Susineridine

Pharmaceutical compound From Wikipedia, the free encyclopedia

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]

Quick facts Clinical data, Other names ...
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
Close

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

References

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