Glucagon

Summary

Glucagon (CHEMBL5314341) is an approved protein (ATC H04AA01) targeting GLP1R and GCGR; indicated across 9 conditions including hypoglycemia and diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: H04AA01
• Targets: 2 (GLP1R, GCGR)
• Indications: 9 conditions
• Clinical trials: 95

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5314341
Name	Glucagon
Type	Protein
Max phase	4
ATC	H04AA01

Also known as: Baqsimi, Glucagon, Glucagon (recombinant dna origin), Glucagon recombinant, human, pig, porcine, Gvoke hypopen, Gvoke kit, Ogluo, glucagon, HSQGTFTSDYSKYLDSRRAQDFVQWLMNT

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
GLP1R	GLP-1 receptor	Full agonist	7	0.2%	P43220
GCGR	glucagon receptor	Full agonist	9	0.2%	P47871

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Glucagon-like peptide 1 receptor, Glucagon-like peptide 1 receptor, Glucagon receptor, Glucocorticoid receptor, Adenylate cyclase, Glucagon receptor, Glucagon receptor.

Bioactivity

ChEMBL activities: 32 potent at pChembl ≥ 5 of 32 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q61606	10.7	EC50	0.02	nM	CHEMBL_ACT_18568482
NR3C1	10.7	EC50	0.02	nM	CHEMBL_ACT_24514224
GCGR	10.67	EC50	0.02	nM	CHEMBL_ACT_19444575
NR3C1	10.52	EC50	0.03	nM	CHEMBL_ACT_24514204
GLP1R	10.36	EC50	0.04	nM	CHEMBL_ACT_18240472
O35659	10.36	EC50	0.04	nM	CHEMBL_ACT_18240526
GLP1R	10.36	EC50	0.04	nM	CHEMBL_ACT_18300862
GLP1R	10.24	EC50	0.06	nM	CHEMBL_ACT_24783670
GCGR	10.22	EC50	0.06	nM	CHEMBL_ACT_18240545
GCGR	10.22	EC50	0.06	nM	CHEMBL_ACT_29103846
GCGR	10.15	EC50	0.07	nM	CHEMBL_ACT_3421636
GCGR	10.1	EC50	0.08	nM	CHEMBL_ACT_24959223
GCGR	10.04	EC50	0.09	nM	CHEMBL_ACT_25940367
Q61606	9.47	EC50	0.34	nM	CHEMBL_ACT_25045467
GCGR	9.3	EC50	0.5	nM	CHEMBL_ACT_18568476
GCGR	9.01	EC50	0.97	nM	CHEMBL_ACT_18312856
P30082	8.82	IC50	1.5	nM	CHEMBL_ACT_1157821
P30082	8.82	IC50	1.5	nM	CHEMBL_ACT_518642
P30082	8.82	IC50	1.5	nM	CHEMBL_ACT_678868
P30082	8.82	IC50	1.5	nM	CHEMBL_ACT_894514
P30082	8.82	IC50	1.5	nM	CHEMBL_ACT_907796
O35659	8.59	EC50	2.6	nM	CHEMBL_ACT_18568484
GLP1R	8.48	EC50	3.3	nM	CHEMBL_ACT_3421667
GLP1R	8.43	EC50	3.74	nM	CHEMBL_ACT_18240543
GLP1R	8.42	EC50	3.8	nM	CHEMBL_ACT_24959187
P30082	8.3	EC50	5	nM	CHEMBL_ACT_907797
P21932	8.23	EC50	5.9	nM	CHEMBL_ACT_1157825
P21932	8.23	EC50	5.9	nM	CHEMBL_ACT_678870
GLP1R	8.11	EC50	7.7	nM	CHEMBL_ACT_18312884
P21932	8.1	EC50	8	nM	CHEMBL_ACT_1157824

Target pathways

Aggregated over 2 target gene(s): GLP1R, GCGR.

Top Reactome pathways

5 total, by targets touching each:

Pathway	Targets	Genes
G alpha (s) signalling events	2	GCGR, GLP1R
Glucagon-type ligand receptors	2	GCGR, GLP1R
Glucagon signaling in metabolic regulation	1	GCGR
Glucagon-like Peptide-1 (GLP1) regulates insulin secretion	1	GLP1R
G alpha (q) signalling events	1	GCGR

Dominant GO biological processes

GO term	Targets
cell surface receptor signaling pathway	2
adenylate cyclase-activating G protein-coupled receptor signaling pathway	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
cellular response to glucagon stimulus	2
activation of adenylate cyclase activity	1
positive regulation of cytosolic calcium ion concentration	1
learning or memory	1
regulation of heart contraction	1
post-translational protein targeting to membrane, translocation	1
negative regulation of blood pressure	1
positive regulation of blood pressure	1
hormone secretion	1
response to psychosocial stress	1
regulation of biological quality	1

Indications & clinical

Indications

9 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
hypoglycemia	4	MONDO:0004946	HP:0001943
diabetes mellitus	4	MONDO:0005015	EFO:0000400
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
obesity disorder	2	MONDO:0011122	EFO:0001073
hyperinsulinemic hypoglycemia	2	MONDO:0005803	EFO:0007318
common cold	1	MONDO:0005709	EFO:0007214
type 2 diabetes mellitus	1	MONDO:0005148	MONDO:0005148
short bowel syndrome	1	MONDO:0015183	MONDO:0015183

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 95.

