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Dasiglucagon

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Also known as: 1544300-84-6, Dasiglucagon [inn], Dasiglucagon [usan], Dasiglucagon [who-dd], Dasiglucagon [usan:inn], Unii-ad4j2o47fq

Molecular Formula

C₁₅₂H₂₂₂N₃₈O₅₀

Molecular Weight

3381.6 g/mol

InChI Key

RZRMFQMNPDPAIX-AJTOSFMRSA-N

Dasiglucagon is a glucagon analog that acts to increase blood sugar levels. 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. 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. 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. 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. Treatments for severe hypoglycemia have mostly been limited to intravenous dextrose and different glucagon formulations. The approval of dasiglucagon marks the first glucagon analog approved for severe hypoglycemia treatment that does not require administration by a healthcare professional.

1 2D Structure

Dasiglucagon

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-2-methylpropanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-carboxy-1-[[(2S)-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid

2.1.2 InChI

InChI=1S/C152H222N38O50/c1-73(2)55-99(133(222)171-98(47-51-116(206)207)132(221)183-111(71-194)144(233)189-122(80(11)197)149(238)239)174-137(226)105(61-85-65-161-91-32-21-20-31-89(85)91)178-129(218)93(34-23-25-53-154)172-146(235)119(75(5)6)187-139(228)103(57-81-27-16-14-17-28-81)176-131(220)97(46-50-115(204)205)170-130(219)96(45-49-114(202)203)167-123(212)76(7)164-127(216)94(35-26-54-160-151(157)158)166-124(213)77(8)165-150(240)152(12,13)190-145(234)107(64-118(210)211)180-134(223)100(56-74(3)4)173-135(224)101(59-83-36-40-87(198)41-37-83)175-128(217)92(33-22-24-52-153)168-142(231)109(69-192)184-136(225)102(60-84-38-42-88(199)43-39-84)177-138(227)106(63-117(208)209)179-143(232)110(70-193)185-148(237)121(79(10)196)188-140(229)104(58-82-29-18-15-19-30-82)181-147(236)120(78(9)195)186-113(201)67-162-126(215)95(44-48-112(156)200)169-141(230)108(68-191)182-125(214)90(155)62-86-66-159-72-163-86/h14-21,27-32,36-43,65-66,72-80,90,92-111,119-122,161,191-199H,22-26,33-35,44-64,67-71,153-155H2,1-13H3,(H2,156,200)(H,159,163)(H,162,215)(H,164,216)(H,165,240)(H,166,213)(H,167,212)(H,168,231)(H,169,230)(H,170,219)(H,171,222)(H,172,235)(H,173,224)(H,174,226)(H,175,217)(H,176,220)(H,177,227)(H,178,218)(H,179,232)(H,180,223)(H,181,236)(H,182,214)(H,183,221)(H,184,225)(H,185,237)(H,186,201)(H,187,228)(H,188,229)(H,189,233)(H,190,234)(H,202,203)(H,204,205)(H,206,207)(H,208,209)(H,210,211)(H,238,239)(H4,157,158,160)/t76-,77-,78+,79+,80+,90-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,119-,120-,121-,122-/m0/s1

2.1.3 InChI Key

RZRMFQMNPDPAIX-AJTOSFMRSA-N

2.1.4 Canonical SMILES

CC(C)CC(C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(C(C)O)C(=O)O)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCCN)NC(=O)C(C(C)C)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(C)(C)NC(=O)C(CC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CC5=CC=C(C=C5)O)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(C(C)O)NC(=O)CNC(=O)C(CCC(=O)N)NC(=O)C(CO)NC(=O)C(CC7=CNC=N7)N

2.1.5 Isomeric SMILES

C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC=N7)N)O

2.2 Synonyms

2.2.1 MeSH Synonyms

1. Zegalogue

2.2.2 Depositor-Supplied Synonyms

1. 1544300-84-6

2. Dasiglucagon [inn]

3. Dasiglucagon [usan]

4. Dasiglucagon [who-dd]

5. Dasiglucagon [usan:inn]

6. Unii-ad4j2o47fq

7. Ad4j2o47fq

8. Zp-ga-1

9. Dtxsid501336774

10. Zp4207

11. Zp-4207

12. 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

13. 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

2.3 Create Date

2017-05-07

3 Chemical and Physical Properties

Molecular Formula	C₁₅₂H₂₂₂N₃₈O₅₀
Molecular Weight	3381.6 g/mol
XLogP3	-15.9
Hydrogen Bond Donor Count	52
Hydrogen Bond Acceptor Count	55
Rotatable Bond Count	110
Exact Mass	3380.6030550 g/mol
Monoisotopic Mass	3379.5997002 g/mol
Topological Polar Surface Area	1450 Å²
Heavy Atom Count	240
Formal Charge	0
Complexity	7900
Isotope Atom Count	0
Defined Atom Stereocenter Count	30
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug 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.

Treatment of hypoglycaemia

5 Pharmacology and Biochemistry

5.1 Pharmacology

Dasiglucagon works to increase blood glucose levels under normal and hypoglycemic conditions. 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.

5.2 FDA Pharmacological Classification

5.2.1 Pharmacological Classes

Glucagon Receptor Agonists [MoA]; Increased Glycogenolysis [PE]; Antihypoglycemic Agent [EPC]

5.3 Absorption, Distribution and Excretion

Absorption

Following subcutaneous administration of 0.6 mg dasiglucagon, the mean peak plasma concentration was 5110 pg/mL (1510 pmol/L). T_max was 35 minutes. In pediatric patients with type 1 diabetes, the mean peak plasma concentration of 3920 pg/mL occurred at around 21 minutes. Dasiglucagon has a higher absorption rate than traditional reconstituted glucagon.

Volume of Distribution

The mean apparent volume of distribution ranged from 47 L to 57 L after subcutaneous administration.

5.4 Metabolism/Metabolites

Like endogenous glucagon, dasiglucagon undergoes proteolytic degradation pathways in blood, liver, and kidney.

5.5 Biological Half-Life

The half-life was approximately 30 minutes following subcutaneous administration. Dasiglucagon has a longer plasma elimination half-life than traditional reconstituted glucagon.

5.6 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 Gs and Gq, and consequently, adenylate cyclase. Adenyl cyclase increases intracellular cyclic AMP, which stimulates glycogenolysis and glucogenesis in the liver. As glucose is primarily released from liver glycogen stores, hepatic stores of glycogen are crucial for dasiglucagon to exert its antihypoglycemic effects.

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