glucagon
Approved
Nov 14, 1960
Glucagon is a polypeptide hormone identical to human glucagon that increases blood glucose and relaxes smooth muscle of the gastrointestinal tract. Glucagon is synthesized in a special non-pathogenic laboratory strain of Escherichia coli bacteria that has been genetically altered by the addition of the gene for glucagon. Glucagon generally elevates the concentration of glucose in the blood by promoting gluconeogenesis and glycogenolysis. Glucagon also decreases fatty acid synthesis in adipose tissue and the liver, as well as promoting lipolysis in these tissues, which causes them to release fatty acids into circulation where they can be catabolised to generate energy in tissues such as skeletal muscle when required. Glucose is stored in the liver in the form of the polysaccharide glycogen, which is a glucan (a polymer made up of glucose molecules). Liver cells (hepatocytes) have glucagon receptors. When glucagon binds to the glucagon receptors, the liver cells convert the glycogen into individual glucose molecules and release them into the bloodstream, in a process known as glycogenolysis. As these stores become depleted, glucagon then encourages the liver and kidney to synthesize additional glucose by gluconeogenesis. Glucagon turns off glycolysis in the liver, causing glycolytic intermediates to be shuttled to gluconeogenesis. Glucagon also regulates the rate of glucose production through lipolysis. Glucagon induces lipolysis in humans under conditions of insulin suppression (such as diabetes mellitus type 1). Glucagon increases blood glucose concentration and is used in the treatment of hypoglycemia. Glucagon administered through a parenteral route relaxes smooth muscle of the stomach, duodenum, small bowel, and colon. Glucagon is also indicated as a diagnostic aid in the radiologic examination of the stomach, duodenum, small bowel, and colon when diminished intestinal motility would be advantageous. — NCATS
Clinical trial activity
126 trials · 87 clinical orgs · 9 marketing orgs
Earliest trial started Oct 1, 1999 (NCT00005889)
Timeline
1990s
- Jun 22, 1998
Novo Nordisk — NDA Secondary Org
2000s
2010s
- May 8, 2015
Fresenius — NDA Secondary Org
- Jul 24, 2019
Eli Lilly — NDA Secondary Org
- Sep 10, 2019
Xeris Pharmaceuticals — Marketing Organization
- Sep 10, 2019
Xeris Pharmaceuticals — NDA Secondary Org
2020s
- Dec 28, 2020
Amphastar Pharmaceuticals — Marketing Organization
- Dec 12, 2024
Mylan — Marketing Organization
- Jul 22, 2025
Lupin — Marketing Organization
- Sep 15, 2025
Cipla — Marketing Organization
Indications
Approved for
Studied for
- Anesthesia and Analgesia · Phase 4
- Bariatric Surgery · Phase 4
- Colonic Neoplasms · Phase 4
- Common Cold · Phase 1
- Congenital Hyperinsulinism · Phase 2
- Diabetes Mellitus · Phase 4
- Diabetes Mellitus, Type 1 · Phase 4
- Diabetes Mellitus, Type 2 · Phase 4
- Drug Overdose · Phase 4
- Fatty Liver · Phase 1
- Fertilization in Vitro · Phase 4
- Glucagon · Phase 1
- Healthy Volunteers · Phase 3
- Hyperinsulinism · Phase 1
- Hypoglycemia · Phase 4
- Hypopituitarism · Phase 4
- Insulin Resistance · Phase 1
- Insulin Secretion · Phase 1
- Liver Diseases · Phase 4
- Non-alcoholic Fatty Liver Disease · Phase 1
- Obesity · Phase 4
- Pharmacology · Phase 3
- Prediabetic State · Phase 1
Mechanism of action
- Glucagon receptorAGONIST
GCGR agonist
Approval history
- approvedPriority reviewNov 14, 1960
Chemistry & pharmacology
SMILES
CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O- Mol. weight
- 3482.8 g/mol
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Prescription Only
Oral
No
Parenteral
Yes
Topical
No
Sources
- WikipediaGlucagon ↗
- NCATS76LA80IG2G ↗
- ChEMBLCHEMBL266481 ↗
- ChEMBLCHEMBL5314342 ↗
- ChEMBLCHEMBL1201508 ↗
- ChEMBLCHEMBL1201618 ↗
- ChEMBLCHEMBL5314341 ↗
Also known as
- biod-961
- glucagen
- glucagen
- glucagen
- glucagen hypokit
- glucagon
- glucagon
- glucagon
- glucagon
- glucagon
- glucagon
- glucagon
- glucagon
- glucagone
- glucagone
- glucagon emergency kit
- glucagon hcl
- glucagon hcl
- glucagon, human
- glucagon hydrochloride
- glucagon hydrochloride
- glucagon hydrochloride
- glucagon hydrochloride recombinant
- glucagon hydrochloride recombinant
- glucagon hydrochloride recombinant
- glucagon hydrochloride recombinant
- glucagon hydrochloride recombinant
- glucagonoid