Phase distribution

Phase	Trials
PHASE1	30
Not specified	26
PHASE2	12
PHASE4	11
PHASE3	9
PHASE2/PHASE3	3
PHASE1/PHASE2	2
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07427251	PHASE4	NOT_YET_RECRUITING	The Postprandial Hypo-Avoid Study
NCT00155376	PHASE4	UNKNOWN	Intravenous-Morphine and Glucagon-Usage Enhanced MR Cholangiography
NCT01155206	PHASE4	COMPLETED	Acute Regulation of Intestinal and Hepatic Lipoprotein Production by Glucagon
NCT01674283	PHASE4	WITHDRAWN	Effect of Glucagon on Uterine Contractility at the Time of Embryo Transfer in in Vitro Fertilization
NCT02078726	PHASE4	COMPLETED	Glucagon Use in Colonoscopies
NCT02232971	PHASE4	UNKNOWN	Treatment of Low Blood Sugar With Glucagon Among Patients With Type 1 Diabetes
NCT02516150	PHASE4	COMPLETED	Effect of Ethanol Intoxication on the Anti-Hypoglycemic Action of Glucagon
NCT03533179	PHASE4	COMPLETED	Glucagon’s Cardiovascular Effects With and Without Beta-blocker-induced Cardioinhibition
NCT04053712	PHASE4	COMPLETED	Dual-hormone Closed-loop Glucose Control in Type 1 Diabetes
NCT04307797	PHASE4	COMPLETED	Effect of Glucagon and Glucagon-like Peptide-1 Co-agonism on Cardiac Function and Metabolism in Overweight Participants with Type 2 Diabetes
NCT04949867	PHASE4	COMPLETED	Dual-Hormone Closed-Loop Glucose Control in Adolescents With Type 1 Diabetes
NCT00206258	PHASE3	COMPLETED	The Role of Amylin and Glucagon in T1DM
NCT00929812	PHASE3	UNKNOWN	Glucagon Modulation of Ghrelin Secretion
NCT01994746	PHASE3	COMPLETED	Efficacy and Safety of Nasal Glucagon for Treatment of Hypoglycemia in Adults
NCT01997411	PHASE2/PHASE3	COMPLETED	Assessment of Intranasal Glucagon in Children and Adolescents With Type 1 Diabetes
NCT02018627	PHASE2/PHASE3	COMPLETED	Equivalence of A Stable Liquid Glucagon Formulation With Freshly Reconstituted Lyophilized Glucagon
NCT02171130	PHASE3	COMPLETED	Clinical Usability of Intranasal Glucagon in Treatment of Hypoglycemia
NCT02402933	PHASE3	COMPLETED	Clinical Usability of Nasal Glucagon in Treatment of Hypoglycemia in Children and Adolescents
NCT03091673	PHASE3	COMPLETED	Glucose Response of G-Pen (Glucagon Injection) in Pediatric T1D Patients
NCT03421379	PHASE3	COMPLETED	A Study of Nasal Glucagon (LY900018) in Japanese Participants With Diabetes Mellitus
NCT03439072	PHASE3	COMPLETED	G-Pen™ Compared to Lilly Glucagon for Hypoglycemia Rescue in Adults With Type 1 Diabetes
NCT03650582	PHASE2/PHASE3	UNKNOWN	Intranasal Glucagon and Energy Balance
NCT03738865	PHASE3	COMPLETED	G-Pen Compared to Glucagen Hypokit for Severe Hypoglycemia Rescue in Adults With Type 1 Diabetes
NCT07300982	PHASE1/PHASE2	NOT_YET_RECRUITING	Studies of Insulin and Glucagon Action in the Liver
NCT00434772	PHASE2	COMPLETED	Glucagon in the Treatment of Hypoglycemia in Newborn Infants of Diabetic Mothers
NCT00797823	PHASE2	COMPLETED	Sensor-Augmented Insulin Delivery: Insulin Plus Glucagon Versus Insulin Alone
NCT01828125	PHASE2	WITHDRAWN	Efficacy of Small Subcutaneous Glucagon Dose to Treat Hypoglycemia in Adults With Type 1 Diabetes
NCT02423980	PHASE2	COMPLETED	G-Pen™ for Hypoglycemia Rescue in T1D Patients
NCT02490098	PHASE2	WITHDRAWN	Closed-loop Control of Postprandial Glucose Levels in Children and Adults With Type 1 Diabetes
NCT02626936	PHASE2	COMPLETED	Safety of Overestimation of a Meal Insulin Bolus in the Context of Dual-hormone Closed-loop Operation
NCT02798250	PHASE2	COMPLETED	Safety of Overestimation of a Meal Insulin Bolus in the Context of Dual-hormone Closed-loop Operation - Part 2
NCT02846857	PHASE2	WITHDRAWN	Closed-loop Control of Glucose Levels (Artificial Pancreas) for 15 Weeks in Adolescents and Adults With Type 1 Diabetes
NCT02937558	PHASE2	COMPLETED	CSI-Glucagon for Prevention of Hypoglycemia in Children With Congenital Hyperinsulinism
NCT02971228	PHASE2	COMPLETED	Feasibility Trial Testing the Bionic Pancreas With ZP4207
NCT03255629	PHASE1/PHASE2	COMPLETED	Closed-Loop Glucagon Pump for Treatment of Post-Bariatric Hypoglycemia
NCT03490942	PHASE2	TERMINATED	Glucagon Infusion in T1D Patients With Recurrent Severe Hypoglycemia: Effects on Counter-Regulatory Responses
NCT05960565	PHASE2	TERMINATED	Glucagon Enhanced Insulin Absorption in Diabetes Mellitus Type 1
NCT02817659	PHASE1	ACTIVE_NOT_RECRUITING	To Determine Tolerability to Glucagon Infusion in Obese Subjects
NCT03139305	PHASE1	ACTIVE_NOT_RECRUITING	Effect of Prolonged (72 Hour) Glucagon Administration on Energy Expenditure in Healthy Obese Subjects
NCT03241706	PHASE1	ACTIVE_NOT_RECRUITING	Liver Glycogen and Hypoglycemia in Humans

