DASIGLUCAGON

Description
Sources: https://pubmed.ncbi.nlm.nih.gov/34047955|https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214231s000lbl.pdf

Dasiglucagon (Zegalogue®) is an antihypoglycaemic agent being developed by Zealand Pharma for the treatment of hypoglycaemia, type 1 diabetes mellitus (T1DM) management and congenital hyperinsulinism. Dasiglucagon is a glucagon receptor agonist, which increases blood glucose concentration by activating hepatic glucagon receptors, thereby stimulating glycogen breakdown and release of glucose from the liver. Hepatic stores of glycogen are necessary for dasiglucagon to produce an antihypoglycemic effect. In March 2021, dasiglucagon received its first approval in the USA for the treatment of severe hypoglycaemia in paediatric and adult patients with diabetes aged 6 years and above. Dasiglucagon, a glucagon analogue, is available as a single-dose autoinjector or prefilled syringe for subcutaneous injection.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glucagon receptor 6 Target ID: CHEMBL1985 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214231s000lbl.pdf	Agonist 2752		9.9 pM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypoglycemia 7 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214231s000lbl.pdf	Primary		Approved 8583	ZEGALOGUE Approved Use Indicated for the treatment of severe hypoglycemia in pediatric and adult patients with diabetes aged 6 years and above. Launch Date 2021

C_max

Value	Dose	Analyte	Population
5107 pg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=7	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.51 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=12 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.16 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=12 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=29	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN
0.334 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.1 mg single, subcutaneous dose: 0.1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.976 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.3 mg single, subcutaneous dose: 0.3 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.57 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2.8 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	1 mg single, subcutaneous dose: 1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
2.61 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=12 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.92 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=12 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=29	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN
0.451 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.1 mg single, subcutaneous dose: 0.1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.36 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.3 mg single, subcutaneous dose: 0.3 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2.64 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
4.81 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	1 mg single, subcutaneous dose: 1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
30 min OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=7	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
28.5 min OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=12 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
37.4 min OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=12 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=29	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN
0.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.1 mg single, subcutaneous dose: 0.1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.625 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.3 mg single, subcutaneous dose: 0.3 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.583 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	0.6 mg single, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.625 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=20	1 mg single, subcutaneous dose: 1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	DASIGLUCAGON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
0.6 mg single, subcutaneous Dose: 0.6 mg Route: subcutaneous Route: single Dose: 0.6 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000MedR.pdf	Other AEs: Adverse event... Other AEs: Adverse event Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000MedR.pdf

AEs

AE	Significance	Dose	Population
Adverse event		0.6 mg single, subcutaneous Dose: 0.6 mg Route: subcutaneous Route: single Dose: 0.6 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000MedR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252	inhibitor 2438	inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C19 2057 CYP1A2 2153

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no [IC50 >25 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no [IC50 >25 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no [IC50 >25 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no [IC50 >25 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214231Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no [IC50 >25 uM]

PubMed

Title	Date	PubMed
Dasiglucagon: A Novel Ready-to-Use Treatment for Severe Hypoglycemia.	2023-03	35861467
Dasiglucagon for treating severe hypoglycemia in patients with diabetes.	2022-07	35848442
Dasiglucagon: an effective medicine for severe hypoglycemia.	2021-12	34223944
Dasiglucagon: First Approval.	2021-06	34047955

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose of ZEGALOGUE in adults and pediatric patients aged 6 years and older is 0.6 mg administered by subcutaneous injection into the lower abdomen, buttocks, thigh, or outer upper arm. If there has been no response after 15 minutes, an additional 0.6 mg dose of ZEGALOGUE from a new device may be administered.

Route of Administration: Subcutaneous

In Vitro Use Guide

In vitro Study 13-149 showed that dasiglucagon does not significantly inhibit CYPs 1A2, 2C9, 2C19, 2D6, and 3A4 isozymes in human liver microsomes with all IC50 values > 25 uM.

Substance Class	Protein Created by `admin` on `Tue Apr 01 19:40:42 GMT 2025` Edited by `admin` on `Tue Apr 01 19:40:42 GMT 2025`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	AD4J2O47FQ
Record Status	`FAILED`
Record Version

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Name

Type

Language

dasiglucagon [INN]

Preferred Name

English

DASIGLUCAGON

Official Name

English

DASIGLUCAGON [USAN]

Common Name

English

Dasiglucagon [WHO-DD]

Common Name

English

(16-(2-METHYLALANINE)(S>X),17-L-ALANINE(R>A),20-L-.ALPHA.-GLUTAMYL(Q>E),21-L-.ALPHA.- GLUTAMYL(D>E),24-L-LYSYL(Q>K),27-L-.ALPHA.-GLUTAMYL(M>E),28-L-SERINE(N>S))HUMAN GLUCAGON

Systematic Name

English

ZP-4207

Code

English

L-THREONINE, L-HISTIDYL-L-SERYL-L-GLUTAMINYLGLYCYL-L-THREONYL-L-PHENYLALANYL-L-THREONYL-L-SERYL-L-.ALPHA.-ASPARTYL-L-TYROSYL-L-SERYL-L-LYSYL-L-TYROSYL-L-LEUCYL-L-.ALPHA.-ASPARTYL-2-METHYLALANYL-L-ALANYL-L-ARGINYL-L-ALANYL-L-.ALPHA.-GLUTAMYL-L-.ALPHA.-GLU

Systematic Name

English

ZP-GA-1

Code

English

HIS-SER-GLN-GLY-THR-PHE-THR-SER-ASP-TYR-SER-LYS-TYR-LEU-ASP-AIB-ALA-ARG-ALA-GLU-GLU-PHE-VAL-LYS-TRP-LEU-GLU-SER-THR

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

569416