Dasiglucagon

Dasiglucagon
Names
Trade namesZegalogue
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
Clinical data
Drug classGlucagon receptor agonist
Main usesLow blood sugar in diabetes[1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Routes of
use		Subcutaneous
Typical dose0.6 mg[1]
External links
AHFS/Drugs.comMonograph
Legal
License data
Legal status
Chemical and physical data
FormulaC152H222N38O50
Molar mass3381.664 g·mol−1
3D model (JSmol)
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
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
  • Key:RZRMFQMNPDPAIX-AJTOSFMRSA-N

Dasiglucagon, sold under the brand name Zegalogue, is a medication used to treat severe low blood sugar in people with diabetes.[1][2] It may be used in those who are at least six years old.[1] It is given by injection under the skin.[1]

Common side effects include nausea, vomiting, headache, diarrhea, and injection site pain.[1] Other side effects may include allergic reactions.[1] In people with a pheochromocytoma it may increase blood pressure while in people with an insulinoma it may result in worsening low blood sugar.[1] While there is no evidence of harm in pregnancy, such use has not been well studied.[1] It is a glucagon receptor agonist.[1]

Dasiglucagon was approved for medical use in the United States in 2021.[1] It is not approved in Europe or the United Kingdom as of 2022.[3] In the United States it costs about 320 USD per dose as of 2022.[4] Glucagon, in comparison, costs about 90 USD.[5]

Medical uses

Dasiglucagon is indicated for the treatment of severe hypoglycemia in people aged six years of age and older with diabetes.[1][6] It appears to be similar in effectiveness to glucagon.[7]

It may not work in those with low liver glycogen reserves such as in starvation.[8]

Dosage

It is used at a dose of 0.6 mg.[1] A second dose may be given after 15 minutes.[1]

Contraindications

Dasiglucagon is contraindicated in people with pheochromocytoma or insulinoma.[1]

History

It was designated an orphan drug in the USA in August 2017.[9]

References

  1. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 "Zegalogue- dasiglucagon injection, solution". DailyMed. Archived from the original on 23 May 2021. Retrieved 22 May 2021.
  2. ↑ Li S, Hu Y, Tan X, Wang D, Hu J, Zou P, Wang L (August 2020). "Evaluating dasiglucagon as a treatment option for hypoglycemia in diabetes". Expert Opinion on Pharmacotherapy. 21 (11): 1311–1318. doi:10.1080/14656566.2020.1747432. PMID 32267182. S2CID 215405434.
  3. ↑ "Dasiglucagon". SPS - Specialist Pharmacy Service. 27 March 2018. Archived from the original on 28 January 2022. Retrieved 30 October 2022.
  4. ↑ "Zegalogue". Archived from the original on 30 October 2022. Retrieved 30 October 2022.
  5. ↑ "Glucagon". Archived from the original on 30 October 2022. Retrieved 30 October 2022.
  6. ↑ "Dasiglucagon: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 22 March 2021. Retrieved 22 March 2021.
  7. ↑ Pieber, TR; Aronson, R; Hövelmann, U; Willard, J; Plum-Mörschel, L; Knudsen, KM; Bandak, B; Tehranchi, R (1 June 2021). "Dasiglucagon-A Next-Generation Glucagon Analog for Rapid and Effective Treatment of Severe Hypoglycemia: Results of Phase 3 Randomized Double-Blind Clinical Trial". Diabetes care. 44 (6): 1361–1367. doi:10.2337/dc20-2995. PMID 35239971.
  8. ↑ "Dasiglucagon Monograph for Professionals". Drugs.com. Retrieved 30 October 2022.
  9. ↑ "Dasiglucagon Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 10 August 2017. Archived from the original on 17 April 2021. Retrieved 22 March 2021.
External sites:
Identifiers:
  • Clinical trial number NCT03378635 for "A Trial to Confirm the Efficacy and Safety of Dasiglucagon in the Treatment of Hypoglycemia in Type 1 Diabetes Subjects" at ClinicalTrials.gov
  • Clinical trial number NCT03688711 for "Trial to Confirm the Clinical Efficacy and Safety of Dasiglucagon in the Treatment of Hypoglycemia in Subjects With T1DM" at ClinicalTrials.gov
  • Clinical trial number NCT03667053 for "Trial to Confirm the Efficacy and Safety of Dasiglucagon in the Treatment of Hypoglycemia in T1DM Children" at ClinicalTrials.gov


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