Dasiglucagon

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Dasiglucagon
Names
Trade namesZegalogue
  • (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]
Routes of
use
Subcutaneous
Typical dose0.6 mg[1]
External links
AHFS/Drugs.comMonograph
US NLMDasiglucagon
Legal
License data
Legal status
Chemical and physical data
FormulaC152H222N38O50
Molar mass3381.664 g·mol−1
3D model (JSmol)
  • 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=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. 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 1.12 1.13 1.14 1.15 "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 links

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