Identification
- Summary
Dasiglucagon is a glucagon analog used to treat severe hypoglycemia in pediatric and adult patients with diabetes.
- Brand Names
- Zegalogue
- Generic Name
- Dasiglucagon
- DrugBank Accession Number
- DB15226
- Background
Dasiglucagon is a glucagon analog that acts to increase blood sugar levels.5 It consists of 29 amino acids similar to endogenous glucagon; however, it contains seven substituted amino acids for improved physical and chemical stability in its drug formulation.6 In March 2021, the FDA approved dasiglucagon to treat severe hypoglycemia in patients six years and older with diabetes. It is available as a subcutaneous injection marketed as ZEGALOGUE.5
Severe hypoglycemia is an acute, life-threatening medical condition resulting from a profound drop in blood glucose levels. It is characterized by neurological impairment, with manifestations like loss of consciousness and seizure. Hypoglycemia is a common side effect of antidiabetic treatments, most notably insulin and sulfonylureas. Although it tends to be more common in type 1 diabetes mellitus, occurring in about 22% to 46% of patients annually, about 7% to 25% of patients with type 2 diabetes mellitus treated with insulin experience severe hypoglycemia a year.6 Even with close monitoring of blood glucose levels, it is not always possible to prevent severe hypoglycemic events in patients with diabetes, and children are particularly at risk for experiencing severe hypoglycemia.7 Treatments for severe hypoglycemia have mostly been limited to intravenous dextrose and different glucagon formulations.6 The approval of dasiglucagon marks the first glucagon analog approved for severe hypoglycemia treatment that does not require administration by a healthcare professional.6
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Chemical Formula
- C152H222N38O50
- Protein Average Weight
- 3382.0 Da (anhydrous, free-base form)
- Sequences
- Not Available
- Synonyms
- Dasiglucagon
Pharmacology
- Indication
Dasiglucagon is an antihypoglycemic agent indicated for the treatment of severe hypoglycemia in pediatric and adult patients with diabetes aged 6 years and above.5
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Severe hypoglycemia •••••••••••• •••••••• ••••••••• - Contraindications & Blackbox Warnings
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Dasiglucagon works to increase blood glucose levels under normal and hypoglycemic conditions.2 After administration of dasiglucagon in adult patients with type 1 diabetes, the mean glucose increase from baseline at 90 minutes was 168 mg/dL. In pediatric patients with type 1 diabetes aged seven to 17 years, the mean glucose increase at 60 minutes after administration of dasiglucagon was 162 mg/dL.5
- Mechanism of action
Dasiglucagon is an analog of glucagon, which is a peptide hormone responsible for increasing blood glucose levels. It has the same mechanism of action as endogenous glucagon by acting as an agonist at glucagon receptors, which are G-coupled receptors expressed throughout the body. Dasiglucagon binds to glucagon receptors in the liver, which activates Gsα and Gq, and consequently, adenylate cyclase. Adenyl cyclase increases intracellular cyclic AMP, which stimulates glycogenolysis and glucogenesis in the liver.3,4 As glucose is primarily released from liver glycogen stores, hepatic stores of glycogen are crucial for dasiglucagon to exert its antihypoglycemic effects.5
Target Actions Organism AGlucagon receptor agonistHumans - Absorption
Following subcutaneous administration of 0.6 mg dasiglucagon, the mean peak plasma concentration was 5110 pg/mL (1510 pmol/L). Tmax was 35 minutes. In pediatric patients with type 1 diabetes, the mean peak plasma concentration of 3920 pg/mL occurred at around 21 minutes.5 Dasiglucagon has a higher absorption rate than traditional reconstituted glucagon.2
- Volume of distribution
The mean apparent volume of distribution ranged from 47 L to 57 L after subcutaneous administration.5
- Protein binding
Not Available
- Metabolism
Like endogenous glucagon, dasiglucagon undergoes proteolytic degradation pathways in blood, liver, and kidney.5
- Route of elimination
Not Available
- Half-life
The half-life was approximately 30 minutes following subcutaneous administration.5 Dasiglucagon has a longer plasma elimination half-life than traditional reconstituted glucagon.2
- Clearance
Not Available
- Adverse Effects
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Overdose may be characterized by nausea, vomiting, inhibition of gastrointestinal tract motility, increased blood pressure, and elevated heart rate. In case of a suspected overdose, serum potassium may decrease so monitoring and correcting of potassium levels may be warranted. A marked increase in blood pressure may be managed by the short-term use of phentolamine mesylate. Appropriate supportive treatment should be initiated.5
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbaloparatide Abaloparatide may increase the hypotensive activities of Dasiglucagon. Acebutolol Acebutolol may increase the hypotensive activities of Dasiglucagon. Aceclofenac The therapeutic efficacy of Dasiglucagon can be decreased when used in combination with Aceclofenac. Acemetacin The therapeutic efficacy of Dasiglucagon can be decreased when used in combination with Acemetacin. Acetylsalicylic acid Acetylsalicylic acid may decrease the antihypertensive activities of Dasiglucagon. - Food Interactions
- No interactions found.
