	18.75	26	7121	8280	70913017
Oesophageal carcinoma	61.20	18.75	26	7121	9340	70911957
Non-cardiogenic pulmonary oedema	60.12	18.75	16	7131	1361	70919936
Infective pulmonary exacerbation of cystic fibrosis	57.78	18.75	27	7120	12131	70909166
Overdose	53.20	18.75	75	7072	169670	70751627
Immunosuppressant drug level increased	51.83	18.75	22	7125	7885	70913412
Inflammatory marker increased	51.64	18.75	23	7124	9251	70912046
Suicide attempt	51.54	18.75	51	7096	79459	70841838
Acute kidney injury	49.32	18.75	131	7016	474493	70446804
Cardiomegaly	44.91	18.75	29	7118	24516	70896781
Lactic acidosis	44.55	18.75	43	7104	64981	70856316
Shock	44.42	18.75	35	7112	40390	70880907
Haemoptysis	42.95	18.75	38	7109	51414	70869883
Myocardial ischaemia	42.83	18.75	28	7119	24172	70897125
Compartment syndrome	41.54	18.75	16	7131	4470	70916827
Pulseless electrical activity	41.06	18.75	22	7125	13193	70908104
Rales	40.93	18.75	24	7123	17111	70904186
Hypoglycaemic seizure	38.52	18.75	10	7137	772	70920525
Cardiac dysfunction	34.12	18.75	13	7134	3524	70917773
Hypoxia	33.38	18.75	44	7103	93300	70827997
Coma scale abnormal	32.41	18.75	16	7131	8100	70913197
Respiratory failure	31.53	18.75	59	7088	168676	70752621
Circulatory collapse	31.21	18.75	27	7120	35447	70885850
Pulse absent	30.31	18.75	16	7131	9314	70911983
Hypoglycaemic unconsciousness	30.22	18.75	9	7138	1151	70920146
Hypothermia	29.71	18.75	21	7126	20573	70900724
Pulmonary vasculitis	27.69	18.75	7	7140	486	70920811
Blood glucose decreased	26.71	18.75	21	7126	24138	70897159
Diabetic ketoacidosis	25.75	18.75	23	7124	31489	70889808
Electrocardiogram U wave present	24.82	18.75	5	7142	123	70921174
Ileus	24.52	18.75	20	7127	24217	70897080
Distributive shock	24.41	18.75	9	7138	2228	70919069
Multiple lentigines syndrome	22.59	18.75	5	7142	195	70921102
Labelled drug-drug interaction medication error	22.52	18.75	19	7128	24108	70897189
Diabetic retinal oedema	22.51	18.75	6	7141	513	70920784
Productive cough	22.14	18.75	33	7114	78304	70842993
CSF pressure increased	21.94	18.75	5	7142	223	70921074
Mental status changes	21.40	18.75	29	7118	63072	70858225
Drug level increased	21.07	18.75	22	7125	36447	70884850
Rhinalgia	20.96	18.75	7	7140	1297	70920000
Neuritis	20.49	18.75	7	7140	1390	70919907
Necrolytic migratory erythema	20.45	18.75	3	7144	9	70921288
Electrocardiogram P wave abnormal	20.35	18.75	5	7142	309	70920988
Sepsis	19.95	18.75	62	7085	244483	70676814
Ascites	19.88	18.75	29	7118	67518	70853779
Rheumatoid arthritis	19.61	18.75	3	7144	291802	70629495
Cytotoxic oedema	19.49	18.75	5	7142	368	70920929
Hyperdynamic left ventricle	19.49	18.75	5	7142	368	70920929
Atrioventricular block first degree	19.42	18.75	13	7134	11660	70909637
Blood glucose increased	19.21	18.75	36	7111	102946	70818351
Metabolic acidosis	19.15	18.75	30	7117	74316	70846981
Colour blindness	19.10	18.75	5	7142	399	70920898
Cataract subcapsular	19.05	18.75	6	7141	925	70920372
Arthralgia	18.80	18.75	14	7133	503376	70417921

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Glucagon receptor	GPCR	P47871	GLR_HUMAN	AGONIST	EC50	9	IUPHAR	CHEMBL
Glucagon-like peptide 1 receptor	GPCR	P43220	GLP1R_HUMAN	AGONIST	Ki	7	IUPHAR
Glucagon receptor	GPCR		GLR_RAT		IC50	8.82	CHEMBL
Adenylate cyclase	Enzyme		D4A3N4_RAT ADCY3_RAT ADCY2_RAT ADCY4_RAT ADCY8_RAT ADCY6_RAT ADCY5_RAT Q8CFM9_RAT		EC50	8.23	CHEMBL
Glucagon-like peptide 1 receptor	GPCR		F8V479_MACFA		EC50	10.51	CHEMBL
Glucagon-like peptide 1 receptor	GPCR		GLP1R_MOUSE		EC50	10.36	CHEMBL

External reference:

ID	Source
D00116	KEGG_DRUG
16941-32-5	SECONDARY_CAS_RN
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

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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