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

40 molecules share ≥1 primary target. Top 40 by shared-target count:

Molecule	Source	Status	Shared targets
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	GCGR, GLP1R
COTADUTIDE	ChEMBL	Phase 2	GCGR, GLP1R
PF-06291874	ChEMBL	Phase 2	GCGR, GLP1R
LIRAGLUTIDE	ChEMBL + PubChem	Phase 4 (approved)	GLP1R
ELAGOLIX	ChEMBL	Phase 4 (approved)	GLP1R
EXENATIDE	ChEMBL	Phase 4 (approved)	GLP1R
LOPERAMIDE	ChEMBL	Phase 4 (approved)	GLP1R
PERPHENAZINE	ChEMBL	Phase 4 (approved)	GLP1R
SECRETIN	ChEMBL	Phase 4 (approved)	GLP1R
SEMAGLUTIDE	ChEMBL	Phase 4 (approved)	GLP1R
TIRZEPATIDE	ChEMBL	Phase 4 (approved)	GLP1R
TOLVAPTAN	ChEMBL	Phase 4 (approved)	GLP1R
ORFORGLIPRON	ChEMBL	Phase 3	GLP1R
ADOMEGLIVANT	ChEMBL	Phase 2	GCGR
DANUGLIPRON	ChEMBL	Phase 2	GLP1R
DEVAZEPIDE	ChEMBL	Phase 2	GLP1R
GLP-1	ChEMBL	Phase 2	GLP1R
LOTIGLIPRON	ChEMBL	Phase 2	GLP1R
MK-0893	ChEMBL	Phase 2	GCGR
MK-3577	ChEMBL	Phase 2	GCGR
Aclidinium Bromide	PubChem	Approved	GCGR
Acyclovir	PubChem	Approved	GCGR
Allopurinol	PubChem	Approved	GCGR
Alogliptin	PubChem	Approved	GCGR
Bosentan	PubChem	Approved	GCGR
Clozapine	PubChem	Approved	GCGR
Crizotinib	PubChem	Approved	GCGR
Desloratadine	PubChem	Approved	GCGR
Ethambutol	PubChem	Approved	GCGR
Fidaxomicin	PubChem	Approved	GCGR
Methotrexate	PubChem	Approved	GCGR
Olanzapine	PubChem	Approved	GCGR
Olmesartan Medoxomil	PubChem	Approved	GCGR
Propoxyphene	PubChem	Approved	GCGR
Pyrazinamide	PubChem	Approved	GCGR
rifampin	PubChem	Approved	GCGR
Sildenafil	PubChem	Approved	GCGR
Tegaserod	PubChem	Approved	GCGR
Tiotropium Bromide Monohydrate	PubChem	Approved	GCGR
Valacyclovir	PubChem	Approved	GCGR