Products
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Ingredient UNII CAS InChI Key Dasiglucagon hydrochloride YQX12245A9 Not Available Not applicable - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Zegalogue Injection, solution 0.6 mg/0.6mL Subcutaneous Zealand Pharma US, Inc 2021-04-05 Not applicable US 
Zegalogue Injection, solution 0.6 mg/0.6mL Subcutaneous Novo Nordisk 2023-06-26 Not applicable US Zegalogue Injection, solution 0.6 mg/0.6mL Subcutaneous Zealand Pharma US, Inc 2021-04-05 Not applicable US Zegalogue Injection, solution 0.6 mg/0.6mL Subcutaneous Novo Nordisk 2023-06-26 Not applicable US
Categories
- ATC Codes
- H04AA02 — Dasiglucagon
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antihypertensive Agents
- Antihypoglycemic Agent
- Glucagon Receptor Agonists
- Glycogenolytic Hormones
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Increased Glycogenolysis
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- Proglucagon
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- AD4J2O47FQ
- CAS number
- 1544300-84-6
References
- General References
- Battelino T, Tehranchi R, Bailey T, Dovc K, Melgaard A, Yager Stone J, Woerner S, von dem Berge T, DiMeglio L, Danne T: Dasiglucagon, a next-generation ready-to-use glucagon analog, for treatment of severe hypoglycemia in children and adolescents with type 1 diabetes: Results of a phase 3, randomized controlled trial. Pediatr Diabetes. 2021 Aug;22(5):734-741. doi: 10.1111/pedi.13220. Epub 2021 Jun 9. [Article]
- Xu B, Tang G, Chen Z: Dasiglucagon: an effective medicine for severe hypoglycemia. Eur J Clin Pharmacol. 2021 Dec;77(12):1783-1790. doi: 10.1007/s00228-021-03183-0. Epub 2021 Jul 5. [Article]
- Jiang G, Zhang BB: Glucagon and regulation of glucose metabolism. Am J Physiol Endocrinol Metab. 2003 Apr;284(4):E671-8. [Article]
- Morris CH, Baker J: Glucagon . [Article]
- FDA Approved Drug Products: ZEGALOGUE (dasiglucagon) injection, for subcutaneous use (March 2021) [Link]
- FDA Center for Drug Evaluation and Research: Summary Review for Dasiglucagon [Link]
- GlobeNewsWire: Zealand Pharma Announces FDA Approval of Zegalogue® (dasiglucagon) injection, for the Treatment of Severe Hypoglycemia in People with Diabetes [Link]
- External Links
- 2535233
- Wikipedia
- Dasiglucagon
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Active Not Recruiting Treatment Congenital Hyperinsulinism (CHI) 1 3 Completed Treatment Congenital Hyperinsulinism (CHI) 1 3 Completed Treatment Hypoglycemia 1 3 Completed Treatment Hypoglycemia / Type 1 Diabetes Mellitus 4 3 Recruiting Treatment Hypoglycemia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Subcutaneous 0.6 mg/0.6mL - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US10442847 No 2019-10-15 2035-02-03 US US11795204 No 2014-01-06 2034-01-06 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Peptide hormone binding
- Specific Function
- G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting gl...
- Gene Name
- GCGR
- Uniprot ID
- P47871
- Uniprot Name
- Glucagon receptor
- Molecular Weight
- 54008.44 Da
References
- Battelino T, Tehranchi R, Bailey T, Dovc K, Melgaard A, Yager Stone J, Woerner S, von dem Berge T, DiMeglio L, Danne T: Dasiglucagon, a next-generation ready-to-use glucagon analog, for treatment of severe hypoglycemia in children and adolescents with type 1 diabetes: Results of a phase 3, randomized controlled trial. Pediatr Diabetes. 2021 Aug;22(5):734-741. doi: 10.1111/pedi.13220. Epub 2021 Jun 9. [Article]
- FDA Approved Drug Products: ZEGALOGUE (dasiglucagon) injection, for subcutaneous use (March 2021) [Link]
- FDA Center for Drug Evaluation and Research: Summary Review for Dasiglucagon [Link]
Drug created at May 20, 2019 15:01 / Updated at November 21, 2021 16:25