Zagociguat

Zagociguat
Clinical data
Other namesCY-6463; CY6463; IW-6463; IW6463
Routes of
administration		Oral[1][2]
Drug classSoluble guanylate cyclase (sGC) stimulator
Pharmacokinetic data
Elimination half-life52.8–67.1 hours[2]
Identifiers
  • 8-[(2-fluorophenyl)methyl]-6-[5-(trifluoromethyl)-1H-1,2,4-triazol-3-yl]imidazo[1,2-a]pyrazine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC16H10F4N6
Molar mass362.292 g·mol−1
3D model (JSmol)
  • C1=CC=C(C(=C1)CC2=NC(=CN3C2=NC=C3)C4=NNC(=N4)C(F)(F)F)F
  • InChI=1S/C16H10F4N6/c17-10-4-2-1-3-9(10)7-11-14-21-5-6-26(14)8-12(22-11)13-23-15(25-24-13)16(18,19)20/h1-6,8H,7H2,(H,23,24,25)
  • Key:GTKNNCQKFKGSHR-UHFFFAOYSA-N

Zagociguat (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code names CY-6463 and IW-6463) is a brain-penetrant soluble guanylate cyclase (sGC) stimulator which is under development for the treatment of Alzheimer's disease, MELAS syndrome, mitochondrial disorders, dementia, and schizophrenia.[1][3][4][2][5] It is taken orally.[1][2] The drug shows pro-cognitive-like and neuroprotective effects in preclinical research.[4][6] Zagociguat was originated by Ironwood Pharmaceuticals and is under development by Cyclerion Therapeutics and/or Tisento Therapeutics.[1][3] As of January 2026, it is in phase 2 clinical trials for Alzheimer's disease, MELAS syndrome, and mitochondrial disorders, whereas no recent development has been reported for dementia or schizophrenia.[1][3]

See also

References

  1. 1 2 3 4 5 "Cyclerion Therapeutics". AdisInsight. 15 January 2026. Retrieved 7 June 2026.
  2. 1 2 3 4 van Kraaij SJ, Gal P, Borghans LG, Klaassen ES, Dijkstra F, Winrow C, et al. (August 2023). "First-in-human trial to assess safety, tolerability, pharmacokinetics, and pharmacodynamics of zagociguat (CY6463), a CNS-penetrant soluble guanylyl cyclase stimulator". Clinical and Translational Science. 16 (8): 1381–1395. doi:10.1111/cts.13537. PMC 10432884. PMID 37118895.
  3. 1 2 3 "Delving into the Latest Updates on Zagociguat with Synapse". Synapse. 3 April 2026. Retrieved 7 June 2026.
  4. 1 2 Correia SS, Iyengar RR, Germano P, Tang K, Bernier SG, Schwartzkopf CD, et al. (2021). "The CNS-Penetrant Soluble Guanylate Cyclase Stimulator CY6463 Reveals its Therapeutic Potential in Neurodegenerative Diseases". Frontiers in Pharmacology. 12 656561. doi:10.3389/fphar.2021.656561. PMC 8181742. PMID 34108877.
  5. ↑ van Kraaij SJ, Borghans L, Klaassen ES, Gal P, van der Grond J, Tripp K, et al. (December 2023). "Randomized placebo-controlled crossover study to assess tolerability and pharmacodynamics of zagociguat, a soluble guanylyl cyclase stimulator, in healthy elderly". British Journal of Clinical Pharmacology. 89 (12): 3606–3617. doi:10.1111/bcp.15861. hdl:1887/3753495. PMID 37488930.
  6. ↑ Burg L, Yoon H, Peng M, Germano P, Reesey Gretzmacher E, Xiao R, et al. (2025). "Zagociguat prevented stressor-induced neuromuscular dysfunction, improved mitochondrial physiology, and increased exercise capacity in diverse mitochondrial respiratory chain disease zebrafish models". Frontiers in Pharmacology. 16 1588426. doi:10.3389/fphar.2025.1588426. PMC 12332506. PMID 40786033.
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