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Susineridine

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Susineridine
Clinical data
Other namesYZJ-4729; YZJ4729
Routes of
administration		Intravenous[1][2]
Drug classμ-Opioid receptor biased partial agonist; Analgesic
Pharmacokinetic data
Elimination half-life0.9–2.5 hours[2][3]
Identifiers
  • 6-propan-2-yl-N-[2-[(9R)-9-pyridin-2-yl-6-oxaspiro[4.5]decan-9-yl]ethyl]-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-4-amine
CAS Number
PubChem CID
Chemical and physical data
FormulaC25H36N4O
Molar mass408.590 g·mol−1
3D model (JSmol)
  • CC(C)C1CC(C2=CC=NN12)NCC[C@]3(CCOC4(C3)CCCC4)C5=CC=CC=N5
  • InChI=1S/C25H36N4O/c1-19(2)22-17-20(21-8-14-28-29(21)22)26-15-11-24(23-7-3-6-13-27-23)12-16-30-25(18-24)9-4-5-10-25/h3,6-8,13-14,19-20,22,26H,4-5,9-12,15-18H2,1-2H3/t20?,22?,24-/m1/s1
  • Key:RUHISKJCCSWSHB-LLAFXHEGSA-N

Susineridine (INNTooltip International Nonproprietary Name; developmental code name YZJ-4729) is an atypical μ-opioid receptor (MOR) agonist and opioid analgesic which is under development for the treatment of postoperative pain.[1][4][2][3] It is given intravenously.[1]

The drug acts as a selective biased partial agonist of the MOR, with functional selectivity for activation of G protein signaling over β-arrestin2 recruitment.[2][3] Its mechanism of action and pharmacological activity are said to be similar to those of oliceridine.[2][3] However, in-vitro findings suggest that susineridine may have a greater degree of G protein bias than oliceridine.[2] The drug produces analgesic effects in multiple animal models of pain and produces less respiratory depression than morphine or oliceridine.[2][3] The pharmacokinetics of susineridine in humans have been studied.[2][3]

Susineridine was patented[5] and first described in the scientific literature in 2023.[2][3] It is under development by Shanghai Haiyan Pharmaceutical Technology in China.[1][4] As of May 2025, the drug is in phase 3 clinical trials for postoperative pain.[1][4]

See also

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References

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  1. ^ a b c d e "YZJ 4729". AdisInsight. Springer Nature Switzerland AG. 2 April 2025. Retrieved 19 February 2026.
  2. ^ a b c d e f g h i Ni Y, Gao H, Ouyang W, Yang G, Cheng M, Ding L (2023). "Pharmacokinetics, metabolite profiling, safety and tolerability of YZJ-4729 tartrate, a novel G protein-biased μ-opioid receptor agonist, in healthy Chinese subjects". Frontiers in Pharmacology. 14 1295319. doi:10.3389/fphar.2023.1295319. PMC 10803517. PMID 38264529.
  3. ^ a b c d e f g Ni Y, Ding C, Cheng M, Ding L (September 2025). "Development and validation of an LC-MS/MS method for quantifying a new G protein selective μ-opioid receptor agonist YZJ-4729 and its major metabolite M10 in human plasma to support a phase I study in healthy subjects". Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences. 1263 124714. doi:10.1016/j.jchromb.2025.124714. PMID 40577954.
  4. ^ a b c "Delving into the Latest Updates on YZJ-4729 with Synapse". Synapse. 30 August 2025. Retrieved 19 February 2026.
  5. ^ US 2023/0128062A1, Hu B, Xie J, Zhang K, Yang W, Shi X, Guan H, "Azabicyclic substituted oxaspiro derivative, preparation method therefor and medical use thereof", published 27 April 2023, assigned to Yangtze River Pharmaceutical Group Co Ltd and Shanghai Haiyan Pharmaceutical Technology Co Ltd