- glucagon, porcine
- glucagon recombinant
- glucagon recombinant
- glucagon recombinant
- glucagon recombinant
- glucagon recombinant
- glucagon (recombinant dna origin)
- glucagonum
- glucagonum
- glukagon
- hyperglycemic-glycogenolytic factor
- ly900018
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06872060 | N/A | Jun 1, 2026 | University of Copenhagen |
| NCT07300982 | Phase 1/Phase 2 (Phase 2) | Apr 30, 2026 | Duke University, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) |
| NCT07246421 | N/A | Jan 1, 2026 | Aarhus University, Novo Nordisk |
| NCT07212868 | Phase 1 | Dec 1, 2025 | National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), University of Texas, San Antonio |
| NCT06921824 | N/A | Apr 30, 2025 | University Hospital Bispebjerg and Frederiksberg, University of Copenhagen |
| NCT06558422 | Phase 1 | Dec 1, 2024 | Columbia University, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), University of California, Berkeley |
| NCT06685146 | N/A | Nov 30, 2024 | University Hospital Bispebjerg and Frederiksberg, University of Copenhagen |
| NCT06986603 | Phase 4 | Nov 26, 2024 | Joslin Diabetes Center, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), University of Alabama, Birmingham, University of Virginia |
| NCT06424106 | N/A | Oct 1, 2024 | Mayo Clinic |
| NCT06588504 | Phase 1 | Sep 10, 2024 | Novo Nordisk |
| NCT06498063 | N/A | Feb 20, 2024 | Novo Nordisk, The Augustinus Foundation, Denmark., University of Copenhagen |
| NCT06126354 | Phase 1 | Dec 1, 2023 | Columbia University, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), Yeshiva University |
| NCT05724134 | Phase 1 | Aug 29, 2023 | Columbia University, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), Yeshiva University |
| NCT05960565 | Phase 2 | Jun 20, 2023 | Norwegian University of Science and Technology |
| NCT05454709 | Phase 2 | Jun 1, 2023 | Inreda Diabetic B.V., Medisch Spectrum Twente |
| NCT05379686 | N/A | Sep 30, 2022 | Steno Diabetes Center Copenhagen |
| NCT04992312 | Phase 1 | Dec 6, 2021 | Eli Lilly |
| NCT05076292 | N/A | Oct 31, 2021 | Steno Diabetes Center Copenhagen |
| NCT05206149 | Phase 4 | Oct 1, 2021 | University of Turin |
| NCT04949867 | Phase 4 | May 20, 2021 | Steno Diabetes Center Copenhagen, Technical University of Denmark, University of Copenhagen |
Organizations
Research & Development (87)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Xeris Pharmaceuticals | For profit | 17 | 13 | 3 | 2013 |
| Eli Lilly | For profit | 16 | 14 | 3 | 2011 |
| National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) | Government | 15 | 0 | 4 | 2013 |
| University of Copenhagen | Academic/Hospital | 14 | 11 | 2 | 2014 |
| University of Montreal | Academic/Hospital | 9 | 9 | 1 | 2013 |
| Novo Nordisk | For profit | 7 | 2 | 3 | 2012 |
| Profil GmbH | For profit | 7 | 1 | 2 | 2009 |
| Zealand Pharma | For profit | 7 | 7 | 3 | 2014 |
| Harvard University | Academic/Hospital | 6 | 4 | 3 | 2014 |
| Steno Diabetes Center Copenhagen | Academic/Hospital | 6 | 5 | 2 | 2018 |
| Oregon Health and Science University | Academic/Hospital | 5 | 1 | 3 | 2008 |
| Baylor University | Academic/Hospital | 4 | 1 | 3 | 1999 |
| Jaeb Center for Health Research | Academic/Hospital | 4 | 4 | 2 | 2013 |
| Juvenile Diabetes Research Foundation | Academic/Hospital | 4 | 0 | 2 | 2008 |
| Locemia Solutions ULC | For profit | 4 | 0 | 1 | 2011 |
| Columbia University | Academic/Hospital | 3 | 3 | 1 | 2023 |
| Emissary International LLC | For profit | 3 | 0 | 1 | 2013 |
| Joslin Diabetes Center | Academic/Hospital | 3 | 2 | 2 | 2016 |
| Legacy Health System | Academic/Hospital | 3 | 3 | 2 | 2008 |
| Sanofi | For profit | 3 | 3 | 1 | 2015 |
Marketing (12)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Amphastar Pharmaceuticals | For profit | MKTG | Dec 28, 2020 |
| Athenex, Inc. | For profit | MKTG | — |
| Cipla | For profit | MKTG | Sep 15, 2025 |
| Eli Lilly | For profit | NDA | Nov 14, 1960 |
| Eli Lilly | For profit | NDA2 | Jul 24, 2019 |
| Fresenius | For profit | NDA2 | May 8, 2015 |
| Lupin | For profit | MKTG | Jul 22, 2025 |
| Lupin | For profit | SYN | Jul 22, 2025 |
| Mylan | For profit | MKTG | Dec 12, 2024 |
| Novo Nordisk | For profit | NDA2 | Jun 22, 1998 |
| Xeris Pharmaceuticals | For profit | MKTG | Sep 10, 2019 |
| Xeris Pharmaceuticals | For profit | NDA2 | Sep 10, 2019 |